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Synthesis and structure-activity relationship studies of 2-(N-substituted)-aminobenzimidazoles as potent negative gating modulators ofsmall conductance Ca2+-activated K+ channels.
J Med Chem 51: 7625-34 (2009)
Neurosearch
Design, Structure-Activity Relationships, X-ray Crystal Structure, and Energetic Contributions of a Critical P1 Pharmacophore: 3-Chloroindole-7-yl-Based Factor Xa Inhibitors.
J Med Chem 51: 7541-51 (2008)
Bristol-Myers Squibb
Novel potent and highly selective human A(3) adenosine receptor antagonists belonging to the 4-amido-2-arylpyrazolo[3,4-c]quinoline series: molecular docking analysis and pharmacological studies.
Bioorg Med Chem 17: 401-10 (2008)
Università
Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 18: 6525-9 (2008)
Korea Research Institute Of Chemical Technology
Synthesis and biological evaluation of helicid analogues as mushroom tyrosinase inhibitors.
Bioorg Med Chem Lett 18: 6490-3 (2008)
Sun Yat-Sen University
Synthesis and biological evaluation of novel sulfonyl-naphthalene-1,4-diols as FabH inhibitors.
Bioorg Med Chem Lett 18: 6402-5 (2008)
Portland State University
1-Deoxygalactonojirimycin-lysine hybrids as potent D-galactosidase inhibitors.
Bioorg Med Chem 16: 10216-20 (2008)
Technische UniversitäT Graz
C-2-aryl O-substituted HI-236 derivatives as non-nucleoside HIV-1 reverse-transcriptase inhibitors.
Bioorg Med Chem 16: 10270-80 (2008)
University Of Cape Town
Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN).
Bioorg Med Chem 16: 9984-90 (2008)
Shandong University
Convergent synthesis and cruzain inhibitory activity of novel 2-(N'-benzylidenehydrazino)-4-trifluoromethyl-pyrimidines.
Bioorg Med Chem 16: 10236-43 (2008)
Universidade Federal De Santa Maria
Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.
Bioorg Med Chem Lett 18: 6390-3 (2008)
The Scripps Research Institute-Florida
The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing.
Bioorg Med Chem Lett 18: 6369-73 (2008)
Astrazeneca Pharmaceuticals
Natural polyprenylated benzophenones inhibiting cysteine and serine proteases.
Eur J Med Chem 44: 1230-9 (2009)
Federal University Of Alfenas
Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity, part 1.
Eur J Med Chem 44: 1710-7 (2009)
Medical University Of Warsaw
Carbonic anhydrase inhibitors. Inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with anions.
Bioorg Med Chem Lett 18: 6327-31 (2008)
Balikesir University
Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.
Bioorg Med Chem Lett 18: 6352-6 (2008)
Amgen
Beta-C-glycosiduronic acids and beta-C-glycosyl compounds: new PTP1B inhibitors.
Bioorg Med Chem Lett 18: 6348-51 (2008)
Cnrs
Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists.
Bioorg Med Chem Lett 18: 6357-61 (2008)
Piramal Life Sciences
11C-labelled PIB analogues as potential tracer agents for in vivo imaging of amyloid beta in Alzheimer's disease.
Eur J Med Chem 44: 1415-26 (2009)
K.U. Leuven
Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology.
Bioorg Med Chem Lett 18: 6398-401 (2008)
Kitasato University
Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV.
Bioorg Med Chem Lett 18: 6332-5 (2008)
Ecole Nationale Sup£Rieure De Chimie De Montpellier
Chroman-3-amides as potent Rho kinase inhibitors.
Bioorg Med Chem Lett 18: 6406-9 (2008)
The Scripps Research Institute
Structure-activity relationships of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the treatment of cough.
Bioorg Med Chem Lett 18: 6340-3 (2008)
Schering-Plough Research Institute
Synthesis and structure-activity relationship of 7-azaindole piperidine derivatives as CCR2 antagonists.
Bioorg Med Chem Lett 18: 6468-70 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Rational design of novel glycomimetics: inhibitors of concanavalin A.
Bioorg Med Chem Lett 18: 6573-5 (2008)
Georgia Southern University
Molecular-targeted antitumor agents. 19. Furospongolide from a marine Lendenfeldia sp. sponge inhibits hypoxia-inducible factor-1 activation in breast tumor cells.
J Nat Prod 71: 1854-60 (2008)
University Of Mississippi
Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists.
J Med Chem 51: 7370-9 (2009)
Glaxosmithkline
Novel acetylcholine and carbamoylcholine analogues: development of a functionally selective alpha4beta2 nicotinic acetylcholine receptor agonist.
J Med Chem 51: 7380-95 (2009)
University Of Copenhagen
Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.
Bioorg Med Chem Lett 18: 6486-9 (2008)
Astrazeneca Pharmaceuticals
Antityrosinase and Antioxidant Effects of ent-Kaurane Diterpenes from Leaves of Broussonetia papyrifera.
J Nat Prod 71: 1930-1933 (2008)
Tajen University
Discovery and development of fatty acid amide hydrolase (FAAH) inhibitors.
J Med Chem 51: 7327-43 (2009)
Johnson & Johnson Pharmaceutical Research And Development
Nicotinic acid receptor agonists.
J Med Chem 51: 7653-62 (2008)
Arena Pharmaceuticals
Discovery of Boronic Acids as Novel and Potent Inhibitors of Fatty Acid Amide Hydrolase.
J Med Chem 51: 7057-60 (2008)
University Of Oxford
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia.
J Med Chem 51: 7094-8 (2008)
Abbott Laboratories
Identification of small molecule agonists of the motilin receptor.
Bioorg Med Chem Lett 18: 6423-8 (2008)
Glaxosmithkline
Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists.
Bioorg Med Chem Lett 18: 6437-40 (2008)
Pfizer
Pyrazoline-based mycobactin analogues as MAO-inhibitors.
Bioorg Med Chem Lett 18: 6362-8 (2008)
Institute Of Technology
Irreversible inhibition of dihydrodipicolinate synthase by 4-oxo-heptenedioic acid analogues.
Bioorg Med Chem 16: 9975-83 (2008)
University Of Melbourne
Modeling the activity of furin inhibitors using artificial neural network.
Eur J Med Chem 44: 1664-73 (2009)
Mahidol University
Discovery of new pyridoacridine alkaloids from Lissoclinum cf. badium that inhibit the ubiquitin ligase activity of Hdm2 and stabilize p53.
Bioorg Med Chem 16: 10022-8 (2008)
National Cancer Institute-Frederick
The importance of CH/pi hydrogen bonds in rational drug design: An ab initio fragment molecular orbital study to leukocyte-specific protein tyrosine (LCK) kinase.
Bioorg Med Chem 16: 10311-8 (2008)
Kissei Pharmaceutical
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 3: Synthesis and activity of isosteric analogs.
Bioorg Med Chem Lett 18: 6444-7 (2008)
Shionogi
Characterization of novel furan compounds on the basis of their radical scavenging activity and cytoprotective effects against glutamate- and lipopolysaccharide-induced insults.
Bioorg Med Chem 16: 10332-7 (2008)
National Institute Of Advanced Industrial Science And Technology (Aist)
Synthesis and biological evaluation of guanylhydrazone coactivator binding inhibitors for the estrogen receptor.
Bioorg Med Chem 16: 10075-84 (2008)
University Of Illinois At Urbana-Champaign
Inhibition of aldose reductase from cataracted eye lenses by finger millet (Eleusine coracana) polyphenols.
Bioorg Med Chem 16: 10085-90 (2008)
Central Food Technological Research Institute
Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity.
Bioorg Med Chem 16: 9911-24 (2008)
Universit£
Synthesis and biological activities of novel nonpeptide angiotensin II receptor antagonists based on benzimidazole derivatives bearing a heterocyclic ring.
Bioorg Med Chem 16: 10301-10 (2008)
Chinese Academy Of Sciences
Modulation of PPAR receptor subtype selectivity of the ligands: aliphatic chain vs aromatic ring as a spacer between pharmacophore and the lipophilic moiety.
Bioorg Med Chem Lett 18: 6471-5 (2008)
Zydus Research Centre
Synthesis and evaluation of a series of homologues of lobelane at the vesicular monoamine transporter-2.
Bioorg Med Chem Lett 18: 6509-12 (2008)
University Of Kentucky
Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction.
Bioorg Med Chem Lett 18: 6279-82 (2008)
Chong Kun Dang Research Institute
Receptor-based 3D-QSAR studies of checkpoint Wee1 kinase inhibitors.
Eur J Med Chem 44: 1383-95 (2009)
Chulalongkorn University
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.
J Med Chem 51: 7075-93 (2009)
Metabasis Therapeutics
Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: mapping of the receptor binding pocket by in silico docking studies.
J Med Chem 51: 7273-86 (2009)
Glaxosmithkline
N-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2).
Bioorg Med Chem Lett 18: 6454-7 (2008)
Wyeth Research
Topological descriptors in modeling the agonistic activity of human A3 adenosine receptor ligands: the derivatives of 2-chloro-N(6)-substituted-4'-thioadenosine-5'-uronamide.
Eur J Med Chem 44: 1377-82 (2009)
Sobhasaria Engineering College
Scalarane sesterterpenes from the sponge Smenospongia sp.
J Nat Prod 71: 1866-71 (2008)
Seoul National University
Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride Synthesis
J Med Chem 51: 7161-8 (2008)
Wyeth Research
Structural Requirements for Eszopiclone and Zolpidem Binding to the gamma-Aminobutyric Acid Type-A (GABAA) Receptor Are Different.
J Med Chem 51: 7243-52 (2008)
University Of Wisconsin At Madison
Identification of pharmacological chaperones for Gaucher disease and characterization of their effects on beta-glucocerebrosidase by hydrogen/deuterium exchange mass spectrometry.
Chembiochem 9: 2650-62 (2008)
Research Institute, Hospital For Sick Children
Quantitative three dimensional structure linear interaction energy model of 5'-O-[N-(salicyl)sulfamoyl]adenosine and the aryl acid adenylating enzyme MbtA.
J Med Chem 51: 7154-60 (2009)
University Of Minnesota
Fragment-based design of small molecule X-linked inhibitor of apoptosis protein inhibitors.
J Med Chem 51: 7111-8 (2008)
Burnham Institute For Medical Research
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
Antimicrob Agents Chemother 53: 186-92 (2009)
Daiichi Sankyo
Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.
Bioorg Med Chem Lett 18: 6062-6 (2008)
Roche Palo Alto
Alpha-mercaptoketone based histone deacetylase inhibitors.
Bioorg Med Chem Lett 18: 6482-5 (2008)
Kalypsys
Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor.
Bioorg Med Chem Lett 18: 6093-6 (2008)
Kalypsys
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics.
Bioorg Med Chem Lett 18: 6151-5 (2008)
Neurocrine Biosciences
Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity.
J Med Chem 51: 7216-33 (2009)
Green Cross
Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP).
J Med Chem 51: 7169-80 (2008)
University Of Michigan
Bis-pyranobenzoquinones as a new family of reversal agents of the multidrug resistance phenotype mediated by P-glycoprotein in mammalian cells and the protozoan parasite Leishmania.
J Med Chem 51: 7132-43 (2009)
Instituto Universitario De Bio-OrgáNica Antonio GonzáLez
Antithyroid drug carbimazole and its analogues: synthesis and inhibition of peroxidase-catalyzed iodination of L-tyrosine.
J Med Chem 51: 7313-7 (2009)
Institute Of Science
Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.
J Med Chem 51: 7265-72 (2009)
Neurocrine Biosciences
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
J Med Chem 51: 7308-12 (2009)
University Of Bologna
Design, synthesis, and pharmacological evaluation of N-bicyclo-5-chloro-1H-indole-2-carboxamide derivatives as potent glycogen phosphorylase inhibitors.
Bioorg Med Chem 16: 10001-12 (2008)
Astellas Pharma
Substituted hippurates and hippurate analogs as substrates and inhibitors of peptidylglycine alpha-hydroxylating monooxygenase (PHM).
Bioorg Med Chem 16: 10061-74 (2008)
University Of South Florida
Identification of 4-[1-[3-chloro-4-[N'-(5-fluoro-2-methylphenyl)ureido]phenylacetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]benzoic acid as a potent, orally active VLA-4 antagonist.
Bioorg Med Chem 16: 9991-10000 (2008)
Daiichi Sankyo
Antiobesity designed multiple ligands: Synthesis of pyrazole fatty acid amides and evaluation as hypophagic agents.
Bioorg Med Chem 16: 10098-105 (2008)
Polymer Functionalization Group (Ictp, Csic)
Search for alpha-helical propensity in the receptor-bound conformation of glucagon-like peptide-1.
Bioorg Med Chem 16: 10106-12 (2008)
University Of Texas At Dallas
Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin.
Bioorg Med Chem 16: 10049-60 (2008)
Kyoto Pharmaceutical University
Activation and inhibition of leukotriene A4 hydrolase aminopeptidase activity by diphenyl ether and derivatives.
Bioorg Med Chem Lett 18: 6549-52 (2008)
Peking University
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.
Bioorg Med Chem Lett 18: 6097-9 (2008)
Glaxosmithkline
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Bioorg Med Chem Lett 18: 6041-5 (2008)
Tsukuba Research Institute
Synthesis of trans-caffeate analogues and their bioactivities against HIV-1 integrase and cancer cell lines.
Bioorg Med Chem Lett 18: 6553-7 (2008)
Zhejiang University
Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.
Bioorg Med Chem Lett 18: 6078-82 (2008)
Irbm-Merck Research Laboratories Rome
Synthesis of alkenyldiarylmethanes (ADAMs) containing benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Eur J Med Chem 44: 1210-4 (2009)
Purdue University
The contribution of plukenetione A to the anti-tumoral activity of Cuban propolis.
Bioorg Med Chem 16: 9635-43 (2008)
Ruhr-University Of Bochum
Synthesis, structure-activity relationships and molecular modeling studies of new indole inhibitors of monoamine oxidases A and B.
Bioorg Med Chem 16: 9729-40 (2008)
Sapienza University Of Rome
SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Bioorg Med Chem Lett 18: 6104-9 (2008)
Merck Research Laboratories
Possible involvement of radical intermediates in the inhibition of cysteine proteases by allenyl esters and amides.
Bioorg Med Chem Lett 18: 6202-5 (2008)
University Of Toyama
Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation.
Bioorg Med Chem Lett 18: 6071-7 (2008)
Pfizer
Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule.
Bioorg Med Chem Lett 18: 6033-6 (2008)
Pfizer
Synthesis of some pyrazolyl benzenesulfonamide derivatives as dual anti-inflammatory antimicrobial agents.
J Enzyme Inhib Med Chem 24: 296-309 (2009)
University Of Alexandria
Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.
Bioorg Med Chem Lett 18: 6067-70 (2008)
Wyeth Research
Influence of selective fluorination on the biological activity and proteolytic stability of glucagon-like peptide-1.
J Med Chem 51: 7303-7 (2009)
Tufts University
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.
J Med Chem 51: 7193-204 (2009)
University Of Regensburg
Quantitative structure-activity relationship of phenoxyphenyl-methanamine compounds with 5HT2A, SERT, and hERG activities.
Bioorg Med Chem Lett 18: 6088-92 (2008)
Pfizer
Interaction of ladder-shaped polyethers with transmembrane alpha-helix of glycophorin A as evidenced by saturation transfer difference NMR and surface plasmon resonance.
Bioorg Med Chem Lett 18: 6115-8 (2008)
Osaka University
Exploring 8-benzyl pteridine-6,7-diones as inhibitors of glutamate racemase (MurI) in gram-positive bacteria.
Bioorg Med Chem Lett 18: 6100-3 (2008)
Astrazeneca R&D Boston
The discovery of equipotent PPARalpha/gamma dual activators.
Bioorg Med Chem Lett 18: 6251-4 (2008)
Glaxosmithkline
Potent benzimidazolone-based CGRP receptor antagonists.
Bioorg Med Chem Lett 18: 6122-5 (2008)
Merck
Virtual screening for Raf-1 kinase inhibitors based on pharmacophore model of substituted ureas.
Eur J Med Chem 44: 1240-9 (2009)
China Pharmaceutical University
Lead Optimization of 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A Adenosine Receptor Antagonists for the Treatment of Parkinson's Disease.
J Med Chem 51: 7099-7110 (2008)
Neurocrine Bioscience
Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes.
J Med Chem 51: 7061-4 (2009)
University Of Southern Denmark
Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.
Bioorg Med Chem Lett 18: 6562-7 (2008)
Pfizer
Validation of high-affinity binding sites for succinic acid through distinguishable binding of gamma-hydroxybutyric acid receptor-specific NCS 382 antipodes.
Bioorg Med Chem Lett 18: 6290-2 (2008)
Hungarian Academy Of Sciences
Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.
Bioorg Med Chem Lett 18: 6142-6 (2008)
Novartis
Synthesis of celecoxib analogs that possess a N-hydroxypyrid-2(1H)one 5-lipoxygenase pharmacophore: biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
Bioorg Med Chem Lett 18: 6138-41 (2008)
University Of Alberta
Design and Synthesis of Orally Bioavailable Benzimidazoles as Raf Kinase Inhibitors.
J Med Chem 51: 7049-52 (2008)
Novartis
Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases.
J Med Chem 51: 7053-6 (2008)
University Of Oxford
Cobalt-alkyne complexes with imidazoline ligands as estrogenic carriers: synthesis and pharmacological investigations.
J Med Chem 51: 7318-22 (2009)
Freie Universitat Berlin
Monodictyochromes A and B, Dimeric Xanthone Derivatives from the Marine Algicolous Fungus Monodictys putredinis.
J Nat Prod 71: 1793-1799 (2008)
University Of Bonn
1,3-Dialkyl-8-(hetero)aryl-9-OH-9-deazaxanthines as potent A2B adenosine receptor antagonists: design, synthesis, structure-affinity and structure-selectivity relationships.
Bioorg Med Chem 16: 9780-9 (2008)
Università
Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).
Bioorg Med Chem Lett 18: 6231-5 (2008)
Vertex Pharmaceuticals
Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for neuronal nicotinic acetylcholine receptors.
Bioorg Med Chem Lett 18: 6147-50 (2008)
Università
Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism.
J Med Chem 51: 6800-7 (2008)
Universita Di Ferrara
The design, synthesis and biological evaluation of 7-alkoxy-4-heteroarylamino-3-cyanoquinolines as dual inhibitors of c-Src and iNOS.
Bioorg Med Chem Lett 18: 6206-9 (2008)
China Pharmaceutical University
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-hydroxymethylphenyl)-1-(4-aminosulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its methanesulfonyl analog: synthesis, biological evaluation and nitric oxide release studies.
Bioorg Med Chem 16: 9694-8 (2008)
University Of Alberta
2-Aminobenzimidazoles as potent ITK antagonists: trans-stilbene-like moieties targeting the kinase specificity pocket.
Bioorg Med Chem Lett 18: 6218-21 (2008)
Boehringer Ingelheim Pharmaceuticals
2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors.
Bioorg Med Chem Lett 18: 6083-7 (2008)
Irbm-Merck Research Laboratories Rome
Synthetic chalcones as efficient inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase PtpA.
Bioorg Med Chem Lett 18: 6227-30 (2008)
Universidade Federal De Santa Catarina
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.
Bioorg Med Chem Lett 18: 6273-8 (2008)
Pfizer
Synthesis of new sulfonate and phosphonate derivatives for cation-independent mannose 6-phosphate receptor targeting.
Bioorg Med Chem Lett 18: 6240-3 (2008)
University Of Montpellier
Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.
Bioorg Med Chem Lett 18: 6214-7 (2008)
Glaxosmithkline
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.
Eur J Med Chem 44: 2361-71 (2009)
Sterling Road
New diterpenoids and the bioactivity of Erythrophleum fordii.
Bioorg Med Chem 16: 9867-70 (2008)
National Cheng Kung University
Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.
Bioorg Med Chem Lett 18: 6222-6 (2008)
Glaxosmithkline
Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.
Bioorg Med Chem Lett 18: 6236-9 (2008)
Sunesis Pharmaceuticals
Structure-activity relationship studies of phenanthridine-based Bcl-XL inhibitors.
J Med Chem 51: 6699-710 (2008)
A* Star
Identification of a new JNK inhibitor targeting the JNK-JIP interaction site.
Proc Natl Acad Sci U S A 105: 16809-13 (2008)
Burnham Institute For Medical Research
Synthesis of triazole-linked beta-C-glycosyl dimers as inhibitors of PTP1B.
Bioorg Med Chem 16: 9757-63 (2008)
Cnrs
Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.
Bioorg Med Chem Lett 18: 5819-23 (2009)
Johnson & Johnson Prd
2-Aryloxymethylmorpholine histamine H(3) antagonists.
Bioorg Med Chem Lett 18: 5796-9 (2009)
Johnson & Johnson Pharmaceutical Research & Development
Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.
J Med Chem 51: 7010-4 (2008)
Pfizer
Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1).
J Med Chem 51: 6725-39 (2008)
Saarland University
Structure-based virtual screening and biological evaluation of Mycobacterium tuberculosis adenosine 5'-phosphosulfate reductase inhibitors.
J Med Chem 51: 6627-30 (2008)
The Scripps Research Institute
1,5-benzodiazepines, a novel class of hepatitis C virus polymerase nonnucleoside inhibitors.
Antimicrob Agents Chemother 52: 4420-31 (2008)
Tibotec
Targeting the X-linked inhibitor of apoptosis protein through 4-substituted azabicyclo[5.3.0]alkane smac mimetics. Structure, activity, and recognition principles.
J Mol Biol 384: 673-89 (2008)
University Of Milano
Modular synthesis of non-peptidic bivalent NPY Y1 receptor antagonists.
Bioorg Med Chem 16: 9858-66 (2008)
UniversitäT Regensburg
Tetrakis-azaaromatic quaternary ammonium salts: novel subtype-selective antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release.
Bioorg Med Chem Lett 18: 5753-7 (2009)
University Of Kentucky
Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABA(A) receptors.
Bioorg Med Chem Lett 18: 5713-6 (2009)
Lund University
Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines.
Bioorg Med Chem Lett 18: 5717-21 (2009)
Astrazeneca
Open-chain half-bastadins mimic the effects of cyclic bastadins on calcium homeostasis in cultured neurons.
Bioorg Med Chem Lett 18: 5734-7 (2009)
Polish Academy Of Sciences
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.
Nat Chem Biol 4: 700-7 (2008)
The Scripps Research Institute
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Nat Chem Biol 4: 691-9 (2008)
University Of California San Francisco
Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist.
Bioorg Med Chem 16: 9817-29 (2008)
Tsukuba Research Institute
The identification of neurotensin NTS1 receptor partial agonists through a ligand-based virtual screening approach.
Bioorg Med Chem Lett 18: 5789-91 (2009)
Wyeth Research
Practical synthesis of bredemolic acid, a natural inhibitor of glycogen phosphorylase.
J Nat Prod 71: 1877-80 (2011)
China Pharmaceutical University
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.
J Med Chem 51: 6808-28 (2008)
Virginia Commonwealth University
N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists.
Bioorg Med Chem Lett 18: 5729-33 (2009)
Actelion Pharmaceuticals
Interaction of kendomycin and semi-synthetic analogues with the anti-apoptotic protein Bcl-xl.
Bioorg Med Chem Lett 18: 5771-3 (2009)
Merlion Pharmaceuticals
Virtual screening to successfully identify novel janus kinase 3 inhibitors: a sequential focused screening approach.
J Med Chem 51: 7015-9 (2008)
Johnson & Johnson Pharmaceutical
Identification and characterization of small molecule inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.
J Biol Chem 283: 35078-85 (2008)
Harvard Medical School
Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.
Bioorg Med Chem 16: 9471-86 (2008)
LinköPing University
Hedgehog/GLI-mediated transcriptional inhibitors from Zizyphus cambodiana.
Bioorg Med Chem 16: 9420-4 (2008)
Chiba University
A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.
Bioorg Med Chem Lett 18: 5763-5 (2009)
Sunesis Pharmaceuticals
Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines.
Bioorg Med Chem Lett 18: 5738-40 (2009)
Glaxosmithkline
Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases.
J Med Chem 51: 6631-4 (2008)
Gsk
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.
J Med Chem 51: 6902-15 (2008)
Abbott Laboratories
Design, synthesis, and structure-affinity relationships of novel series of sialosides as CD22-specific inhibitors.
J Med Chem 51: 6665-81 (2008)
Gifu University
Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
J Med Chem 51: 6889-901 (2008)
Tsukuba Research Institute
DcpS as a therapeutic target for spinal muscular atrophy.
ACS Chem Biol 3: 711-22 (2008)
Decode Chemistry
Synthesis, biological evaluation, and molecular modeling investigation of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives with PPARalpha and PPARgamma agonist activity.
Bioorg Med Chem 16: 9498-510 (2008)
Università
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket.
Bioorg Med Chem Lett 18: 5809-14 (2009)
Schering-Plough Research Institute
Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors.
Bioorg Med Chem Lett 18: 5758-62 (2009)
Glaxosmithkline
Design, synthesis and evaluation of tetrahydropyran based COX-1/-2 inhibitors.
Eur J Med Chem 44: 1278-87 (2009)
Guru Nanak Dev University
Synthesis, biological evaluation, structural-activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators.
Bioorg Med Chem 16: 9554-73 (2008)
Trinity College
Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists.
Bioorg Med Chem 16: 9524-35 (2008)
Astellas Pharma
Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities.
Bioorg Med Chem 16: 9425-31 (2008)
Chinese Academy Of Sciences
Novel and orally active 5-(1,3,4-oxadiazol-2-yl)pyrimidine derivatives as selective FLT3 inhibitors.
Bioorg Med Chem Lett 18: 5472-7 (2008)
Kyowa Hakko Kogyo
'Reverse' alpha-ketoamide-based p38 MAP kinase inhibitors.
Bioorg Med Chem Lett 18: 5456-9 (2008)
Kemia
Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor.
Bioorg Med Chem Lett 18: 5554-8 (2008)
Merck Frosst Center For Therapeutic Research
2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability.
Bioorg Med Chem Lett 18: 5402-5 (2008)
Neurocrine Biosciences
The 'Ethereal' nature of TLR4 agonism and antagonism in the AGP class of lipid A mimetics.
Bioorg Med Chem Lett 18: 5350-4 (2008)
Glaxosmithkline
Identification of novel inhibitors of extracellular signal-regulated kinase 2 based on the structure-based virtual screening.
Bioorg Med Chem Lett 18: 5372-6 (2008)
Sejong University
Advances toward new antidepressants with dual serotonin transporter and 5-HT1A receptor affinity within a class of 3-aminochroman derivatives. Part 2.
J Med Chem 51: 6980-7004 (2008)
Wyeth Research
Emerging protein targets for anticancer metallodrugs: inhibition of thioredoxin reductase and cathepsin B by antitumor ruthenium(II)-arene compounds.
J Med Chem 51: 6773-81 (2008)
University Of Florence
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
J Med Chem 51: 6740-51 (2008)
University Of Santiago De Compostela
Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies.
J Med Chem 51: 6829-38 (2008)
Friedrich-Alexander University
Pharmacophore modeling and molecular docking led to the discovery of inhibitors of human immunodeficiency virus-1 replication targeting the human cellular aspartic acid-glutamic acid-alanine-aspartic acid box polypeptide 3.
J Med Chem 51: 6635-8 (2008)
Istituto Di Genetica Molecolare
Structure-based approach to the development of potent and selective inhibitors of dihydrofolate reductase from cryptosporidium.
J Med Chem 51: 6839-52 (2008)
University Of Connecticut At Storrs
Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.
J Med Chem 51: 6642-5 (2008)
The Scripps Research Institute
2-Phenyl-imidazo[1,2-a]pyridine compounds containing hydrophilic groups as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity and electrophysiological studies.
J Med Chem 51: 6876-88 (2008)
Universita Degli Studi Di Bari
Vinylogous ureas as a novel class of inhibitors of reverse transcriptase-associated ribonuclease H activity.
ACS Chem Biol 3: 635-44 (2008)
National Cancer Institute-Bethesda
Tetrahydrolipstatin analogues as modulators of endocannabinoid 2-arachidonoylglycerol metabolism.
J Med Chem 51: 6970-9 (2008)
Sapienza University Of Rome
Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone.
J Biol Chem 283: 33516-26 (2008)
University Of Pittsburgh
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
Bioorg Med Chem 16: 9188-201 (2008)
Toray Industries
Axial chirality and affinity at the GABA(A) receptor of pyrimido[1,2-a][1,4]benzodiazepines and related compounds.
Bioorg Med Chem 16: 9519-23 (2008)
The University Of Tokyo
Design and synthesis of sulfoximine based inhibitors for HIV-1 protease.
Bioorg Med Chem Lett 18: 5406-10 (2008)
University Of Minnesota
Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
Bioorg Med Chem Lett 18: 5581-5 (2008)
Glaxosmithkline
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
Bioorg Med Chem Lett 18: 5443-7 (2008)
Vanderbilt University Medical Center
Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds.
Bioorg Med Chem Lett 18: 5391-5 (2008)
Lundbeck Research Usa
Small molecule modulators of toll-like receptors.
J Med Chem 51: 6621-6 (2008)
Schering-Plough Research Institute
Bornyl- and isobornyl-Delta8-tetrahydrocannabinols: a novel class of cannabinergic ligands.
J Med Chem 51: 6393-9 (2008)
Northeastern University
Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding.
J Med Chem 51: 6293-302 (2008)
University Of Kentucky
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.
J Med Chem 51: 6318-33 (2008)
Seoul National University
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
J Med Chem 51: 6503-11 (2008)
Merck Research Laboratories
Aromatic esters of progesterone as 5alpha-reductase and prostate growth inhibitors.
J Enzyme Inhib Med Chem 24: 655-62 (2009)
National University Of Mexico City
Acetylcholinesterase/butyrylcholinesterase inhibition activity of some new carbacylamidophosphate derivatives.
J Enzyme Inhib Med Chem 24: 566-76 (2009)
Tarbiat Modares University
Inhibition of Candida albicans isocitrate lyase activity by sesterterpene sulfates from the tropical sponge Dysidea sp.
Bioorg Med Chem Lett 18: 5377-80 (2008)
Seoul National University
Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine K(Ca) channel blockers.
Bioorg Med Chem Lett 18: 5694-7 (2008)
Bristol-Myers Squibb
1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
Bioorg Med Chem Lett 18: 5368-71 (2008)
Shandong University
Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors.
Bioorg Med Chem 16: 9247-60 (2008)
Kissei Pharmaceutical
5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk).
Bioorg Med Chem Lett 18: 5541-4 (2008)
Johnson & Johnson Pharmaceutical Research And Development
A copper(I)-catalyzed 1,2,3-triazole azide-alkyne click compound is a potent inhibitor of a multidrug-resistant HIV-1 protease variant.
J Med Chem 51: 6263-70 (2008)
The Scripps Research Institute
5-N-methylated quindoline derivatives as telomeric g-quadruplex stabilizing ligands: effects of 5-N positive charge on quadruplex binding affinity and cell proliferation.
J Med Chem 51: 6381-92 (2008)
Sun Yat-Sen University
Synthesis and utilization of chiral alpha-methylated alpha-amino acids with a carboxyalkyl side chain in the design of novel Grb2-SH2 peptide inhibitors free of phosphotyrosine.
J Med Chem 51: 6371-80 (2008)
Chinese Academy Of Sciences
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
J Med Chem 51: 6334-47 (2008)
University Of Arizona
Discovery of novel PPAR ligands by a virtual screening approach based on pharmacophore modeling, 3D shape, and electrostatic similarity screening.
J Med Chem 51: 6303-17 (2008)
University Of Innsbruck
Synthesis and biological evaluation of new donepezil-like Thiaindanones as AChE inhibitors.
J Enzyme Inhib Med Chem 23: 696-703 (2008)
Centre D'Etudes Et De Recherche Sur Le MÉDicament De Normandie
Carbonic anhydrase inhibitors: synthesis and inhibition studies against mammalian isoforms I-XV with a series of 2-(hydrazinocarbonyl)-3-substituted-phenyl-1H-indole-5-sulfonamides.
Bioorg Med Chem 16: 9113-20 (2008)
Istanbul University
In vitro inhibition of salicylic acid derivatives on human cytosolic carbonic anhydrase isozymes I and II.
Bioorg Med Chem 16: 9101-5 (2008)
Ataturk University
Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).
Bioorg Med Chem Lett 18: 5545-9 (2008)
Johnson & Johnson
(3R)-3-amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide as a potent dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Bioorg Med Chem Lett 18: 5435-8 (2008)
Toray Industries
A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity.
Bioorg Med Chem Lett 18: 5424-7 (2008)
University Of Athens
Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead.
Bioorg Med Chem Lett 18: 5537-40 (2008)
Johnson & Johnson
Novel potent inhibitors of A. thaliana cytokinin oxidase/dehydrogenase.
Bioorg Med Chem 16: 9268-75 (2008)
Ieb As Cr & Palacký
Synergistic effect of basic residues at positions 14-15 of nociceptin on binding affinity and receptor activation.
Bioorg Med Chem 16: 9261-7 (2008)
TBA
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.
Bioorg Med Chem Lett 18: 5428-30 (2008)
Glaxosmithkline
Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA.
Bioorg Med Chem Lett 18: 5415-9 (2008)
University Of Washington
Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas.
Bioorg Med Chem Lett 18: 5481-6 (2008)
Glaxosmithkline
Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead.
Bioorg Med Chem Lett 18: 5451-5 (2008)
Glaxosmithkline
Meroditerpenoids from the brown alga Sargassum siliquastrum.
J Nat Prod 71: 1714-9 (2008)
Seoul National University
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
J Med Chem 51: 6471-7 (2008)
Merck Research Laboratories
Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.
J Med Chem 51: 6547-57 (2008)
Abbott Laboratories
Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors.
J Med Chem 51: 6400-9 (2008)
Trinity College
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.
J Med Chem 51: 6271-9 (2008)
Amgen
3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.
J Med Chem 51: 6280-92 (2008)
Amgen
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.
J Med Chem 51: 6359-70 (2008)
Universit£
Evidence for the mechanism of action of the antifungal phytolaccoside B isolated from Phytolacca tetramera Hauman.
J Nat Prod 71: 1720-5 (2008)
Universidad Nacional De Rosario
Soluble 3',6-substituted indirubins with enhanced selectivity toward glycogen synthase kinase -3 alter circadian period.
J Med Chem 51: 6421-31 (2008)
University Of Athens
Thiophene bioisosteres of spirocyclic sigma receptor ligands. 1. N-substituted spiro[piperidine-4,4'-thieno[3,2-c]pyrans].
J Med Chem 51: 6531-7 (2008)
Institut FüR Pharmazeutische And Medizinische Chemie Der UniversitäT MüüNster
4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.
Bioorg Med Chem 16: 9202-11 (2008)
Wyeth Research
Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors.
Bioorg Med Chem Lett 18: 5487-92 (2008)
Astrazeneca
Pyrazolidine-3,5-dione derivatives as potent non-steroidal agonists of farnesoid X receptor: virtual screening, synthesis, and biological evaluation.
Bioorg Med Chem Lett 18: 5497-502 (2008)
Graduate School Of The Chinese Academy Of Sciences
Synthesis of (3,4-dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists.
Bioorg Med Chem Lett 18: 5420-3 (2008)
Pharmacopeia
The molecular interactions of buspirone analogues with the serotonin transporter.
Bioorg Med Chem 16: 9283-94 (2008)
National Medicines Institute
3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: a novel series of mGluR2 positive allosteric modulators.
Bioorg Med Chem Lett 18: 5493-6 (2008)
Pfizer
Using proton nuclear magnetic resonance to study the mode of ribonuclease A inhibition by competitive and noncompetitive inhibitors.
Bioorg Med Chem Lett 18: 5503-6 (2008)
Institute Of Technology
Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.
J Med Chem 51: 6259-62 (2008)
Merck Research Laboratories
1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators.
J Med Chem 51: 6614-8 (2008)
European Research Centre For Drug Discovery And Development (Natsyndrugs)
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.
J Med Chem 51: 6609-13 (2008)
Ewha Womans University
Modified peptides as potent inhibitors of the postsynaptic density-95/N-methyl-D-aspartate receptor interaction.
J Med Chem 51: 6450-9 (2008)
University Of Copenhagen
Alpha,beta-methylene-2'-deoxynucleoside 5'-triphosphates as noncleavable substrates for DNA polymerases: isolation, characterization, and stability studies of novel 2'-deoxycyclonucleosides, 3,5'-cyclo-dG, and 2,5'-cyclo-dT.
J Med Chem 51: 6460-70 (2008)
University Of Rhode Island
Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis.
J Med Chem 51: 6410-20 (2008)
Merck Frosst Centre For Therapeutic Research
Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1.
J Med Chem 51: 6538-46 (2008)
Glaxosmithkline
Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.
J Med Chem 51: 6571-80 (2008)
Abbott Laboratories
Toward optimization of the linker substructure common to transthyretin amyloidogenesis inhibitors using biochemical and structural studies.
J Med Chem 51: 6348-58 (2008)
The Scripps Research Institute
Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors.
Mol Pharmacol 74: 1587-98 (2008)
University Of Konstanz
Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1).
Bioorg Med Chem 16: 9349-58 (2008)
National Institute Of Diabetes And Digestive And Kidney Diseases
Mycophenolic acid analogs with a modified metabolic profile.
Bioorg Med Chem 16: 9340-5 (2008)
University Of Minnesota
Novel insights into GPCR-peptide interactions: mutations in extracellular loop 1, ligand backbone methylations and molecular modeling of neurotensin receptor 1.
Bioorg Med Chem 16: 9359-68 (2008)
Friedrich-Alexander University
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
Bioorg Med Chem Lett 18: 5528-32 (2008)
Irbm/Merck Research Laboratories
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.
Bioorg Med Chem Lett 18: 5609-13 (2008)
Glaxosmithkline
Small, non-peptide C5a receptor antagonists: part 1.
Bioorg Med Chem Lett 18: 5601-4 (2008)
Pfizer
Analogues of 2-phenyl-ethenesulfonic acid phenyl ester have dual functions of inhibiting expression of inducible nitric oxide synthase and activating peroxisome proliferator-activated receptor gamma.
Bioorg Med Chem Lett 18: 5676-9 (2008)
National Health Research Institutes
Novel protoporphyrinogen oxidase inhibitors: 3H-pyrazolo[3,4-d][1,2,3]triazin-4-one derivatives.
J Agric Food Chem 56: 9535-42 (2008)
Nankai University
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
J Med Chem 51: 6599-603 (2008)
Georgia State University
Combining ligand-based pharmacophore modeling, quantitative structure-activity relationship analysis and in silico screening for the discovery of new potent hormone sensitive lipase inhibitors.
J Med Chem 51: 6478-94 (2008)
University Of Jordan
Cortisone dissociates the Shaker family K+ channels from their beta subunits.
Nat Chem Biol 4: 708-14 (2008)
Columbia University College Of Physicians And Surgeons
Discovery of 3-acetyl-4-hydroxy-2-pyranone derivatives and their difluoridoborate complexes as a novel class of HIV-1 integrase inhibitors.
Bioorg Med Chem 16: 8988-98 (2008)
University Of Southern California
Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators.
Bioorg Med Chem Lett 18: 5567-70 (2008)
The Ohio State University
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
Bioorg Med Chem Lett 18: 5439-42 (2008)
Vanderbilt University Medical Center
Design, synthesis and structure-activity relationship of simple bis-amides as potent inhibitors of GlyT1.
Bioorg Med Chem Lett 18: 5533-6 (2008)
F. Hoffmann-La Roche
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
Bioorg Med Chem Lett 18: 5586-90 (2008)
Zydus Research Centre
Small, non-peptide C5a receptor antagonists: part 2.
Bioorg Med Chem Lett 18: 5605-8 (2008)
Pfizer
Structure-guided development of efficacious antifungal agents targeting Candida glabrata dihydrofolate reductase.
Chem Biol 15: 990-6 (2008)
University Of Connecticut
Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries.
Chem Biol 15: 969-78 (2008)
Duke University Medical Center
An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.
Science 321: 1673-5 (2008)
Prolysis
Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential.
J Nat Prod 71: 1783-6 (2008)
Vanderbilt University
4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.
J Med Chem 51: 6581-91 (2008)
Kudos Pharmaceuticals
A beta-fluoroamine inhibitor of purine nucleoside phosphorylase.
J Med Chem 51: 5880-4 (2008)
Industrial Research
Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].
J Med Chem 51: 5866-70 (2008)
National University Of Singapore
Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.
J Med Chem 51: 5813-22 (2008)
Università
Potent dual thymidylate synthase and dihydrofolate reductase inhibitors: classical and nonclassical 2-amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine antifolates.
J Med Chem 51: 5789-97 (2008)
Duquesne University
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
J Med Chem 51: 5758-65 (2008)
Glaxosmithkline
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
J Med Chem 51: 5702-13 (2008)
Tel Aviv University
Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.
J Med Chem 51: 5663-79 (2008)
Glaxosmithkline
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation.
J Med Chem 51: 5594-607 (2008)
National Taiwan University
Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity.
J Med Chem 51: 5585-93 (2008)
University Of Florida
Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists.
J Med Chem 51: 5506-21 (2008)
Emory University
Chemical probes for histone-modifying enzymes.
Nat Chem Biol 4: 590-7 (2008)
Johns Hopkins University School Of Medicine
Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist.
J Pharmacol Exp Ther 327: 716-26 (2008)
Bristol-Myers Squibb
Binding is not enough: flexibility is needed for photocrosslinking of Lck kinase by benzophenone photoligands.
Bioorg Med Chem 16: 8824-9 (2008)
Hunter College Of Cuny
Identification of novel protein kinase CK1 delta (CK1delta) inhibitors through structure-based virtual screening.
Bioorg Med Chem Lett 18: 5672-5 (2008)
Università
6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors.
Bioorg Med Chem Lett 18: 5653-6 (2008)
Glaxosmithkline
Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist.
Bioorg Med Chem Lett 18: 5689-93 (2008)
Pfizer
Triterpenoids from the leaves of Diospyros kaki (persimmon) and their inhibitory effects on protein tyrosine phosphatase 1B.
J Nat Prod 71: 1775-8 (2008)
Chosun University
X-ray crystal structure of human heme oxygenase-1 in complex with 1-(adamantan-1-yl)-2-(1H-imidazol-1-yl)ethanone: a common binding mode for imidazole-based heme oxygenase-1 inhibitors.
J Med Chem 51: 5943-52 (2008)
Queen'S University
Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.
J Med Chem 51: 5915-8 (2008)
Glaxosmithkline
Caspofungin-resistant Candida tropicalis strains causing breakthrough fungemia in patients at high risk for hematologic malignancies.
Antimicrob Agents Chemother 52: 4181-3 (2008)
University Of Medicine And Dentistry Of New Jersey
Synthesis of 1-arylpiperazyl-2-phenylcyclopropanes designed as antidopaminergic agents: cyclopropane-based conformationally restricted analogs of haloperidol.
Bioorg Med Chem 16: 8875-81 (2008)
Hokkaido University
Docking study, synthesis, and in vitro evaluation of fluoro-MADAM derivatives as SERT ligands for PET imaging.
Bioorg Med Chem 16: 9050-5 (2008)
University Of Tours
Structure-activity study at positions 3 and 4 of human neuropeptide S.
Bioorg Med Chem 16: 8841-5 (2008)
University Of Ferrara
Aminostyrylbenzofuran derivatives as potent inhibitors for Abeta fibril formation.
Bioorg Med Chem Lett 18: 5591-3 (2008)
Institute Of Science And Technology
Novel design principle validated: glucopyranosylidene-spiro-oxathiazole as new nanomolar inhibitor of glycogen phosphorylase, potential antidiabetic agent.
Bioorg Med Chem Lett 18: 5680-3 (2008)
University Of Debrecen
Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators.
Bioorg Med Chem Lett 18: 5626-30 (2008)
Vanderbilt University Medical Center
Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists.
Bioorg Med Chem Lett 18: 5698-700 (2008)
Glaxosmithkline
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.
Bioorg Med Chem Lett 18: 5648-52 (2008)
Sunesis Pharmaceuticals
Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.
Bioorg Med Chem Lett 18: 5618-21 (2008)
Genomics Institute Of The Novartis Research Foundation
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
Bioorg Med Chem 16: 8781-94 (2008)
University Of Athens
A study of the structure-activity relationship of GABA(A)-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis.
Bioorg Med Chem 16: 8853-62 (2008)
University Of Wisconsin-Milwaukee
Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: chemistry, biological activities, and molecular modeling.
Bioorg Med Chem Lett 18: 5206-8 (2008)
Abbott Laboratories
Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors.
Bioorg Med Chem Lett 18: 5186-9 (2008)
Sunesis Pharmaceuticals
Molecular design to enhance the penetration into the retina via ocular instillation.
Bioorg Med Chem Lett 18: 5174-7 (2008)
Senju Pharmaceutical
Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha4beta2 nicotinic acetylcholine receptor potentiators.
Bioorg Med Chem Lett 18: 5209-12 (2008)
Amgen
Design, synthesis, and docking studies of novel benzopyrone derivatives as H(1)-antihistaminic agents.
Bioorg Med Chem 16: 9009-17 (2008)
Cairo University
Peptidyl epoxides extended in the P' direction as cysteine protease inhibitors: effect on affinity and mechanism of inhibition.
Bioorg Med Chem 16: 9032-9 (2008)
Bar-Ilan University
Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Bioorg Med Chem 16: 8922-31 (2008)
Amgen
Novel naphthoquinone and quinolinedione inhibitors of CDC25 phosphatase activity with antiproliferative properties.
Bioorg Med Chem 16: 9040-9 (2008)
University Of Paris
Anacardic acid derivatives as inhibitors of glyceraldehyde-3-phosphate dehydrogenase from Trypanosoma cruzi.
Bioorg Med Chem 16: 8889-95 (2008)
Universidade Federal De S£O Carlos
Bisphosphonate inhibitors of ATP-mediated HIV-1 reverse transcriptase catalyzed excision of chain-terminating 3'-azido, 3'-deoxythymidine: a QSAR investigation.
Bioorg Med Chem 16: 8959-67 (2008)
University Of Illinois At Urbana-Champaign
Kinase array design, back to front: biaryl amides.
Bioorg Med Chem Lett 18: 5285-9 (2008)
Glaxosmithkline
Design, synthesis, and structure-activity relationships of novel insulin receptor tyrosine kinase activators.
J Med Chem 51: 6173-87 (2008)
Telik
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
J Med Chem 51: 5932-42 (2008)
Uppsala University
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
J Med Chem 51: 5893-6 (2008)
Adolor
Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity.
Bioorg Med Chem Lett 18: 5213-6 (2008)
European Research Centre For Drug Discovery And Development (Natsyndrugs)
A novel class of small molecule inhibitors of Hsp90.
ACS Chem Biol 3: 645-54 (2008)
Yale University
Design, synthesis, and evaluation of potent and selective ligands for the dopamine 3 (D3) receptor with a novel in vivo behavioral profile.
J Med Chem 51: 5905-8 (2008)
University Of Michigan
Blocking estrogen signaling after the hormone: pyrimidine-core inhibitors of estrogen receptor-coactivator binding.
J Med Chem 51: 6512-30 (2008)
University Of Illinois At Urbana-Champaign
N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands.
Bioorg Med Chem 16: 8335-8 (2008)
Chinese Academy Of Sciences
Structure-activity relationships of compounds targeting mycobacterium tuberculosis 1-deoxy-D-xylulose 5-phosphate synthase.
Bioorg Med Chem Lett 18: 5320-3 (2008)
University Of Illinois At Chicago
Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold.
Bioorg Med Chem Lett 18: 5259-62 (2008)
Genomics Institute Of The Novartis Research Foundation
Structure-activity relationship of ortho- and meta-phenol based LFA-1 ICAM inhibitors.
Bioorg Med Chem Lett 18: 5245-8 (2008)
Biogen Idec
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.
Bioorg Med Chem Lett 18: 5280-4 (2008)
Novartis Institutes For Biomedical Research
Synthesis of bivalent beta2-adrenergic and adenosine A1 receptor ligands.
J Med Chem 51: 6128-37 (2008)
Monash University
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.
J Med Chem 51: 6034-43 (2008)
National Institute Of Mental Health
Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics.
J Med Chem 51: 6085-94 (2008)
Universidad De Santiago De Compostela
Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies.
J Med Chem 51: 6021-33 (2008)
Purdue University
Identification of BRAF inhibitors through in silico screening.
J Med Chem 51: 6121-7 (2008)
University Of Pennsylvania
Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety.
J Med Chem 51: 6005-13 (2008)
Tufts University
Identification, characterization and initial hit-to-lead optimization of a series of 4-arylamino-3-pyridinecarbonitrile as protein kinase C theta (PKCtheta) inhibitors.
J Med Chem 51: 5958-63 (2008)
Wyeth Research
CYP19 (aromatase): exploring the scaffold flexibility for novel selective inhibitors.
Bioorg Med Chem 16: 8349-58 (2008)
Università
Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity.
Bioorg Med Chem 16: 8745-59 (2008)
Université
Molecular design of potent tyrosinase inhibitors having the bibenzyl skeleton.
Bioorg Med Chem Lett 18: 5252-4 (2008)
Utsunomiya University
Designing rapid onset selective serotonin re-uptake inhibitors. Part 3: Site-directed metabolism as a strategy to avoid active circulating metabolites: structure-activity relationships of (thioalkyl)phenoxy benzylamines.
Bioorg Med Chem Lett 18: 5303-6 (2008)
Pfizer
Synthesis and characterization of new piperazine-type inhibitors for mitochondrial NADH-ubiquinone oxidoreductase (complex I).
Biochemistry 47: 10816-26 (2008)
Kyoto University
Screening of herbal constituents for aromatase inhibitory activity.
Bioorg Med Chem 16: 8466-70 (2008)
King'S College London
Synthesis of 3-phenylnaphthalenic derivatives as new selective MT(2) melatoninergic ligands.
Bioorg Med Chem 16: 8339-48 (2008)
University Of Lille 2
Triazole oxytocin antagonists: identification of aryl ether replacements for a biaryl substituent.
Bioorg Med Chem Lett 18: 5242-4 (2008)
Pfizer
Design and synthesis of a series of meta aniline-based LFA-1 ICAM inhibitors.
Bioorg Med Chem Lett 18: 5249-51 (2008)
Biogen Idec
Immucillins in custom catalytic-site cavities.
Bioorg Med Chem Lett 18: 5900-3 (2008)
Albert Einstein College Of Medicine Of Yeshiva University
Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.
Bioorg Med Chem Lett 18: 5255-8 (2008)
Genomics Institute Of The Novartis Research Foundation
Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
J Nat Prod 71: 1513-7 (2008)
University Of Milan
Discovery of novel nitrobenzothiazole inhibitors for Mycobacterium tuberculosis ATP phosphoribosyl transferase (HisG) through virtual screening.
J Med Chem 51: 5984-92 (2008)
Yale University
Structure-activity relationships for a novel series of dopamine D2-like receptor ligands based on N-substituted 3-aryl-8-azabicyclo[3.2.1]octan-3-ol.
J Med Chem 51: 6095-109 (2008)
National Institute On Drug Abuses
Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
Bioorg Med Chem 16: 8729-36 (2008)
Jagiellonian University Medical College
Methoxy-substituted 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives exhibit differential binding affinities at the 5-HT(2A) receptor.
Bioorg Med Chem Lett 18: 5268-71 (2008)
Virginia Commonwealth University
Optimization of a series of multi-isoform PI3 kinase inhibitors.
Bioorg Med Chem Lett 18: 5299-302 (2008)
Ucb Pharma
Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase.
Bioorg Med Chem Lett 18: 5307-10 (2008)
Merck Research Laboratories
Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7.
Bioorg Med Chem Lett 18: 5294-8 (2008)
Mrc Technology
Dual DAT/sigma1 receptor ligands based on 3-(4-(3-(bis(4-fluorophenyl)amino)propyl)piperazin-1-yl)-1-phenylpropan-1-ol.
Bioorg Med Chem Lett 18: 5238-41 (2008)
National Institute On Drug Abuse-Intramural Research Program
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
Bioorg Med Chem Lett 18: 5316-9 (2008)
Bristol-Myers Squibb
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
Bioorg Med Chem Lett 18: 4993-6 (2008)
Yuhan Research Institute
Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.
Bioorg Med Chem Lett 18: 4929-31 (2008)
Wyeth Research
2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists.
J Med Chem 51: 6165-72 (2008)
Monash University
Discovery of orally bioavailable 1,3,4-trisubstituted 2-oxopiperazine-based melanocortin-4 receptor agonists as potential antiobesity agents.
J Med Chem 51: 6055-66 (2008)
Procter & Gamble Pharmaceuticals
Multiple and single binding modes of fragment-like kinase inhibitors revealed by molecular modeling, residue type-selective protonation, and nuclear overhauser effects.
J Med Chem 51: 6225-9 (2008)
Bristol Myers Squibb Research And Development
N9-substituted 2,4-diaminoquinazolines: synthesis and biological evaluation of lipophilic inhibitors of pneumocystis carinii and toxoplasma gondii dihydrofolate reductase.
J Med Chem 51: 6195-200 (2008)
Duquesne University
N-alkyl-5H-pyrido[4,3-b]indol-1-amines and derivatives as novel urotensin-II receptor antagonists.
Bioorg Med Chem Lett 18: 4936-9 (2008)
Glaxosmithkline
Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists.
Bioorg Med Chem Lett 18: 5101-6 (2008)
Tsukuba Research Institute
Discovery of the catechol structural moiety as a Stat3 SH2 domain inhibitor by virtual screening.
Bioorg Med Chem Lett 18: 4988-92 (2008)
Wyeth Pharmaceuticals
Targeting the ribose and phosphate binding site of p38 mitogen-activated protein (MAP) kinase: synthesis and biological testing of 2-alkylsulfanyl-, 4(5)-aryl-, 5(4)-heteroaryl-substituted imidazoles.
J Med Chem 51: 5630-40 (2008)
Eberhard-Karls University Of TüBingen
Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor acti
J Med Chem 51: 5897-900 (2008)
Bristol-Myers Squibb
Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach.
J Med Chem 51: 6138-49 (2008)
Saarland University
Design, synthesis, and biological evaluation of potent c-Met inhibitors.
J Med Chem 51: 5766-79 (2008)
Amgen
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
J Med Chem 51: 5843-55 (2008)
Merck Research Laboratories
Pharmacophore modeling and virtual screening for designing potential PLK1 inhibitors.
Bioorg Med Chem Lett 18: 4972-7 (2008)
Sichuan University
New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter.
Bioorg Med Chem Lett 18: 4940-3 (2008)
University Of Glasgow
Synthesis and SAR study of N-(4-hydroxy-3-(2-hydroxynaphthalene-1-yl)phenyl)-arylsulfonamides: heat shock protein 90 (Hsp90) inhibitors with submicromolar activity in an in vitro assay.
Bioorg Med Chem Lett 18: 4982-7 (2008)
Emory University
Synthesis and biological affinity of new imidazo- and indol-arylpiperazine derivatives: further validation of a pharmacophore model for alpha(1)-adrenoceptor antagonists.
Bioorg Med Chem Lett 18: 5140-5 (2008)
Universit£
Synthesis of a 200-member library of squaric acid N-hydroxylamide amides.
Bioorg Med Chem Lett 18: 4968-71 (2008)
University Of Lille
Predictive QSAR modeling of HIV reverse transcriptase inhibitor TIBO derivatives.
Eur J Med Chem 44: 1509-24 (2009)
Jadavpur University
Identification of hydrolytically stable and selective P2Y(1) receptor agonists.
Eur J Med Chem 44: 1525-36 (2009)
Bar-Ilan University
Achiral oligoamines as versatile tool for the development of aspartic protease inhibitors.
Bioorg Med Chem 16: 8574-86 (2008)
Philipps University Marburg
Promising core structure for nuclear receptor ligands: design and synthesis of novel estrogen receptor ligands based on diphenylamine skeleton.
Bioorg Med Chem Lett 18: 5050-3 (2008)
Tohoku Pharmaceutical University
Evaluation of a focused library of N-aryl L-homoserine lactones reveals a new set of potent quorum sensing modulators.
Bioorg Med Chem Lett 18: 5978-81 (2008)
University Of Wisconsin-Madison
Molecular modeling aided design of nicotinic acid receptor GPR109A agonists.
Bioorg Med Chem Lett 18: 4963-7 (2008)
Merck Research Laboratories
Adamantyl-substituted retinoid-derived molecules that interact with the orphan nuclear receptor small heterodimer partner: effects of replacing the 1-adamantyl or hydroxyl group on inhibition of cancer cell growth, induction of cancer cell apoptosis, and inhibition of SRC homology 2 domain-containi
J Med Chem 51: 5650-62 (2008)
Burnham Institute For Medical Research
Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.
Bioorg Med Chem Lett 18: 4978-81 (2008)
Kitasato University
Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1alpha prolyl hydroxylase-2 inhibitors.
Bioorg Med Chem Lett 18: 5023-6 (2008)
Amgen
Discovery of thieno[2,3-c]pyridines as potent COT inhibitors.
Bioorg Med Chem Lett 18: 4952-5 (2008)
Abbott Bioresearch Center
Design and synthesis of fluorescent SGLT2 inhibitors.
Bioorg Med Chem Lett 18: 4944-7 (2008)
Pfizer
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain.
J Med Chem 51: 5502-5 (2008)
Novartis
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .
J Med Chem 51: 5522-32 (2008)
Piramed Pharma
Lipid-lowering (hetero)aromatic tetrahydro-1,4-oxazine derivatives with antioxidant and squalene synthase inhibitory activity.
J Med Chem 51: 5861-5 (2008)
University Of Athens
Discovery and labeling of high-affinity 3,4-diarylpyrazolines as candidate radioligands for in vivo imaging of cannabinoid subtype-1 (CB1) receptors.
J Med Chem 51: 5608-16 (2008)
National Institute Of Mental Health
Molecular engineering of conotoxins: the importance of loop size to alpha-conotoxin structure and function.
J Med Chem 51: 5575-84 (2008)
University Of Queensland
Aminoacyl-anthraquinone conjugates as telomerase inhibitors: synthesis, biophysical and biological evaluation.
J Med Chem 51: 5566-74 (2008)
University Of Padova
6-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) forms an irreversible bond to the active site of the GluR2 AMPA receptor.
J Med Chem 51: 5856-60 (2008)
University Of California San Francisco
Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening.
J Med Chem 51: 5552-65 (2008)
Universit£
Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.
Bioorg Med Chem 16: 8546-56 (2008)
National Institute Of Diabetes And Digestive And Kidney Diseases
Design and synthesis of 6-fluoro-2-naphthyl derivatives as novel CCR3 antagonists with reduced CYP2D6 inhibition.
Bioorg Med Chem 16: 8607-18 (2008)
Astellas Pharma
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
Bioorg Med Chem 16: 8072-81 (2008)
Sapienza University Of Rome
Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors.
Bioorg Med Chem Lett 18: 5134-9 (2008)
F. Hoffmann-La Roche
Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands.
Bioorg Med Chem Lett 18: 5032-6 (2008)
The Schering Plough Research Institute
Trace amine-associated receptor 1 (TAAR1) is activated by amiodarone metabolites.
Bioorg Med Chem Lett 18: 5920-2 (2008)
University Of California San Francisco
1-Benzylbenzimidazoles: the discovery of a novel series of bradykinin B(1) receptor antagonists.
Bioorg Med Chem Lett 18: 5027-31 (2008)
Neurogen
Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels.
Bioorg Med Chem Lett 18: 5875-8 (2008)
University Of California
New PPARgamma ligands based on barbituric acid: virtual screening, synthesis and receptor binding studies.
Bioorg Med Chem Lett 18: 4959-62 (2008)
National Institute Of Pharmaceutical Education And Research
Discovery of novel series of benzoic acid derivatives containing biphenyl ether moiety as potent and selective human beta(3)-adrenergic receptor agonists: Part IV.
Bioorg Med Chem Lett 18: 5037-40 (2008)
Astellas Pharma
Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics.
Bioorg Med Chem Lett 18: 5904-8 (2008)
Yale University
Syntheses and structure-activity relationships of novel, potent, and selective trans-2-[3-oxospiro[isobenzofuran-1(3H),1'-cyclohexan]-4'-yl]benzimidazole NPY Y5 receptor antagonists.
Bioorg Med Chem Lett 18: 4997-5001 (2008)
Banyu Tsukuba Research Institute
Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design.
Bioorg Med Chem Lett 18: 5895-9 (2008)
Genomics Institute Of The Novartis Research Foundation
Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.
Bioorg Med Chem Lett 18: 4948-51 (2008)
Merck Research Laboratories
3,4-Dihydro-2H-1,4-benzoxazine derivatives combining thrombin inhibitory and glycoprotein IIb/IIIa receptor antagonistic activity as a novel class of antithrombotic compounds with dual function.
J Med Chem 51: 5617-29 (2008)
University Of Ljubljana
Potent cationic inhibitors of West Nile virus NS2B/NS3 protease with serum stability, cell permeability and antiviral activity.
J Med Chem 51: 5714-21 (2008)
University Of Queensland
Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis.
J Med Chem 51: 5798-806 (2008)
Universit£
Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor.
J Med Chem 51: 5875-9 (2008)
Dipartimento Di Scienze Farmaceutiche
Butyrylcholinesterase inhibitory activity of testosterone and some of its metabolites.
J Enzyme Inhib Med Chem 24: 553-8 (2009)
University Of Jordan
Mutations M184V and Y115F in HIV-1 reverse transcriptase discriminate against "nucleotide-competing reverse transcriptase inhibitors".
J Biol Chem 283: 29904-11 (2008)
Mcgill University
A domino effect in antifolate drug action in Escherichia coli.
Nat Chem Biol 4: 602-8 (2008)
Princeton University
Synthesis and pharmacological evaluation of bis-3-(3,4-dichlorophenyl)acrylamide derivatives as glycogen phosphorylase inhibitors.
Bioorg Med Chem 16: 8627-34 (2008)
Astellas Pharma
Dual inhibition of monoamine oxidase B and antagonism of the adenosine A(2A) receptor by (E,E)-8-(4-phenylbutadien-1-yl)caffeine analogues.
Bioorg Med Chem 16: 8676-84 (2008)
North-West University
Development of novel tail-modified anandamide analogs.
Bioorg Med Chem Lett 18: 5912-5 (2008)
Northeastern University
Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4'-piperidin]-1'-yl}benzimidazole derivatives.
Bioorg Med Chem Lett 18: 5010-4 (2008)
Banyu Tsukuba Research Institute
Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.
Bioorg Med Chem Lett 18: 5115-7 (2008)
Amgen
Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists.
Bioorg Med Chem 16: 8516-25 (2008)
Abbott Laboratories
Derivatives of 1,4-bis(3-hydroxycarbonyl-4-hydroxyl)styrylbenzene as PTP1B inhibitors with hypoglycemic activity.
Bioorg Med Chem 16: 8643-52 (2008)
Inha University
Novel azolyl-(phenylmethyl)]aryl/heteroarylamines: potent CYP26 inhibitors and enhancers of all-trans retinoic acid activity in neuroblastoma cells.
Bioorg Med Chem 16: 8301-13 (2008)
Cardiff University
Discovery of a novel class of PPARdelta partial agonists.
Bioorg Med Chem Lett 18: 5018-22 (2008)
Gsk
ortho-dihydroxyisoflavone derivatives from aged Doenjang (Korean fermented soypaste) and its radical scavenging activity.
Bioorg Med Chem Lett 18: 5006-9 (2008)
Amorepacific
Discovery and optimization of (R)-prolinol-derived agonists of the Growth Hormone Secretagogue receptor (GHSR).
Bioorg Med Chem Lett 18: 5083-6 (2008)
Bristol-Myers Squibb
Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.
Bioorg Med Chem Lett 18: 5002-5 (2008)
Anadys Pharmaceuticals
Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
Bioorg Med Chem 16: 8563-73 (2008)
University Of Wisconsin-Madison
Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists.
Bioorg Med Chem Lett 18: 5063-5 (2008)
Bristol-Myers Squibb
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
Bioorg Med Chem Lett 18: 5015-7 (2008)
Wyeth Research
Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists.
Bioorg Med Chem Lett 18: 5118-22 (2008)
Amgen
Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands.
Bioorg Med Chem Lett 18: 5075-7 (2008)
Glaxosmithkline
Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile.
Bioorg Med Chem Lett 18: 5107-10 (2008)
Merck
Docking, 3D-QSAR studies and in silico ADME prediction on c-Src tyrosine kinase inhibitors.
Eur J Med Chem 44: 990-1000 (2009)
Universit£
Discovery of potent and selective small-molecule PAR-2 agonists.
J Med Chem 51: 5490-3 (2008)
Acadia Pharmaceuticals
Synthesis of new sulfonyl pyrrolidine derivatives as matrix metalloproteinase inhibitors.
Bioorg Med Chem 16: 7932-8 (2008)
Shandong University
7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity.
Bioorg Med Chem Lett 18: 5130-3 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Design, synthesis, and evaluation of novel organophosphorus inhibitors of bacterial ureases.
J Med Chem 51: 5736-44 (2008)
Wroclaw University Of Technology
Synthesis and biological activity of 1-methyl-tryptophan-tirapazamine hybrids as hypoxia-targeting indoleamine 2,3-dioxygenase inhibitors.
Bioorg Med Chem 16: 8661-9 (2008)
The University Of Tokushima
Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
J Med Chem 51: 5680-9 (2008)
Cephalon
Discovery of novel Cdc25 phosphatase inhibitors with micromolar activity based on the structure-based virtual screening.
J Med Chem 51: 5533-41 (2008)
Sejong University
Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.
Bioorg Med Chem Lett 18: 5126-9 (2008)
Deltagen Research Laboratories
Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor antagonists.
J Med Chem 51: 5397-412 (2008)
National Health Research Institutes
Synthesis of novel beta-lactone inhibitors of fatty acid synthase.
J Med Chem 51: 5285-96 (2008)
The Burnham Institute For Medical Research
Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid.
J Med Chem 51: 5449-53 (2008)
Eberhard Karls University Tuebingen
Crystal structures of rat vitamin D receptor bound to adamantyl vitamin D analogs: structural basis for vitamin D receptor antagonism and partial agonism.
J Med Chem 51: 5320-9 (2008)
Tokyo Medical And Dental University
Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring.
Bioorg Med Chem 16: 8022-8 (2008)
Tohoku Pharmaceutical University
Oleanolic acid and its derivatives: new inhibitor of protein tyrosine phosphatase 1B with cellular activities.
Bioorg Med Chem 16: 8697-705 (2008)
Chinese Academy Of Sciences
A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins.
Bioorg Med Chem Lett 18: 4761-3 (2008)
University Of Bonn
Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.
Bioorg Med Chem Lett 18: 4770-3 (2008)
Bristol Myers Squibb
Synthesis and evaluation of indolinyl- and indolylphenylacetylenes as PET imaging agents for beta-amyloid plaques.
Bioorg Med Chem Lett 18: 4823-7 (2008)
University Of Pennsylvania
Effect of cathepsin K inhibitors on bone resorption.
J Med Chem 51: 5459-62 (2008)
Novartis Institutes For Biomedical Research
Novel glucagon receptor antagonists with improved selectivity over the glucose-dependent insulinotropic polypeptide receptor.
J Med Chem 51: 5387-96 (2008)
Novo Nordisk
Conformationally constrained analogues of diacylglycerol. 30. An investigation of diacylglycerol-lactones containing heteroaryl groups reveals compounds with high selectivity for Ras guanyl nucleotide-releasing proteins.
J Med Chem 51: 5371-86 (2008)
National Cancer Institute-Frederick
Modulating G-protein coupled receptor/G-protein signal transduction by small molecules suggested by virtual screening.
J Med Chem 51: 5297-303 (2008)
Washington University
Aryl sulfones as novel bradykinin B1 receptor antagonists for treatment of chronic pain.
Bioorg Med Chem Lett 18: 4764-9 (2008)
Amgen
Synthesis of both enantiomers of hydroxypipecolic acid derivatives equivalent to 5-azapyranuronic acids and evaluation of their inhibitory activities against glycosidases.
Bioorg Med Chem 16: 8273-86 (2008)
Tohoku Pharmaceutical University
Thermodynamic and kinetic characterization of host-guest association between bolaform surfactants and alpha- and beta-cyclodextrins.
J Phys Chem B 112: 11310-6 (2008)
Lund University
2-Thiazolylimino/heteroarylimino-5-arylidene-4-thiazolidinones as new agents with SHP-2 inhibitory action.
J Med Chem 51: 5221-8 (2008)
Aristotle University
Inhibition of IkappaB kinase-beta and anticancer activities of novel chalcone adamantyl arotinoids.
J Med Chem 51: 5431-40 (2008)
Universidade De Vigo
Design and synthesis of a metabolically stable and potent antitussive agent, a novel delta opioid receptor antagonist, TRK-851.
Bioorg Med Chem 16: 7956-67 (2008)
Toray Industries
Characterization of the binding properties of SIRT2 inhibitors with a N-(3-phenylpropenoyl)-glycine tryptamide backbone.
Bioorg Med Chem 16: 8054-62 (2008)
University Of Kuopio
Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues.
Bioorg Med Chem 16: 8011-21 (2008)
China Pharmaceutical University
Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents.
Bioorg Med Chem 16: 7992-8002 (2008)
China Pharmaceutical University
Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.
Bioorg Med Chem 16: 8127-35 (2008)
University Of Leipzig
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Bioorg Med Chem Lett 18: 4798-801 (2008)
Merck Research Laboratories
Conformationally constrained analogues of diacylglycerol. 29. Cells sort diacylglycerol-lactone chemical zip codes to produce diverse and selective biological activities.
J Med Chem 51: 5198-220 (2008)
National Cancer Institute-Frederick
Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119.
J Med Chem 51: 5172-5 (2008)
Arena Pharmaceuticals
Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1.
J Med Chem 51: 5229-42 (2008)
Universite Paris-Descartes
Limited inhibitory effects of oseltamivir and zanamivir on human sialidases.
Antimicrob Agents Chemother 52: 3484-91 (2008)
Miyagi Cancer Center Research Institute
Potent CCR4 antagonists: synthesis, evaluation, and docking study of 2,4-diaminoquinazolines.
Bioorg Med Chem 16: 7968-74 (2008)
Astellas Pharma
Synthesis and calpain inhibitory activity of peptidomimetic compounds with constrained amino acids at the P2 position.
Bioorg Med Chem Lett 18: 4806-8 (2008)
The University Of Tennessee Health Science Center
Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer.
Bioorg Med Chem Lett 18: 4794-7 (2008)
Astrazeneca R&D Boston
Kempopeptins A and B, serine protease inhibitors with different selectivity profiles from a marine cyanobacterium, Lyngbya sp.
J Nat Prod 71: 1625-9 (2008)
University Of Florida
Anti-HIV-1 activity of phloroglucinol derivative, 6,6'-bieckol, from Ecklonia cava.
Bioorg Med Chem 16: 7921-6 (2008)
Pukyong National University
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
Bioorg Med Chem Lett 18: 4838-43 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Thiazolidinone CFTR inhibitors with improved water solubility identified by structure-activity analysis.
Bioorg Med Chem 16: 8187-95 (2008)
University Of California
Discovery of betamethasone 17alpha-carbamates as dissociated glucocorticoid receptor modulators in the rat.
Bioorg Med Chem 16: 7535-42 (2008)
Merck Research Laboratories
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.
Bioorg Med Chem Lett 18: 4907-12 (2008)
Ariad Pharmaceuticals
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.
J Med Chem 51: 5243-63 (2008)
Vertex Pharmaceuticals
Inhibition of siderophore biosynthesis in Mycobacterium tuberculosis with nucleoside bisubstrate analogues: structure-activity relationships of the nucleobase domain of 5'-O-[N-(salicyl)sulfamoyl]adenosine.
J Med Chem 51: 5349-70 (2008)
University Of Minnesota
Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.
J Med Chem 51: 5330-41 (2008)
Bristol-Myers Squibb
Cytosporone B is an agonist for nuclear orphan receptor Nur77.
Nat Chem Biol 4: 548-56 (2008)
Xiamen University
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
J Med Chem 51: 5471-89 (2008)
Matrix Laboratories
Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase.
J Med Chem 51: 5441-8 (2008)
The Scripps Research Institute
Synthesis and biological evaluation of (-)- and (+)-debromoflustramine B and its analogues as selective butyrylcholinesterase inhibitors.
J Med Chem 51: 5271-84 (2008)
Instituto PolitéCnico Nacional
The structure-activity relationship study on 2-, 5-, and 6-position of the water soluble 1,4-dihydropyridine derivatives blocking N-type calcium channels.
Bioorg Med Chem Lett 18: 4813-6 (2008)
Ajinomoto
2-Substituted piperazine-derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity.
Bioorg Med Chem Lett 18: 4833-7 (2008)
Merck
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
J Med Chem 51: 5423-30 (2008)
Abbott Laboratories
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.
Bioorg Med Chem Lett 18: 4844-8 (2008)
Amgen
Discovery of 1,3-disubstituted-1H-pyrrole derivatives as potent melanin-concentrating hormone receptor 1 (MCH-R1) antagonists.
Bioorg Med Chem Lett 18: 4859-63 (2008)
Astrazeneca R&D MöLndal
Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands.
Bioorg Med Chem Lett 18: 4817-22 (2008)
Neurocrine Biosciences
Bioactive 5alpha-pregnane-type steroidal alkaloids from Sarcococca hookeriana.
J Nat Prod 71: 1481-4 (2008)
Bielefeld University
Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds.
J Med Chem 51: 4948-56 (2008)
Moffitt Cancer Center
Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.
J Med Chem 51: 4866-9 (2008)
Glaxosmithkline
Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.
J Med Chem 51: 5019-34 (2008)
Amgen
Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic activity in vivo.
J Med Chem 51: 5075-84 (2008)
Universit£
Synthesis and discovery of high affinity folate receptor-specific glycinamide ribonucleotide formyltransferase inhibitors with antitumor activity.
J Med Chem 51: 5052-63 (2008)
Wayne State University School Of Medicine
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
J Med Chem 51: 5109-17 (2008)
University Of Cagliari
Redesigning kinase inhibitors to enhance specificity.
J Med Chem 51: 4890-8 (2008)
Rice University
NMR screening for lead compounds using tryptophan-mutated proteins.
J Med Chem 51: 5035-42 (2008)
Institute For Biochemistry
Novel 1,4-benzothiazine derivatives as large conductance Ca2+-activated potassium channel openers.
J Med Chem 51: 5085-92 (2008)
Universit£
Structure-activity relationship studies on a novel class of antiproliferative agents derived from Lavendustin A. Part I: Ring A modifications.
Bioorg Med Chem 16: 7552-60 (2008)
Novartis Institutes For Biomedical Research
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).
Bioorg Med Chem 16: 8224-36 (2008)
University Of Bonn
Discovery of a potent and selective aurora kinase inhibitor.
Bioorg Med Chem Lett 18: 4880-4 (2008)
Sunesis Pharmaceuticals
8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK).
Bioorg Med Chem Lett 18: 4885-90 (2008)
Newcastle University
A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity.
Bioorg Med Chem Lett 18: 4896-9 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Biomimetic synthesis of the IDO inhibitors exiguamine A and B.
Nat Chem Biol 4: 535-7 (2008)
University Of California
Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable.
Bioorg Med Chem Lett 18: 4723-6 (2008)
Astrazeneca
Potent and selective pyrazole-based inhibitors of B-Raf kinase.
Bioorg Med Chem Lett 18: 4692-5 (2008)
Array Biopharma
Stereoselective synthesis and biological evaluation of 3,4-diaminocyclohexanecarboxylic acid derivatives as factor Xa inhibitors.
Bioorg Med Chem Lett 18: 4587-92 (2008)
Daiichi Sankyo
Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge.
Bioorg Med Chem 16: 7715-27 (2008)
Saarland University
Synthesis of stable and selective inhibitors of human galectins-1 and -3.
Bioorg Med Chem 16: 7811-23 (2008)
Universit£
A new multi-gram synthetic route to labeling precursors for the D(2/3) PET agent 18F-fallypride.
Bioorg Med Chem Lett 18: 4467-9 (2008)
Vanderbilt University
Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.
Bioorg Med Chem Lett 18: 4533-7 (2008)
Chugai Pharmaceutical
Discovery of dihydroquinoxalinone acetamides containing bicyclic amines as potent Bradykinin B1 receptor antagonists.
Bioorg Med Chem Lett 18: 4477-81 (2008)
Amgen
Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.
Bioorg Med Chem Lett 18: 4474-6 (2008)
Harvard Medical School
Synthesis and biological evaluation of N-mercaptoacylproline and N-mercaptoacylthiazolidine-4-carboxylic acid derivatives as leukotriene A4 hydrolase inhibitors.
Bioorg Med Chem Lett 18: 4529-32 (2008)
Santen Pharmaceutical
Synthesis and antiviral properties of some polyphenols related to Salvia genus.
Bioorg Med Chem Lett 18: 4736-40 (2008)
Umr Cnrs 8009
Aminomethylpiperazines as selective urotensin antagonists.
Bioorg Med Chem Lett 18: 4470-3 (2008)
Glaxosmithkline
Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer.
J Med Chem 51: 5009-18 (2008)
Saarland University
Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.
J Med Chem 51: 5064-74 (2008)
Saarland University
Inhibitory effects of benzyl benzoate and its derivatives on angiotensin II-induced hypertension.
Bioorg Med Chem 16: 7843-52 (2008)
Nagoya University
Alkamides from the fruits of Piper longum and Piper nigrum displaying potent cell adhesion inhibition.
Bioorg Med Chem Lett 18: 4544-6 (2008)
Korea Research Institute Of Bioscience And Biotechnology
4-(1H-indazol-5-yl)-6-phenylpyrimidin-2(1H)-one analogs as potent CDC7 inhibitors.
Bioorg Med Chem Lett 18: 4482-5 (2008)
Novartis Institutes Of Biomedical Research
Stereoselectivity of binding of alpha-(N-benzylamino)benzylphosphonic acids to prostatic acid phosphatase.
Bioorg Med Chem Lett 18: 4620-3 (2008)
National Academy Of Sciences Of Ukraine
2-Arylpyrimidines: novel CRF-1 receptor antagonists.
Bioorg Med Chem Lett 18: 4486-90 (2008)
Neurogen
Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability.
Bioorg Med Chem Lett 18: 4491-4 (2008)
Neurocrine Biosciences
Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.
Eur J Med Chem 44: 1067-85 (2009)
Institute Of Organic Synthesis
New NSAIDs-NO hybrid molecules with antiproliferative properties on human prostatic cancer cell lines.
Bioorg Med Chem Lett 18: 4655-7 (2008)
Université
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.
Bioorg Med Chem Lett 18: 5916-9 (2008)
The Scripps Research Institute
Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.
Bioorg Med Chem Lett 18: 4503-7 (2008)
Neurocrine Biosciences
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.
Bioorg Med Chem Lett 18: 4495-8 (2008)
Neurocrine Biosciences
Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy.
Bioorg Med Chem Lett 18: 4682-7 (2008)
Kissei Pharmaceutical
Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (PMX 610, NSC 721648).
J Med Chem 51: 5135-9 (2008)
Cardiff University
Design and synthesis of a novel series of N-alkyl isatin acylhydrazone derivatives that act as selective cannabinoid receptor 2 agonists for the treatment of neuropathic pain.
J Med Chem 51: 4932-47 (2008)
The University Of Texas M.D. Anderson Cancer Center
Synthesis, stereochemical identification, and selective inhibitory activity against human monoamine oxidase-B of 2-methylcyclohexylidene-(4-arylthiazol-2-yl)hydrazones.
J Med Chem 51: 4874-80 (2008)
Sapienza University Of Rome
Structure-activity study of phosphoramido acid esters as acetylcholinesterase inhibitors.
J Enzyme Inhib Med Chem 23: 556-61 (2008)
Imam Hossein University
Effects of hydroxybenzyl alcohols on melanogenesis in melanocyte-keratinocyte co-culture and monolayer culture of melanocytes.
J Enzyme Inhib Med Chem 23: 526-34 (2008)
National Tsing Hua University
Structure based development of phenylimidazole-derived inhibitors of indoleamine 2,3-dioxygenase.
J Med Chem 51: 4968-77 (2008)
Bryn Mawr College
3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.
J Med Chem 51: 5101-8 (2008)
Arena Pharmaceuticals
Sulindac derivatives that activate the peroxisome proliferator-activated receptor gamma but lack cyclooxygenase inhibition.
J Med Chem 51: 4911-9 (2008)
Vanderbilt University Center For Structural Biology
Investigations on the 4-quinolone-3-carboxylic acid motif. 1. Synthesis and structure-activity relationship of a class of human immunodeficiency virus type 1 integrase inhibitors.
J Med Chem 51: 5125-9 (2008)
Universita Degli Studi Di Siena
Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and effic
J Med Chem 51: 4858-61 (2008)
Bristol-Myers Squibb Research & Development
Molecular and biochemical characterization of SHV-56, a novel inhibitor-resistant beta-lactamase from Klebsiella pneumoniae.
Antimicrob Agents Chemother 52: 3792-4 (2008)
University Of Bordeaux
2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity.
Bioorg Med Chem 16: 7646-53 (2008)
Zhejiang University
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.
Bioorg Med Chem Lett 18: 4642-6 (2008)
Novartis Institutes For Biomedical Research
Discovery of piperidine carboxamide TRPV1 antagonists.
Bioorg Med Chem Lett 18: 4569-72 (2008)
Johnson & Johnson Pharmaceutical Research And Development
4-(1,1-Dioxo-1,4-dihydro-1lambda6-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-ones as potent inhibitors of HCV NS5B polymerase.
Bioorg Med Chem Lett 18: 4628-32 (2008)
Anadys Pharmaceuticals
Efficient synthesis and utilization of phenyl-substituted heteroaromatic carboxylic acids as aryl diketo acid isosteres in the design of novel HIV-1 integrase inhibitors.
Bioorg Med Chem Lett 18: 4521-4 (2008)
Chinese Academy Of Sciences
Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: effect of introduction of fluorine at the linker part.
Bioorg Med Chem Lett 18: 4525-8 (2008)
The University Of Tokyo
Knowledge-based design of 7-azaindoles as selective B-Raf inhibitors.
Bioorg Med Chem Lett 18: 4610-4 (2008)
Glaxosmithkline
Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.
Bioorg Med Chem Lett 18: 4573-7 (2008)
Neurogen
Novel ligands rationally designed for characterizing I2-imidazoline binding sites nature and functions.
J Med Chem 51: 5130-4 (2008)
Università
Synthesis and pharmacological evaluation of pentacyclic 6a,7-dihydrodiindole and 2,3-dihydrodiindole derivatives as novel melatoninergic ligands.
Bioorg Med Chem 16: 7654-61 (2008)
University Of WüRzburg
Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling.
Bioorg Med Chem Lett 18: 5838-41 (2008)
The Scripps Research Institute
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.
J Med Chem 51: 4986-99 (2008)
Astex
Facile radiosynthesis of fluorine-18 labeled beta-blockers. Synthesis, radiolabeling, and ex vivo biodistribution of [18F]-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol.
J Med Chem 51: 5093-100 (2008)
Centre For Addiction And Mental Health
In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil.
Bioorg Med Chem 16: 7599-606 (2008)
Universidade Federal De Lavras-Ufla
A synthetic method for peptide-PEG-lipid conjugates: application of octreotide-PEG-DSPE synthesis.
Bioorg Med Chem Lett 18: 4593-6 (2008)
Kuang Tien General Hospital
4-Amino-6-arylamino-pyrimidine-5-carbaldehyde hydrazones as potent ErbB-2/EGFR dual kinase inhibitors.
Bioorg Med Chem Lett 18: 4615-9 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Structure-based virtual screening for identification of novel 11beta-HSD1 inhibitors.
Eur J Med Chem 44: 1167-71 (2009)
Institute Of Materia Medica
Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes.
J Med Chem 51: 4851-7 (2008)
Amgen
Discovery of a novel series of benzoic acid derivatives as potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. 3. Phenylethanolaminotetraline (PEAT) skeleton containing biphenyl or biphenyl ether moiety.
J Med Chem 51: 4804-22 (2008)
Astellas Pharma
Discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a potent inducer of apoptosis with high in vivo activity.
J Med Chem 51: 4771-9 (2008)
Epicept
Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.
J Med Chem 51: 4430-48 (2008)
Johannes Gutenberg University
Synthesis and evaluation in vitro and in vivo of a 11C-labeled cyclooxygenase-2 (COX-2) inhibitor.
Bioorg Med Chem 16: 7662-70 (2008)
Institute Of Radiopharmacy
Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines.
Bioorg Med Chem 16: 7691-7 (2008)
Quaid-I-Azam University
Synthesis and preliminary pharmacological evaluation of novel derivatives of L-beta-threo-benzylaspartate as inhibitors of the neuronal glutamate transporter EAAT3.
Bioorg Med Chem 16: 7740-8 (2008)
The University Of Montana
Baicalin, a prodrug able to reach the CNS, is a prolyl oligopeptidase inhibitor.
Bioorg Med Chem 16: 7516-24 (2008)
Institut De Recerca BiomèDica De Barcelona
Design, synthesis and biological evaluation of new tryptamine and tetrahydro-beta-carboline-based selective inhibitors of CDK4.
Bioorg Med Chem 16: 7728-39 (2008)
University Of Leicester
Allosteric FBPase inhibitors gain 10(5) times in potency when simultaneously binding two neighboring AMP sites.
Bioorg Med Chem Lett 18: 4708-12 (2008)
F. Hoffmann-La Roche
Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, and biological activities.
J Med Chem 51: 4744-50 (2008)
Fondazione Cenci Bolognettiuniversit£
Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases.
J Med Chem 51: 4672-84 (2008)
Astrazeneca
False positives in a reporter gene assay: identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase.
J Med Chem 51: 4724-9 (2008)
Leiden/Amsterdam Center For Drug Research
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
Antimicrob Agents Chemother 52: 3467-77 (2008)
Walter Reed Army Institute Of Research
Characterization of the new metallo-beta-lactamase VIM-13 and its integron-borne gene from a Pseudomonas aeruginosa clinical isolate in Spain.
Antimicrob Agents Chemother 52: 3589-96 (2008)
Hospital Son Dureta
Novel dimeric aryldiketo containing inhibitors of HIV-1 integrase: effects of the phenyl substituent and the linker orientation.
Bioorg Med Chem 16: 7777-87 (2008)
Chinese Academy Of Sciences
Correlation of inhibitor effects on enzyme activity and thermal stability for the integral membrane protein fatty acid amide hydrolase.
Bioorg Med Chem Lett 18: 5847-50 (2008)
The Scripps Research Institute
3-(4-(6-Fluoroalkoxy-3,4-dihydroisoquinoline-2(1H)-yl)cyclohexyl)-1H-indole-5-carbonitriles for SERT imaging: chemical synthesis, evaluation in vitro and radiofluorination.
Bioorg Med Chem Lett 18: 4727-30 (2008)
Institut FüR InterdisziplinäRe Isotopenforschung
Synthesis and evaluation of acylguanidine FXa inhibitors.
Bioorg Med Chem Lett 18: 4696-9 (2008)
Bristol-Myers Squibb Research And Development
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.
Bioorg Med Chem Lett 18: 4700-4 (2008)
Ucb Pharma
Epiboxidine and novel-related analogues: a convenient synthetic approach and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes.
Bioorg Med Chem Lett 18: 4651-4 (2008)
Università
Inhibition of human mitochondrial carbonic anhydrases VA and VB with para-(4-phenyltriazole-1-yl)-benzenesulfonamide derivatives.
Bioorg Med Chem Lett 18: 4624-7 (2008)
Griffith University
Oxadiazole-carbonylaminothioureas as SIRT1 and SIRT2 inhibitors.
J Med Chem 51: 4377-80 (2008)
University Of Kuopio
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
J Med Chem 51: 4370-3 (2008)
University Of Illinois At Chicago
Fluorinated phenylcyclopropylamines. Part 5: Effects of electron-withdrawing or -donating aryl substituents on the inhibition of monoamine oxidases A and B by 2-aryl-2-fluoro-cyclopropylamines.
Bioorg Med Chem 16: 7148-66 (2008)
UniversitäT MüNster
New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties.
Bioorg Med Chem 16: 7759-69 (2008)
Laboratorio De Radicales Libres (Iqog, Csic)
Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors.
Bioorg Med Chem Lett 18: 4713-5 (2008)
Université
Cinnamic acids and mono-substituted benzoic acids as useful capping groups for the preparation of hNK2 receptor antagonists.
Bioorg Med Chem Lett 18: 4705-7 (2008)
Menarini Ricerche
Design of Helicobacter pylori glutamate racemase inhibitors as selective antibacterial agents: a novel pro-drug approach to increase exposure.
Bioorg Med Chem Lett 18: 4716-22 (2008)
Astrazeneca R&D Boston
Discovery and stereoselective synthesis of the novel isochroman neurokinin-1 receptor antagonist 'CJ-17,493'.
Bioorg Med Chem 16: 7193-205 (2008)
Pfizer
Muscarinic receptor 1 agonist activity of novel N-arylthioureas substituted 3-morpholino arecoline derivatives in Alzheimer's presenile dementia models.
Bioorg Med Chem 16: 7095-101 (2008)
University Of Mysore
Structure-activity relationship of flavonoids as influenza virus neuraminidase inhibitors and their in vitro anti-viral activities.
Bioorg Med Chem 16: 7141-7 (2008)
Peking Union Medical College
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.
Bioorg Med Chem Lett 18: 4267-74 (2008)
Amgen
Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies.
Bioorg Med Chem Lett 18: 4282-6 (2008)
Universita Degli Studi Di Firenze
Synthesis and evaluation of heteroaryl-ketone derivatives as a novel class of VEGFR-2 inhibitors.
Bioorg Med Chem Lett 18: 4344-7 (2008)
Imclone Systems
Nitrogen-containing flavonoid analogues as CDK1/cyclin B inhibitors: synthesis, SAR analysis, and biological activity.
Bioorg Med Chem 16: 7128-33 (2008)
Dalian University Of Technology
Design and optimization of potent, selective antagonists of Oxytocin.
Bioorg Med Chem Lett 18: 4278-81 (2008)
Pfizer
Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase.
Bioorg Med Chem Lett 18: 5842-6 (2008)
The Scripps Research Institute
Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents.
J Med Chem 51: 4404-11 (2008)
Toray Industries
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
J Med Chem 51: 4449-55 (2008)
Leiden/Amsterdam Center For Drug Research
(9S)-9-(2-hydroxy-4,4-dimethyl-6-oxo-1-cyclohexen-1-yl)-3,3-dimethyl-2,3,4,9-tetrahydro-1H-xanthen-1-one, a selective and orally active neuropeptide Y Y5 receptor antagonist.
J Med Chem 51: 4765-70 (2008)
Tsukuba Research Institute
Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A.
J Med Chem 51: 4388-91 (2008)
University Of Belgrade
Structural basis for the potent calpain inhibitory activity of peptidyl alpha-ketoacids.
J Med Chem 51: 4346-50 (2008)
University Of Tennessee Health Science Center
Structure-activity relationship studies on vitamin D lactam derivatives as vitamin D receptor antagonist.
Bioorg Med Chem Lett 18: 4287-90 (2008)
Tokyo University Of Agriculture And Technology
Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors.
Bioorg Med Chem Lett 18: 4298-302 (2008)
Abbott Laboratories
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Bioorg Med Chem Lett 18: 4352-4 (2008)
Roche Palo Alto
Selective nucleoside triphosphate diphosphohydrolase-2 (NTPDase2) inhibitors: nucleotide mimetics derived from uridine-5'-carboxamide.
J Med Chem 51: 4518-28 (2008)
University Of Bonn
Structure-based development of novel adenylyl cyclase inhibitors.
J Med Chem 51: 4456-64 (2008)
Ruhr-University Bochum
Slow self-activation enhances the potency of viridin prodrugs.
J Med Chem 51: 4699-707 (2008)
Harvard Medical School
Identification and validation of human DNA ligase inhibitors using computer-aided drug design.
J Med Chem 51: 4553-62 (2008)
University Of Maryland
Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics.
J Med Chem 51: 4685-98 (2008)
Saarland University
A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability.
J Med Chem 51: 4465-75 (2008)
Genentech
Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase.
J Med Chem 51: 4392-403 (2008)
Institute For Chemical Biology
Synthesis and biological evaluation of some new N(4)-substituted isatin-3-thiosemicarbazones.
J Enzyme Inhib Med Chem 24: 437-46 (2009)
Bahauddin Zakariya University
Sesquiterpenes from the Hainan Sponge Dysidea septosa.
J Nat Prod 71: 1399-403 (2008)
Chinese Academy Of Sciences
Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors.
Bioorg Med Chem 16: 7167-76 (2008)
Piramal Life Sciences
Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
Bioorg Med Chem 16: 7117-27 (2008)
Zydus Research Centre
N-Benzyl-N-(pyrrolidin-3-yl)carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors.
Bioorg Med Chem Lett 18: 4308-11 (2008)
Pfizer
Synthesis and evaluation of alpha,alpha'-disubstituted phenylacetate derivatives for T-type calcium channel blockers.
Bioorg Med Chem Lett 18: 4424-7 (2008)
Institute Of Science And Technology
Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase.
Bioorg Med Chem Lett 18: 4348-51 (2008)
Roche Palo Alto
N-Acyl-3-amino-5H-furanone derivatives as new inhibitors of LuxR-dependent quorum sensing: Synthesis, biological evaluation and binding mode study.
Bioorg Med Chem Lett 18: 4321-4 (2008)
Insa
4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.
Bioorg Med Chem Lett 18: 4316-20 (2008)
Ucb Pharma
Amines and oximes derived from deoxybenzoins as Helicobacter pylori urease inhibitors.
Eur J Med Chem 44: 2246-51 (2009)
Nanjing University
High affinity conformationally constrained nociceptin/orphanin FQ(1-13) amide analogues.
J Med Chem 51: 4385-7 (2008)
University Of Maryland
QSAR study of imidazoline antihypertensive drugs.
Bioorg Med Chem 16: 7134-40 (2008)
University Of Belgrade
Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors.
Bioorg Med Chem Lett 18: 4388-92 (2008)
Harvard Medical School
Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.
Bioorg Med Chem Lett 18: 4355-9 (2008)
Pfizer
The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase.
Bioorg Med Chem Lett 18: 4373-6 (2008)
Gsk
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064.
Bioorg Med Chem Lett 18: 4339-43 (2008)
Gsk
N-(thiazol-2-yl)-2-thiophene carboxamide derivatives as Abl inhibitors identified by a pharmacophore-based database screening of commercially available compounds.
Bioorg Med Chem Lett 18: 4328-31 (2008)
Università
Novel inhibitors of anthrax edema factor.
Bioorg Med Chem 16: 7225-33 (2008)
University Of Texas Medical Branch
Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.
J Med Chem 51: 4632-40 (2008)
Gsk
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
J Med Chem 51: 4823-33 (2008)
Kyoto Pharmaceutical Industries
Selectivity determinants of inhibitor binding to human 20alpha-hydroxysteroid dehydrogenase: crystal structure of the enzyme in ternary complex with coenzyme and the potent inhibitor 3,5-dichlorosalicylic acid.
J Med Chem 51: 4844-8 (2008)
Monash University
Pyrazole inhibitors of coactivator associated arginine methyltransferase 1 (CARM1).
Bioorg Med Chem Lett 18: 4438-41 (2008)
Bristol-Myers Squibb Pharmaceutical Research And Development
Design, synthesis and evaluation of novel uracil acetamide derivatives as potential inhibitors of Plasmodium falciparum dUTP nucleotidohydrolase.
Eur J Med Chem 44: 678-88 (2009)
University Of Wales Cardiff
Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode.
Bioorg Med Chem Lett 18: 4442-6 (2008)
Astrazeneca Pharmaceuticals
Exploring 9-benzyl purines as inhibitors of glutamate racemase (MurI) in Gram-positive bacteria.
Bioorg Med Chem Lett 18: 4368-72 (2008)
Astrazeneca R&D Boston
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.
Bioorg Med Chem Lett 18: 4428-32 (2008)
Glaxosmithkline
Discovery of imidazole carboxamides as potent and selective CCK1R agonists.
Bioorg Med Chem Lett 18: 4393-6 (2008)
Merck Research Laboratories
Structure of daidzin, a naturally occurring anti-alcohol-addiction agent, in complex with human mitochondrial aldehyde dehydrogenase.
J Med Chem 51: 4482-7 (2008)
University Of Oxford
Naturally occurring homoisoflavonoids function as potent protein tyrosine kinase inhibitors by c-Src-based high-throughput screening.
J Med Chem 51: 4419-29 (2008)
Institute Of Materia Medica
In silico studies of urease inhibitors to explore ligand-enzyme interactions.
J Enzyme Inhib Med Chem 24: 151-6 (2009)
Quaid-I-Azam University
Inhibitory effects on mushroom tyrosinase by flavones from the stem barks of Morus lhou (S.) Koidz.
J Enzyme Inhib Med Chem 23: 922-30 (2008)
Gyeongsang National University
New tryptophanase inhibitors: towards prevention of bacterial biofilm formation.
J Enzyme Inhib Med Chem 24: 350-5 (2009)
Ben-Gurion University Of The Negev
Kinetic properties and inhibition of the dimeric dUTPase-dUDPase from Campylobacter jejuni.
J Enzyme Inhib Med Chem 24: 111-6 (2009)
Instituto De Parastiologia Y Biomedicina "Lopez-Neyra
Carbonic anhydrase inhibitors. Biphenylsulfonamides with inhibitory action towards the transmembrane, tumor-associated isozymes IX possess cytotoxic activity against human colon, lung and breast cancer cell lines.
J Enzyme Inhib Med Chem 24: 499-505 (2009)
Egyptian Petroleum Research Institute
Design and synthesis of substituted imidazole and triazole N-phenylbenzo[d]oxazolamine inhibitors of retinoic acid metabolizing enzyme CYP26.
J Enzyme Inhib Med Chem 24: 487-98 (2009)
Cardiff University
Synthesis and cytotoxic, anti-inflammatory, and anti-oxidant activities of 2',5'-dialkoxylchalcones as cancer chemopreventive agents.
Bioorg Med Chem 16: 7270-6 (2008)
Kaohsiung Medical University
Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP).
Bioorg Med Chem Lett 18: 4360-3 (2008)
Glaxosmithkline
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.
Bioorg Med Chem Lett 18: 4420-3 (2008)
Wyeth Research
Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists.
Bioorg Med Chem Lett 18: 4377-9 (2008)
F. Hoffmann-La Roche
The effect of 5-alkyl modification on the biological activity of pyrrolo[2,3-d]pyrimidine containing classical and nonclassical antifolates as inhibitors of dihydrofolate reductase and as antitumor and/or antiopportunistic infection agents.
J Med Chem 51: 4589-600 (2008)
Duquesne University
Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush.
J Med Chem 51: 4381-4 (2008)
University Of Bologna
Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging properties.
J Med Chem 51: 4751-64 (2008)
The Johns Hopkins University School Of Medicine
Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
J Med Chem 51: 4708-14 (2008)
University Of Washington
The discovery of small molecule chemical probes of Bcl-X(L) and Mcl-1.
Bioorg Med Chem 16: 7443-9 (2008)
Entremed
The influence of an ethylene spacer on the 5-HT(1A) and 5-HT(2A) receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones.
Eur J Med Chem 44: 800-8 (2009)
Jagiellonian University Medical College
Structure-activity correlations for beta-phenethylamines at human trace amine receptor 1.
Bioorg Med Chem 16: 7415-23 (2008)
Rti International
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Bioorg Med Chem Lett 18: 4433-7 (2008)
Glaxosmithkline
Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists.
Bioorg Med Chem Lett 18: 3844-7 (2008)
Korea Research Institute Of Chemical Technology
Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors.
Bioorg Med Chem Lett 18: 4087-91 (2008)
Ranbaxy Research Laboratories
A three-step synthesis from rebeccamycin of an efficient checkpoint kinase 1 inhibitor.
Eur J Med Chem 44: 2234-8 (2009)
Université
Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships.
Bioorg Med Chem 16: 6841-9 (2008)
Uppsala University
Functionalized pyrrolidine inhibitors of human type II alpha-mannosidases as anti-cancer agents: optimizing the fit to the active site.
Bioorg Med Chem 16: 7337-46 (2008)
Ecole Polytechnique FéDéRale De Lausanne
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
Eur J Med Chem 44: 809-17 (2009)
RzeszóW University Of Technology
Kinetic studies and bioactivity of potential manzamine prodrugs.
J Nat Prod 71: 1218-21 (2008)
The University Of Mississippi
Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.
J Med Chem 51: 4780-9 (2008)
Tsukuba Research Institute
Synthesis, biological evaluation, and enzyme docking simulations of 1,5-diarylpyrrole-3-alkoxyethyl ethers as selective cyclooxygenase-2 inhibitors endowed with anti-inflammatory and antinociceptive activity.
J Med Chem 51: 4476-81 (2008)
Universita Di Siena
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
J Med Chem 51: 4839-43 (2008)
Academy Of Sciences Of The Czech Republic
Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands.
J Med Chem 51: 4529-38 (2008)
Università
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
Bioorg Med Chem 16: 7311-20 (2008)
Alma Mater Studiorum-University Of Bologna
2-N-Methyl modifications and SAR studies of manzamine A.
Bioorg Med Chem 16: 6702-6 (2008)
The University Of Mississippi
In vitro inhibition of glycogen-degrading enzymes and glycosidases by six-membered sugar mimics and their evaluation in cell cultures.
Bioorg Med Chem 16: 7330-6 (2008)
Hokuriku University
Comparative molecular dynamics simulations of the potent synthetic classical cannabinoid ligand AMG3 in solution and at binding site of the CB1 and CB2 receptors.
Bioorg Med Chem 16: 7377-87 (2008)
The National Hellenic Research Foundation
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
Bioorg Med Chem 16: 7291-301 (2008)
Florida A&M University
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists.
Bioorg Med Chem Lett 18: 3848-51 (2008)
Abbott Bioresearch Center
Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists.
Bioorg Med Chem Lett 18: 3852-5 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Oxidative inactivation of protein tyrosine phosphatase 1B by organic hydroperoxides.
Bioorg Med Chem Lett 18: 5856-9 (2008)
University Of Missouri-Columbia
4-Hydroxy-5-pyrrolinone-3-carboxamide HIV-1 integrase inhibitors.
Bioorg Med Chem Lett 18: 3865-9 (2008)
Irbm-Mrl Rome
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition.
Bioorg Med Chem Lett 18: 3856-9 (2008)
Pfizer
Functional cloning and characterization of the multidrug efflux pumps NorM from Neisseria gonorrhoeae and YdhE from Escherichia coli.
Antimicrob Agents Chemother 52: 3052-60 (2008)
Iowa State University
Discovery of novel and potent aryl diamines as leukotriene A4 hydrolase inhibitors.
Bioorg Med Chem Lett 18: 3895-8 (2008)
Berlex Biosciences
Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.
J Med Chem 51: 4226-38 (2008)
University Of Bath
Structure of the BH3 domains from the p53-inducible BH3-only proteins Noxa and Puma in complex with Mcl-1.
J Mol Biol 380: 958-71 (2008)
University Of Otago
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
J Med Chem 51: 4150-69 (2008)
Johnson & Johnson Pharmaceutical
Ribose-modified purine nucleosides as ribonucleotide reductase inhibitors. Synthesis, antitumor activity, and molecular modeling of N6-substituted 3'-C-methyladenosine derivatives.
J Med Chem 51: 4260-9 (2008)
Università
SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: discovery of PSN-GK1.
J Med Chem 51: 4340-5 (2008)
(Osi) Prosidion
A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo.
Nat Chem Biol 4: 483-90 (2008)
Simon Fraser University
Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton.
Bioorg Med Chem 16: 7046-54 (2008)
The University Of Tokyo
Synthesis of N-alkyl glycine amides as potent inhibitors of leukotriene A4 hydrolase.
Bioorg Med Chem Lett 18: 3891-4 (2008)
Berlex Biosciences
Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.
Bioorg Med Chem Lett 18: 3955-8 (2008)
Abbott Laboratories
Synthesis of new dipyrrolo- and furopyrrolopyrazinones related to tripentones and their biological evaluation as potential kinases (CDKs1-5, GSK-3) inhibitors.
Eur J Med Chem 44: 708-16 (2009)
Université
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
Bioorg Med Chem 16: 7429-35 (2008)
Universit£
Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands.
Bioorg Med Chem Lett 18: 3919-24 (2008)
Zydus Research Centre
The molecular structure of epoxide hydrolase B from Mycobacterium tuberculosis and its complex with a urea-based inhibitor.
J Mol Biol 381: 897-912 (2008)
University Of Alberta
QSAR prediction of inhibition of aldose reductase for flavonoids.
Bioorg Med Chem 16: 7470-6 (2008)
Inifta (Unlp, Cct La Plata-Conicet)
A novel Syk family kinase inhibitor: design, synthesis, and structure-activity relationship of 1,2,4-triazolo[4,3-c]pyrimidine and 1,2,4-triazolo[1,5-c]pyrimidine derivatives.
Bioorg Med Chem 16: 7347-57 (2008)
Kissei Pharmaceutical
Homo- and hetero-bivalent edrophonium-like ammonium salts as highly potent, dual binding site AChE inhibitors.
Bioorg Med Chem 16: 7450-6 (2008)
Università
Synthesis and binding studies of 2-O- and 11-O-substituted N-alkylnoraporphines.
Bioorg Med Chem Lett 18: 3971-3 (2008)
Harvard Medical School
T-type Ca2+ channel blockers suppress the growth of human cancer cells.
Bioorg Med Chem Lett 18: 3899-901 (2008)
Kyung Hee University
Synthesis of macrocyclic trypanosomal cysteine protease inhibitors.
Bioorg Med Chem Lett 18: 5860-3 (2008)
Scripps Florida
Bis(sulfonamide) isosters of mycophenolic adenine dinucleotide analogues: inhibition of inosine monophosphate dehydrogenase.
Bioorg Med Chem 16: 7462-9 (2008)
University Of Minnesota
A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands.
Bioorg Med Chem Lett 18: 3929-31 (2008)
Wyeth Research
Isosteric exchange of the acylsulfonamide moiety in Abbott's Bcl-XL protein interaction antagonist.
Bioorg Med Chem Lett 18: 4115-7 (2008)
University Of Pittsburgh
Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR).
Bioorg Med Chem Lett 18: 3974-7 (2008)
Albert Einstein College Of Medicine
ERRgamma tethers strongly bisphenol A and 4-alpha-cumylphenol in an induced-fit manner.
Biochem Biophys Res Commun 373: 408-13 (2008)
Kyushu University
Illudalic acid as a potential LAR inhibitor: synthesis, SAR, and preliminary studies on the mechanism of action.
Bioorg Med Chem 16: 7399-409 (2008)
Chinese Academy Of Sciences
Novel sterically hindered cannabinoid CB1 receptor ligands.
Bioorg Med Chem 16: 7510-5 (2008)
University Of Salerno
Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid.
Bioorg Med Chem 16: 7424-8 (2008)
Universita Degli Studi Di Firenze
Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase.
Bioorg Med Chem Lett 18: 3942-5 (2008)
Kudos Pharmaceuticals
Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry.
Bioorg Med Chem Lett 18: 3978-81 (2008)
Sunesis Pharmaceuticals
Discovery of novel hydroxy-thiazoles as HIF-alpha prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation.
Bioorg Med Chem Lett 18: 3925-8 (2008)
Amgen
Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region.
J Med Chem 51: 4122-49 (2008)
Eberhard Karls University Tuebingen
Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model.
J Med Chem 51: 4068-71 (2008)
Wyeth Research
Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
J Med Chem 51: 4093-103 (2008)
Universite Blaise Pascal
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
J Med Chem 51: 4085-92 (2008)
Universite Blaise Pascal
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.
J Med Chem 51: 4289-99 (2008)
Universit£
N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
J Med Chem 51: 4179-87 (2008)
University Of Copenhagen
Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.
J Med Chem 51: 4239-52 (2008)
Merck Research Laboratories
Synthesis and pharmacological evaluation of novel gamma-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors.
J Med Chem 51: 4315-20 (2008)
Astrazeneca
Inhibition of the signal transducer and activator of transcription-3 (STAT3) signaling pathway by 4-oxo-1-phenyl-1,4-dihydroquinoline-3-carboxylic acid esters.
J Med Chem 51: 4115-21 (2008)
Wyeth Research
Is quantum mechanics necessary for predicting binding free energy?
J Med Chem 51: 4280-8 (2008)
University Of Z£Rich
Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.
Bioorg Med Chem Lett 18: 3950-4 (2008)
Glaxosmithkline
Discovery of novel 1,2,3,4-tetrahydroisoquinolines and 3,4-dihydroisoquinoline-1(2H)-ones as potent and selective inhibitors of KDR: synthesis, SAR, and pharmacokinetic properties.
Bioorg Med Chem Lett 18: 4054-8 (2008)
Amgen
New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
J Med Chem 51: 4270-9 (2008)
Hungarian Academy Of Sciences
Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.
Bioorg Med Chem Lett 18: 4075-80 (2008)
Bristol-Myers Squibb
Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors?
Bioorg Med Chem Lett 18: 3938-41 (2008)
Università
Discovery of selective and nonpeptidic cathepsin S inhibitors.
Bioorg Med Chem Lett 18: 3959-62 (2008)
Novartis Institutes For Biomedical Research
Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling.
Bioorg Med Chem 16: 6903-10 (2008)
Emory University
Synthesis, human telomerase inhibition and anti-proliferative studies of a series of 2,7-bis-substituted amido-anthraquinone derivatives.
Bioorg Med Chem 16: 6976-86 (2008)
National Defense Medical Center
Discovery of brain penetrant, soluble, pyrazole amide EP1 receptor antagonists.
Bioorg Med Chem Lett 18: 4027-32 (2008)
Glaxosmithkline
Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase.
Bioorg Med Chem Lett 18: 4006-10 (2008)
Ewha Womans University
Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives.
Bioorg Med Chem 16: 6707-23 (2008)
Wyeth Research
4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor.
Bioorg Med Chem 16: 6799-812 (2008)
The University Of Tokyo
Novel aminopeptidase N inhibitors derived from 1,3,4-thiadiazole scaffold.
Bioorg Med Chem 16: 6663-8 (2008)
Shandong University
Synthesis, biological evaluation and molecular modelling of N-heterocyclic dipeptide aldehydes as selective calpain inhibitors.
Bioorg Med Chem 16: 6911-23 (2008)
University Of Canterbury
Simultaneous identification of multiple receptors of natural product using an optimized cDNA phage display cloning.
Bioorg Med Chem Lett 18: 3995-8 (2008)
Chinese Academy Of Sciences
Designing rapid onset selective serotonin re-uptake inhibitors. 2: structure-activity relationships of substituted (aryl)benzylamines.
Bioorg Med Chem Lett 18: 4018-21 (2008)
Pfizer
Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts.
Bioorg Med Chem Lett 18: 3988-91 (2008)
Korea Research Institute Of Chemical Technology
Carbamates with differential mechanism of inhibition toward acetylcholinesterase and butyrylcholinesterase.
J Med Chem 51: 4200-12 (2008)
Dalhousie University
Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor.
J Med Chem 51: 4072-5 (2008)
Methylgene
The many roles for fluorine in medicinal chemistry.
J Med Chem 51: 4359-69 (2008)
Merck Research Laboratories
Potency and selectivity of trifluoroacetylimino and pyrazinoylimino nicotinic insecticides and their fit at a unique binding site niche.
J Med Chem 51: 4213-8 (2008)
University Of California
Investigation of the effects of some sulfonamide derivatives on the activities of glucose-6-phosphate dehydrogenase, 6-phospho gluconate dehydrogenase and glutathione reductase from human erythrocytes.
J Enzyme Inhib Med Chem 23: 418-23 (2008)
Dumlupinar University
alpha-Chymotrypsin inhibition studies on the lignans from Vitex negundo Linn.
J Enzyme Inhib Med Chem 23: 400-5 (2008)
University Of Karachi
Modulation of Anopheles gambiae Epsilon glutathione transferase activity by plant natural products in vitro.
J Enzyme Inhib Med Chem 23: 391-9 (2008)
University Of Zimbabwe
Butyrylcholinesterase, lipoxygenase inhibiting and antifungal alkaloids from Isatis tinctoria.
J Enzyme Inhib Med Chem 23: 313-6 (2008)
Pcsir Laboratories Complex
BACE1 inhibitory effects of lavandulyl flavanones from Sophora flavescens.
Bioorg Med Chem 16: 6669-74 (2008)
Gyeongsang National University School Of Medicine
Synthesis and biological activity of some new flavonyl-2,4-thiazolidinediones.
Bioorg Med Chem 16: 6747-51 (2008)
Ankara University
Modeling, analysis, and validation of a novel HIV integrase structure provide insights into the binding modes of potent integrase inhibitors.
J Mol Biol 380: 504-19 (2008)
Gilead Sciences
Structure-activity relationships of 7-deaza-6-benzylthioinosine analogues as ligands of Toxoplasma gondii adenosine kinase.
J Med Chem 51: 3934-45 (2008)
University Of Georgia
Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines.
Bioorg Med Chem 16: 6675-81 (2008)
Chinese Academy Of Sciences
Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists.
Bioorg Med Chem Lett 18: 4199-203 (2008)
Schering-Plough Research Institute
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.
Cancer Res 68: 4774-82 (2008)
Boehringer Ingelheim Austria
Xanthones from the botanical dietary supplement mangosteen (Garcinia mangostana) with aromatase inhibitory activity.
J Nat Prod 71: 1161-6 (2008)
University Of Illinois At Chicago
Spheciosterol sulfates, PKCzeta inhibitors from a philippine sponge Spheciospongia sp.
J Nat Prod 71: 1213-7 (2008)
University Of Utah
Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles.
J Med Chem 51: 3985-4001 (2008)
Nycomed
Ensemble-based virtual screening reveals potential novel antiviral compounds for avian influenza neuraminidase.
J Med Chem 51: 3878-94 (2008)
University Of California
The use of natural product scaffolds as leads in the search for trypanothione reductase inhibitors.
Bioorg Med Chem 16: 6689-95 (2008)
Pontificia Universidad Catolica Del Peru
Locking the two ends of tetrapeptidic HTLV-I protease inhibitors inside the enzyme.
Bioorg Med Chem 16: 6880-90 (2008)
Kyoto Pharmaceutical University
Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists.
Bioorg Med Chem Lett 18: 4204-9 (2008)
Schering-Plough Research Institute
Modulation of peripheral serotonin levels by novel tryptophan hydroxylase inhibitors for the potential treatment of functional gastrointestinal disorders.
J Med Chem 51: 3684-7 (2008)
Lexicon Pharmaceuticals
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors.
J Med Chem 51: 4038-49 (2008)
Wyeth Research
Synthesis and biological evaluation of substituted [18F]imidazo[1,2-a]pyridines and [18F]pyrazolo[1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positron emission tomography.
J Med Chem 51: 3700-12 (2008)
Radiopharmaceuticals Research Institute
7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.
J Med Chem 51: 3777-87 (2008)
Abbott Laboratories
Small neutralizing molecules to inhibit actions of the chemokine CXCL12.
J Biol Chem 283: 23189-99 (2008)
UniversitÉ
Synthesis and monoamine transporter binding properties of 2beta-[3'-(substituted benzyl)isoxazol-5-yl]- and 2beta-[3'-methyl-4'-(substituted phenyl)isoxazol-5-yl]-3beta-(substituted phenyl)tropanes.
Bioorg Med Chem 16: 6682-8 (2008)
Research Triangle Institute
Anti-retroviral and cytostatic activity of 2',3'-dideoxyribonucleoside 3'-disulfides.
Bioorg Med Chem 16: 6824-31 (2008)
Université
Ligands to the (IRAP)/AT4 receptor encompassing a 4-hydroxydiphenylmethane scaffold replacing Tyr2.
Bioorg Med Chem 16: 6924-35 (2008)
Uppsala University
Discovery of a novel series of Notch-sparing gamma-secretase inhibitors.
Bioorg Med Chem Lett 18: 4232-6 (2008)
Wyeth Research
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.
Bioorg Med Chem Lett 18: 4154-8 (2008)
University Of Antwerp
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors.
Bioorg Med Chem Lett 18: 4159-62 (2008)
University Of Antwerp
A re-examination of the difluoromethylenesulfonic acid group as a phosphotyrosine mimic for PTP1B inhibition.
Bioorg Med Chem 16: 6764-77 (2008)
University Of Waterloo
Novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives as dihydrofolate inhibitor: design, synthesis and antifolate activity.
Eur J Med Chem 44: 764-71 (2009)
Peking University
Design, synthesis, and structure-affinity relationship studies in NK1 receptor ligands based on azole-fused quinolinecarboxamide moieties.
Bioorg Med Chem 16: 6850-9 (2008)
Università
Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.
Bioorg Med Chem Lett 18: 4137-41 (2008)
Amgen
Amino acid anthranilamide derivatives as a new class of glycogen phosphorylase inhibitors.
Bioorg Med Chem Lett 18: 4068-71 (2008)
Glaxosmithkline
Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase.
Bioorg Med Chem Lett 18: 4181-5 (2008)
Anadys Pharmaceuticals
Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors.
Bioorg Med Chem Lett 18: 4210-4 (2008)
University Of Algarve
Novel H3 receptor antagonists with improved pharmacokinetic profiles.
Bioorg Med Chem Lett 18: 4133-6 (2008)
Arena Pharmaceuticals
(D)-2-tert-Butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid: synthesis and incorporation into the growth hormone secretagogues.
Bioorg Med Chem Lett 18: 4072-4 (2008)
Bristol Myers Squibb
Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).
J Med Chem 51: 3688-91 (2008)
Amgen
A tissue-selective nonsteroidal progesterone receptor modulator: 7,9-difluoro-5-(3-methylcyclohex-2-enyl)-2,2,4-trimethyl-1,2-dihydrochromeno[3,4-f]quinoline.
J Med Chem 51: 3696-9 (2008)
Ligand Pharmaceuticals
2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.
J Med Chem 51: 3946-52 (2008)
Merck Research Laboratories
Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model.
J Med Chem 51: 3953-60 (2008)
Amgen
Discovery of a novel series of biphenyl benzoic acid derivatives as highly potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. Part II.
J Med Chem 51: 4002-20 (2008)
Astellas Pharma
The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity.
Bioorg Med Chem Lett 18: 4191-4 (2008)
Merck Research Laboratories
Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.
Bioorg Med Chem Lett 18: 4098-101 (2008)
Vanderbilt University Medical Center
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
Bioorg Med Chem Lett 18: 4118-23 (2008)
Bristol-Myers Squibb
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
Bioorg Med Chem Lett 18: 4224-7 (2008)
Neurocrine Biosciences
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.
Eur J Med Chem 44: 772-84 (2009)
Zhejiang University
New trypanocidal hybrid compounds from the association of hydrazone moieties and benzofuroxan heterocycle.
Bioorg Med Chem 16: 6995-7004 (2008)
Unviersidad De La RepÚBlica
Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.
Bioorg Med Chem Lett 18: 4168-71 (2008)
Schering-Plough Research Institute
Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.
Bioorg Med Chem Lett 18: 4242-8 (2008)
Astrazeneca R&D Boston
3-Alkenyl-2-azetidinones as fatty acid amide hydrolase inhibitors.
Bioorg Med Chem Lett 18: 4163-7 (2008)
Université
Anti-HIV-1 protease activity of lanostane triterpenes from the vietnamese mushroom Ganoderma colossum.
J Nat Prod 71: 1022-6 (2008)
University Of Toyama
Alpha-glucosidase inhibitor from Kothala-himbutu (Salacia reticulata WIGHT).
J Nat Prod 71: 981-4 (2008)
Fuji-Sangyo
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.
J Med Chem 51: 3905-12 (2008)
Universit£
Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.
J Med Chem 51: 4030-7 (2008)
University Of Berne
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
Antimicrob Agents Chemother 52: 2861-9 (2008)
Katholieke Universiteit Leuven
Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Bioorg Med Chem 16: 6965-75 (2008)
Abbott Laboratories
Affinity of 3-acyl substituted 4-quinolones at the benzodiazepine site of GABA(A) receptors.
Bioorg Med Chem 16: 6936-48 (2008)
Lund University
Synthesis and biological evaluation of 1-(benzenesulfonamido)-2-[5-(N-hydroxypyridin-2(1H)-one)]acetylene regioisomers: a novel class of 5-lipoxygenase inhibitors.
Bioorg Med Chem Lett 18: 4195-8 (2008)
University Of Alberta
The metabolism of CYP2C9 and CYP2C19 for gliclazide by homology modeling and docking study.
Eur J Med Chem 44: 854-61 (2009)
Jilin University
Thermodynamic and structure guided design of statin based inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase.
J Med Chem 51: 3804-13 (2008)
Boehringer Ingelheim Pharmaceuticals
Theoretical studies on the structure and symmetry of the transmembrane region of glutamatergic GluR5 receptor.
J Med Chem 51: 3765-76 (2008)
Medical University Of Lublin
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
J Med Chem 51: 3692-5 (2008)
Merck Research Laboratories
Synthesis and screening of small molecule inhibitors of anthrax edema factor.
Bioorg Med Chem Lett 18: 4215-8 (2008)
The University Of Texas Medical Branch
Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors.
Bioorg Med Chem Lett 18: 4186-90 (2008)
Merck Research Laboratories
Pyrazolopyridines as a novel structural class of potent and selective PDE4 inhibitors.
Bioorg Med Chem Lett 18: 4237-41 (2008)
Glaxosmithkline
Imidazopyridines as VLA-4 integrin antagonists.
Bioorg Med Chem Lett 18: 4146-9 (2008)
Ucb Pharma
Identification of novel non-peptide CXCR4 antagonists by ligand-based design approach.
Bioorg Med Chem Lett 18: 4124-9 (2008)
Kyoto University
Discovery of potent CCR4 antagonists: Synthesis and structure-activity relationship study of 2,4-diaminoquinazolines.
Bioorg Med Chem 16: 7021-32 (2008)
Astellas Pharma
2-Substituted-16-ene-22-thia-1alpha,25-dihydroxy-26,27-dimethyl-19-norvitamin D3 analogs: Synthesis, biological evaluation, and crystal structure.
Bioorg Med Chem 16: 6949-64 (2008)
Tokyo Medical And Dental University
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
Bioorg Med Chem Lett 18: 3682-6 (2008)
Neurocrine Biosciences
Protein subtype-targeting through ligand epimerization: talose-selectivity of galectin-4 and galectin-8.
Bioorg Med Chem Lett 18: 3691-4 (2008)
Lund University
Discovery of potent, orally active benzimidazole glucagon receptor antagonists.
Bioorg Med Chem Lett 18: 3701-5 (2008)
Merck Research Laboratories
Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells.
Bioorg Med Chem Lett 18: 3745-8 (2008)
Cardiff University
Petrosamine, a potent anticholinesterase pyridoacridine alkaloid from a Thai marine sponge Petrosia n. sp.
Bioorg Med Chem 16: 6560-7 (2008)
Mahidol University
Three-dimensional QSAR analyses of 1,3,4-trisubstituted pyrrolidine-based CCR5 receptor inhibitors.
Eur J Med Chem 43: 2724-34 (2008)
Beijing University Of Technology
A novel class of cycloalkano[b]pyridines as potent and orally active opioid receptor-like 1 antagonists with minimal binding affinity to the hERG K+ channel.
J Med Chem 51: 4021-9 (2008)
Tsukuba Research Institute
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
J Med Chem 51: 3788-803 (2008)
Moltech
[11C]cyclopropyl-FLB 457: a PET radioligand for low densities of dopamine D2 receptors.
Bioorg Med Chem 16: 6467-73 (2008)
Institutet
Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine-5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors.
Bioorg Med Chem 16: 6509-21 (2008)
Astellas Pharma
Dopamine/serotonin receptor ligands. Part 17: a cross-target SAR approach: affinities of azecine-styled ligands for 5-HT(2A) versus D1 and D2 receptors.
Bioorg Med Chem Lett 18: 3809-13 (2008)
Friedrich-Schiller-Universit£T Jena
Characterization of the drug binding specificity of rat liver fatty acid binding protein.
J Med Chem 51: 3755-64 (2008)
Monash University (Parkville Campus)
Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries.
J Med Chem 51: 4188-99 (2008)
University Of Innsbruck
Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.
J Med Chem 51: 3814-24 (2008)
Eberhard-Karls University
Sodium late current blockers in ischemia reperfusion: is the bullet magic?
J Med Chem 51: 3856-66 (2008)
Pierre Fabre Research Center
Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.
J Med Chem 51: 3825-40 (2008)
University Of Sydney
Exploring the substituent effects on a novel series of C1'-dimethyl-aryl Delta8-tetrahydrocannabinol analogs.
Bioorg Med Chem 16: 6489-500 (2008)
University Of Tennessee-Memphis
First synthesis of alpha-aminoalkyl-(N-substituted)thiocarbamoyl-phosphinates: inhibitors of aminopeptidase N (APN/CD13) with the new zinc-binding group.
Bioorg Med Chem Lett 18: 3734-6 (2008)
Wroc£?Aw University Of Technology
Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.
Bioorg Med Chem Lett 18: 3741-4 (2008)
Università
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
Bioorg Med Chem Lett 18: 3716-9 (2008)
Glaxosmithkline
Development of a novel fluorescent probe for fluorescence correlation spectroscopic detection of kinase inhibitors.
Bioorg Med Chem Lett 18: 3752-5 (2008)
The University Of Tokyo
Design, synthesis and evaluation of isaindigotone derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors.
Bioorg Med Chem Lett 18: 3790-3 (2008)
Sun Yat-Sen University
Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design.
Bioorg Med Chem Lett 18: 3706-10 (2008)
Merck Research Laboratories
Design, synthesis and characterization of N9/N7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors.
Eur J Med Chem 44: 1788-93 (2009)
Eberhard-Karls University
A class of potent tyrosinase inhibitors: alkylidenethiosemicarbazide compounds.
Eur J Med Chem 44: 1773-8 (2009)
Sun Yat-Sen University
Novel benzimidazole derivatives as selective CB2 agonists.
Bioorg Med Chem Lett 18: 3695-700 (2008)
Astrazeneca R&D MontréAl
Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum.
J Med Chem 51: 3649-53 (2008)
University Of Texas At Dallas
Chemically induced dimerization of human nonpancreatic secretory phospholipase A2 by bis-indole derivatives.
J Med Chem 51: 3360-6 (2008)
Peking University
Potent in vitro activity of tomopenem (CS-023) against methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosa.
Antimicrob Agents Chemother 52: 2849-54 (2008)
Daiichi Sankyo
Synthesis and biological activities of reveromycin A and spirofungin A derivatives.
Bioorg Med Chem Lett 18: 3756-60 (2008)
Riken (Institute Of Physical And Chemical Research)
Naturally Occurring Pentacyclic Triterpenes as Inhibitors of Glycogen Phosphorylase: Synthesis, Structure-Activity Relationships, and X-ray Crystallographic Studies.
J Med Chem 51: 3540-54 (2008)
China Pharmaceutical University
1-[(Imidazolidin-2-yl)imino]indazole. Highly alpha 2/I1 selective agonist: synthesis, X-ray structure, and biological activity.
J Med Chem 51: 3599-608 (2008)
Medical University Of Gda£?Sk
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
J Med Chem 51: 3588-98 (2008)
Laboratori De Qu�Mica Farmac�Utica (Unitat Associada Al Csic)
Synthesis of 3',4'-epoxynoraristeromycin analogs for molecular labeling probe of S-adenosyl-l-homocysteine hydrolase.
Bioorg Med Chem 16: 6575-9 (2008)
Gifu University
Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine.
Bioorg Med Chem Lett 18: 3778-82 (2008)
Tsukuba Research Institute
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.
Bioorg Med Chem 16: 6319-32 (2008)
Niddk
Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.
Bioorg Med Chem 16: 6423-35 (2008)
Saarland University
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.
Bioorg Med Chem Lett 18: 3504-8 (2008)
Ligand Pharmaceuticals
Carbonic anhydrase inhibitors: design of spin-labeled sulfonamides incorporating TEMPO moieties as probes for cytosolic or transmembrane isozymes.
Bioorg Med Chem Lett 18: 3475-80 (2008)
Universit£
Design, synthesis and evaluation of potent thymidylate synthase X inhibitors.
Bioorg Med Chem Lett 18: 3628-31 (2008)
Ecole Nationale Sup£Rieure De Chimie De Paris
Phloroglucinols with antioxidant activity and xanthonolignoids from the heartwood of Hypericum geminiflorum.
J Nat Prod 71: 1027-31 (2008)
Kaohsiung Medical University
Conformationally constrained analogues of N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716): design, synthesis, computational analysis, and biological evaluations.
J Med Chem 51: 3526-39 (2008)
Research Triangle Institute
2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.
Bioorg Med Chem 16: 6617-40 (2008)
Wyeth Research
Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1).
Bioorg Med Chem Lett 18: 3513-6 (2008)
Amgen
Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma agonists.
Bioorg Med Chem Lett 18: 3545-50 (2008)
Bristol-Myers Squibb R & D
Analogs of JHU75528, a PET ligand for imaging of cerebral cannabinoid receptors (CB1): development of ligands with optimized lipophilicity and binding affinity.
Eur J Med Chem 44: 593-608 (2009)
Johns Hopkins University School Of Medicine
Clavatadine A, a natural product with selective recognition and irreversible inhibition of factor XIa.
J Med Chem 51: 3583-7 (2008)
Griffith University
TrkA kinase inhibitors from a library of modified and isosteric Staurosporine aglycone.
Bioorg Med Chem Lett 18: 3551-5 (2008)
Cephalon
Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases.
Bioorg Med Chem Lett 18: 3495-9 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates.
J Med Chem 51: 3487-98 (2008)
Università
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.
J Med Chem 51: 3422-36 (2008)
Takeda Pharmaceutical
Homology modeling and site-directed mutagenesis to identify selective inhibitors of endothelin-converting enzyme-2.
J Med Chem 51: 3378-87 (2008)
Mount Sinai School Of Medicine
Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
J Med Chem 51: 3609-16 (2008)
Theravance
Flavonoids for controlling starch digestion: structural requirements for inhibiting human alpha-amylase.
J Med Chem 51: 3555-61 (2008)
Nestle Research Center
Synthesis and Biological Evaluation of d-Amino Acid Oxidase Inhibitors.
J Med Chem 51: 3357-9 (2008)
Mgi Pharma
Comparative study of the susceptibilities of major epidemic clones of methicillin-resistant Staphylococcus aureus to oxacillin and to the new broad-spectrum cephalosporin ceftobiprole.
Antimicrob Agents Chemother 52: 2709-17 (2008)
The Rockefeller University
Pyronane monoterpenoids from the fruit of Gardenia jasminoides.
J Nat Prod 71: 995-9 (2008)
Chungnam National University
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
Bioorg Med Chem 16: 6589-600 (2008)
Wyeth Research
Parallel one-pot synthesis and structure-activity relationship study of symmetric formimidoester disulfides as a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Bioorg Med Chem 16: 6353-63 (2008)
Universit£
Inhibitory effects of a series of 7-substituted-indazoles toward nitric oxide synthases: particular potency of 1H-indazole-7-carbonitrile.
Bioorg Med Chem 16: 5962-73 (2008)
Université
2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as inhibitors of glycogen synthase kinase-3 (GSK-3).
Bioorg Med Chem Lett 18: 3578-81 (2008)
Kemia
Development of potent and selective small-molecule human Urotensin-II antagonists.
Bioorg Med Chem Lett 18: 3500-3 (2008)
Glaxosmithkline
Novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin-1-yl)propyl]-1,2,4-oxadiazole-5-carboxamides as selective GSK-3 inhibitors.
Bioorg Med Chem Lett 18: 3661-6 (2008)
Chemical Diversity Research Institute
A peptoid antagonist of VEGF receptor 2 recognizes a 'hotspot' in the extracellular domain distinct from the hormone-binding site.
Bioorg Med Chem 16: 6338-43 (2008)
University Of Texas Southwestern Medical Center
Structure-activity relationships of a peptide inhibitor of the human FcRn:human IgG interaction.
Bioorg Med Chem 16: 6394-405 (2008)
Syntonix Pharmaceuticals
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.
Bioorg Med Chem 16: 6379-86 (2008)
Abbott Laboratories
IRAK-4 inhibitors. Part III: a series of imidazo[1,2-a]pyridines.
Bioorg Med Chem Lett 18: 3656-60 (2008)
Ucb Pharma
Synthesis and structure-activity relationship of aminopyrimidine IKK2 inhibitors.
Bioorg Med Chem Lett 18: 3622-7 (2008)
Ucb Pharma
Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway.
Bioorg Med Chem Lett 18: 3603-6 (2008)
Nicholas Piramal Research Centre
Carbonic anhydrase inhibitors: Inhibition of the new membrane-associated isoform XV with phenols.
Bioorg Med Chem Lett 18: 3593-6 (2008)
Universit£
Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment.
Bioorg Med Chem Lett 18: 3641-5 (2008)
Wyeth Research
Analogues of N-hydroxy-N'-phenylthiourea and N-hydroxy-N'-phenylurea as inhibitors of tyrosinase and melanin formation.
Bioorg Med Chem Lett 18: 3607-10 (2008)
Mayoly Spindler
Discovery of novel small-molecule inhibitors of human epidermal growth factor receptor-2: combined ligand and target-based approach.
J Med Chem 51: 3367-77 (2008)
University Of Southern California
Design, synthesis and spectroscopic studies of resveratrol aliphatic acid ligands of human serum albumin.
Bioorg Med Chem 16: 6406-14 (2008)
East Tennessee State University
Design and synthesis of 2-pyridones as novel inhibitors of the Bacillus anthracis enoyl-ACP reductase.
Bioorg Med Chem Lett 18: 3565-9 (2008)
University Of Illinois At Chicago
Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype.
Bioorg Med Chem Lett 18: 3646-51 (2008)
University Of Pennsylvania
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
Eur J Med Chem 44: 519-25 (2009)
Institut FüR Pharmazeutische Und Medizinische Chemie
Structure-based optimization of a potent class of arylamide FMS inhibitors.
Bioorg Med Chem Lett 18: 3632-7 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense.
J Nat Prod 71: 972-80 (2008)
Heinrich-Heine-Universit£T
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
J Med Chem 51: 3437-48 (2008)
University Of Illinois At Chicago
4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4 (CDK4).
J Med Chem 51: 3507-25 (2008)
Wyeth Research
Identification of MMP-12 inhibitors by using biosensor-based screening of a fragment library.
J Med Chem 51: 3449-59 (2008)
Uppsala University
Development of paramagnetic probes for molecular recognition studies in protein kinases.
J Med Chem 51: 3460-5 (2008)
Institute For Medical Research
Synthesis, induced-fit docking investigations, and in vitro aldose reductase inhibitory activity of non-carboxylic acid containing 2,4-thiazolidinedione derivatives.
Bioorg Med Chem 16: 5840-52 (2008)
Universit£
Biosynthesis and recycling of nicotinamide cofactors in mycobacterium tuberculosis. An essential role for NAD in nonreplicating bacilli.
J Biol Chem 283: 19329-41 (2008)
National Institutes Of Health
High-throughput evaluation of relative cell permeability between peptoids and peptides.
Bioorg Med Chem 16: 5853-61 (2008)
University Of Texas Southwestern Medical Center
Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Bioorg Med Chem 16: 6415-22 (2008)
Lanzhou University
Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity.
Bioorg Med Chem Lett 18: 3611-5 (2008)
Pfizer
Synthesis and biological evaluation of a library of resveratrol analogues as inhibitors of COX-1, COX-2 and NF-kappaB.
Bioorg Med Chem 17: 1044-54 (2009)
Purdue University
Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter.
Bioorg Med Chem 16: 6364-70 (2008)
Hadassah Hebrew University Hospital
Substituted dipiperidine alcohols as potent CCR2 antagonists.
Bioorg Med Chem Lett 18: 3562-4 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Pyrrolo[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.
Bioorg Med Chem Lett 18: 3616-21 (2008)
Anadys Pharmaceuticals
Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.
Bioorg Med Chem Lett 18: 3667-71 (2008)
Adolor
Synthesis, HIV-RT inhibitory activity and SAR of 1-benzyl-1H-1,2,3-triazole derivatives of carbohydrates.
Eur J Med Chem 44: 373-83 (2009)
Universidade Federal Fluminense
Synthesis and serotonin receptor activity of the arylpiperazine alkyl/propoxy derivatives of new azatricycloundecanes.
Eur J Med Chem 44: 152-64 (2008)
Institute Of Pharmacology Of The Polish Academy Of Sciences
Lycoparins A-C, new alkaloids from Lycopodium casuarinoides inhibiting acetylcholinesterase.
Bioorg Med Chem 16: 6167-71 (2008)
Hoshi University
Evaluation of novel hyphodermin derivatives as glycogen phosphorylase a inhibitors.
Bioorg Med Chem 16: 6172-8 (2008)
Griffith University
Design and synthesis of 7-alkoxy-4-heteroarylamino-3-quinolinecarbonitriles as dual inhibitors of c-Src kinase and nitric oxide synthase.
Bioorg Med Chem 16: 5890-8 (2008)
China Pharmaceutical University
3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors.
Bioorg Med Chem Lett 18: 3158-62 (2008)
Boehringer Ingelheim Pharma
Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Bioorg Med Chem Lett 18: 3168-72 (2008)
Bristol-Myers Squibb
Structure-based design of an organoruthenium phosphatidyl-inositol-3-kinase inhibitor reveals a switch governing lipid kinase potency and selectivity.
ACS Chem Biol 3: 305-16 (2008)
University Of Pennsylvania
New PPARgamma ligands based on 2-hydroxy-1,4-naphthoquinone: computer-aided design, synthesis, and receptor-binding studies.
Bioorg Med Chem Lett 18: 3192-5 (2008)
National Institute Of Pharmaceutical Education And Research
IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding.
Bioorg Med Chem Lett 18: 3291-5 (2008)
Ucb Pharma
Identification of halosalicylamide derivatives as a novel class of allosteric inhibitors of HCV NS5B polymerase.
Bioorg Med Chem Lett 18: 3173-7 (2008)
Abbott Laboratories
Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.
Bioorg Med Chem Lett 18: 3242-7 (2008)
Merck Research Laboratories
Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.
Bioorg Med Chem Lett 18: 3224-9 (2008)
Bristol-Myers Squibb Research And Development
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.
Bioorg Med Chem Lett 18: 3178-82 (2008)
Merck Research Laboratories
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.
J Med Chem 51: 3154-70 (2008)
Universit£
Synthesis and evaluation of [2-(4-quinolyloxy)phenyl]methanone derivatives: novel selective inhibitors of transforming growth factor-beta kinase.
J Med Chem 51: 3326-9 (2008)
Kirin Pharma
Design, synthesis, and evaluation of potential inhibitors of nitric oxide synthase.
Bioorg Med Chem 16: 6193-206 (2008)
Instituto De QuíMica MéDica
Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor.
Bioorg Med Chem Lett 18: 3200-5 (2008)
Merck Frosst Centre For Therapeutic Research
Effects of amide constituents from pepper on adipogenesis in 3T3-L1 cells.
Bioorg Med Chem Lett 18: 3272-7 (2008)
Kyoto Pharmaceutical University
Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists.
Bioorg Med Chem Lett 18: 3163-7 (2008)
Merck Research Laboratories
Design of antiangiogenic hypoxic cell radiosensitizers: 2-nitroimidazoles containing a 2-aminomethylene-4-cyclopentene-1,3-dione moiety.
Bioorg Med Chem 16: 6042-53 (2008)
The University Of Tokushima
IRAK-4 inhibitors. Part 1: a series of amides.
Bioorg Med Chem Lett 18: 3211-4 (2008)
Ucb Pharma
Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold.
J Med Chem 51: 3261-74 (2008)
Cancer Research Uk Centre For Cancer Therapeutics
Synthesis, fluorine-18 radiolabeling, and in vitro characterization of 1-iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivatives as potential PET radioligands for imaging peripheral benzodiazepine receptor.
Bioorg Med Chem 16: 6145-55 (2008)
Emory University
Steroidal lactones as inhibitors of 17beta-hydroxysteroid dehydrogenase type 5: chemical synthesis, enzyme inhibitory activity, and assessment of estrogenic and androgenic activities.
Eur J Med Chem 44: 632-44 (2009)
Chul Research Center And University Laval
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.
Nat Chem Biol 4: 357-65 (2008)
Nerviano Medical Sciences Oncology
Conformation-opioid activity relationships of bicyclic guanidines from 3D similarity analysis.
Bioorg Med Chem 16: 5932-8 (2008)
Torrey Pines Institute For Molecular Studies
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.
Bioorg Med Chem 16: 6116-23 (2008)
Purdue University
Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.
Bioorg Med Chem Lett 18: 3230-5 (2008)
Neurocrine Bioscience
Identification of novel benzimidazole series of potent and selective ORL1 antagonists.
Bioorg Med Chem Lett 18: 3278-81 (2008)
Banyu Tsukuba Research Institute
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.
Bioorg Med Chem Lett 18: 3236-41 (2008)
Schering-Plough Research Institute
Synthesis, ligand-receptor modeling studies and pharmacological evaluation of novel 4-modified-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent and selective human A3 adenosine receptor antagonists.
Bioorg Med Chem 16: 6086-102 (2008)
Universita' Di Firenze
Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
Bioorg Med Chem 16: 6286-96 (2008)
University Of Queensland
Design, synthesis, and QSAR studies of novel lysine derives as amino-peptidase N/CD13 inhibitors.
Bioorg Med Chem 16: 5473-81 (2008)
Shandong University
Identification of non-lipid LPA3 antagonists by virtual screening.
Bioorg Med Chem 16: 6207-17 (2008)
The University Of Memphis
Substituted benzyl-pyrimidines targeting thymidine monophosphate kinase of Mycobacterium tuberculosis: synthesis and in vitro anti-mycobacterial activity.
Bioorg Med Chem 16: 6075-85 (2008)
Cnrs
Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.
Bioorg Med Chem 16: 5514-28 (2008)
Duquesne University
Design and evaluation of a novel series of 2,3-oxidosqualene cyclase inhibitors with low systemic exposure, relationship between pharmacokinetic properties and ocular toxicity.
Bioorg Med Chem 16: 6218-32 (2008)
Laboratoire Glaxosmithkline
'Hybrid' benzofuran-benzopyran congeners as rigid analogs of hallucinogenic phenethylamines.
Bioorg Med Chem 16: 6242-51 (2008)
University Of Wisconsin-La Crosse
Evaluation of the amino acid binding site of Mycobacterium tuberculosis glutamine synthetase for drug discovery.
Bioorg Med Chem 16: 5501-13 (2008)
Uppsala University
Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy.
Bioorg Med Chem Lett 18: 3392-9 (2008)
Glaxosmithkline
Selective inhibition of aromatase by a dihydroisocoumarin from Xyris pterygoblephara.
J Nat Prod 71: 1082-4 (2008)
Universidade Federal De Minas Gerais
A prodomain peptide of Plasmodium falciparum cysteine protease (falcipain-2) inhibits malaria parasite development.
J Med Chem 51: 3116-23 (2008)
International Center For Genetic Engineering And Biotechnology
Trifluoromethoxyl substituted phenylethylene diamines as high affinity sigma receptor ligands with potent anti-cocaine actions.
J Med Chem 51: 3322-5 (2008)
University Of Maryland
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.
J Med Chem 51: 3145-53 (2008)
Gedeon Richter
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
J Med Chem 51: 4059-67 (2008)
Merck Frosst Centre For Therapeutic Research
Interaction of antagonists with calmodulin: insights from molecular dynamics simulations.
J Med Chem 51: 3081-93 (2008)
Semmelweis University
Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors.
J Med Chem 51: 3077-80 (2008)
University Of Namur
Chemical target validation studies of aminopeptidase in malaria parasites using alpha-aminoalkylphosphonate and phosphonopeptide inhibitors.
Antimicrob Agents Chemother 52: 3221-8 (2008)
Trinity College
Synthesis and in vitro antimycobacterial activity of B-ring modified diaryl ether InhA inhibitors.
Bioorg Med Chem Lett 18: 3029-33 (2008)
Stony Brook University
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
J Med Chem 51: 3275-87 (2008)
Uppsala University
Recent developments in fragment-based drug discovery.
J Med Chem 51: 3661-80 (2008)
Astex Therapeutics
Synthesis and antibacterial activity of novel pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid derivatives carrying the 3-cyclopropylaminomethyl-4-substituted-1-pyrrolidinyl group as a C-10 substituent.
J Med Chem 51: 3238-49 (2008)
Kyorin Pharmaceutical
Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.
J Med Chem 51: 3313-7 (2008)
Gsk
Preparation of piperazine derivatives as 5-HT7 receptor antagonists.
Bioorg Med Chem 16: 5405-12 (2008)
Ewha Womans University
Synthesis and structure based optimization of novel Akt inhibitors.
Bioorg Med Chem Lett 18: 3359-63 (2008)
Pfizer
Muscarinic antagonists with multiple stereocenters: Synthesis, affinity profile and functional activity of isomeric 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine sulfoxide derivatives.
Bioorg Med Chem 16: 5490-500 (2008)
Universit£
The discovery of fused pyrrole carboxylic acids as novel, potent D-amino acid oxidase (DAO) inhibitors.
Bioorg Med Chem Lett 18: 3386-91 (2008)
Merck Sharp & Dohme
Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility.
Nat Chem Biol 4: 347-56 (2008)
The Scripps Research Institute
Support vector machines classification of hERG liabilities based on atom types.
Bioorg Med Chem 16: 6252-60 (2008)
F. Hoffmann-La Roche
Aminopyrazine CB1 receptor inverse agonists.
Bioorg Med Chem Lett 18: 3376-81 (2008)
Neurogen
Demonstration of direct binding of cIAP1 degradation-promoting bestatin analogs to BIR3 domain: Synthesis and application of fluorescent bestatin ester analogs.
Bioorg Med Chem Lett 18: 3354-8 (2008)
The University Of Tokyo
Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.
Bioorg Med Chem Lett 18: 3282-5 (2008)
Banyu Tsukuba Research Institute
Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.
J Med Chem 51: 3061-4 (2008)
Schering-Plough Research Institute
Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.
J Med Chem 51: 3065-8 (2008)
Amgen
P2Y1 receptor antagonists as novel antithrombotic agents.
Bioorg Med Chem Lett 18: 3338-43 (2008)
Pfizer
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.
Bioorg Med Chem Lett 18: 3328-32 (2008)
Neurocrine Bioscience
Changes in the plasmodial surface anion channel reduce leupeptin uptake and can confer drug resistance in Plasmodium falciparum-infected erythrocytes.
Antimicrob Agents Chemother 52: 2346-54 (2008)
National Institute Of Allergy And Infectious Diseases
Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
Bioorg Med Chem Lett 18: 3431-5 (2008)
Ligand Pharmaceuticals
Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.
Bioorg Med Chem Lett 18: 3301-5 (2008)
Neurocrine Biosciences
Design and synthesis of N-alkyl oxindolylidene acetic acids as a new class of potent Cdc25A inhibitors.
Bioorg Med Chem Lett 18: 3350-3 (2008)
Doshisha Women'S College Of Liberal Arts
Novel bis-(arylsulfonamide) hydroxamate-based selective MMP inhibitors.
Bioorg Med Chem Lett 18: 3333-7 (2008)
North Dakota State University
5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers.
Bioorg Med Chem Lett 18: 3344-9 (2008)
Neurocrine Biosciences
The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives.
Bioorg Med Chem Lett 18: 3310-4 (2008)
Pfizer
Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Bioorg Med Chem Lett 18: 3412-6 (2008)
Merck Research Laboratories
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Bioorg Med Chem Lett 18: 3405-11 (2008)
Merck Research Laboratories
Design, synthesis and evaluation of novel sulfonyl pyrrolidine derivatives as matrix metalloproteinase inhibitors.
Bioorg Med Chem 16: 5398-404 (2008)
Shandong University
2-Trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors.
Bioorg Med Chem Lett 18: 3456-61 (2008)
Irbm/Merck Research Laboratories
Substituted benzo[d]oxazol-2(3H)-one derivatives with preference for the sigma1 binding site.
Eur J Med Chem 44: 124-30 (2008)
University Of Trieste
Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists.
J Med Chem 51: 3030-4 (2008)
Abbott Laboratories
Activation of the endocannabinoid system by organophosphorus nerve agents.
Nat Chem Biol 4: 373-8 (2008)
University Of California
Bis-tetrahydroisoquinoline derivatives: AG525E1, a new step in the search for non-quaternary non-peptidic small conductance Ca(2+)-activated K(+) channel blockers.
Bioorg Med Chem Lett 18: 3440-5 (2008)
University Of Li£Ge
Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.
Eur J Med Chem 44: 7-17 (2008)
Zhejiang University
Novel 2-aryl-naphtho[1,2-d]oxazole derivatives as potential PTP-1B inhibitors showing antihyperglycemic activities.
Eur J Med Chem 44: 109-16 (2008)
Central Drug Research Institute
Synthesis of 5-chloro-N-aryl-1H-indole-2-carboxamide derivatives as inhibitors of human liver glycogen phosphorylase a.
Bioorg Med Chem 16: 5452-64 (2008)
Astellas Pharma
Synthesis and receptor binding properties of 2beta-alkynyl and 2beta-(1,2,3-triazol)substituted 3beta-(substituted phenyl)tropane derivatives.
Bioorg Med Chem 16: 5529-35 (2008)
Research Triangle Institute
Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.
Bioorg Med Chem Lett 18: 2900-4 (2008)
Lg Life Sciences
Farnesyl pyrophosphate synthase enantiospecificity with a chiral risedronate analog, [6,7-dihydro-5H-cyclopenta[c]pyridin-7-yl(hydroxy)methylene]bis(phosphonic acid) (NE-10501): Synthetic, structural, and modeling studies.
Bioorg Med Chem Lett 18: 2878-82 (2008)
University Of Southern California
Reactive derivatives for affinity labeling in the ifenprodil site of NMDA receptors.
Bioorg Med Chem Lett 18: 2765-70 (2008)
University Of Strasburg
Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.
Bioorg Med Chem Lett 18: 2850-3 (2008)
Wyeth Research
Discovery of a novel submicromolar inhibitor of the lymphoid specific tyrosine phosphatase.
Bioorg Med Chem Lett 18: 2840-4 (2008)
Columbia University
Dual binding site inhibitors of B-RAF kinase.
Bioorg Med Chem Lett 18: 2825-9 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases.
Bioorg Med Chem Lett 18: 2793-8 (2008)
Methylgene
Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Bioorg Med Chem Lett 18: 2799-804 (2008)
Merck
Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.
Bioorg Med Chem Lett 18: 2776-80 (2008)
Astrazeneca
4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.
J Med Chem 51: 2944-53 (2008)
Vu University Amsterdam
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
J Med Chem 51: 2887-90 (2008)
Glaxosmithkline
Sulfamoyl benzamides as novel CB2 cannabinoid receptor ligands.
Bioorg Med Chem Lett 18: 2830-5 (2008)
Adolor
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
Bioorg Med Chem Lett 18: 2809-12 (2008)
The Broad Institute Of Harvard And Mit
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
Antimicrob Agents Chemother 52: 2909-14 (2008)
Universit£
Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.
J Med Chem 51: 2879-82 (2008)
Amgen
Combination of non-natural D-amino acid derivatives and allophenylnorstatine-dimethylthioproline scaffold in HIV protease inhibitors have high efficacy in mutant HIV.
J Med Chem 51: 2992-3004 (2008)
Kyoto Pharmaceutical University
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
Bioorg Med Chem Lett 18: 2813-9 (2008)
National Institute Of Diabetes And Digestive And Kidney Diseases
New tetrazole-based selective anandamide uptake inhibitors.
Bioorg Med Chem Lett 18: 2820-4 (2008)
Sapienza University Of Rome
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.
Bioorg Med Chem Lett 18: 2845-9 (2008)
Bristol-Myers Squibb Research And Development
2-Aminomethyl piperidines as novel urotensin-II receptor antagonists.
Bioorg Med Chem Lett 18: 2860-4 (2008)
Glaxosmithkline
Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.
Bioorg Med Chem Lett 18: 2865-70 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Conformation-activity relationship on novel 4-pyridylmethylthio derivatives with antiangiogenic activity.
Bioorg Med Chem Lett 18: 2939-43 (2008)
Santen Pharmaceutical
Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
Bioorg Med Chem Lett 18: 2883-5 (2008)
University Of California
Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones.
Eur J Med Chem 44: 303-11 (2009)
Katholieke Universiteit Leuven
Non-peptide gonadotropin-releasing hormone receptor antagonists.
J Med Chem 51: 3331-48 (2008)
Neurocrine Biosciences
Benzofuran-based hybrid compounds for the inhibition of cholinesterase activity, beta amyloid aggregation, and abeta neurotoxicity.
J Med Chem 51: 2883-6 (2008)
University Of Bologna
2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Enzyme-Ligand Co-Crystal Structure and Demonstration of Pharmacodynamic Effects in C57Bl/6 Mice.
J Med Chem 51: 2933-43 (2008)
Biovitrum
Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.
Bioorg Med Chem 16: 5606-18 (2008)
Neurocrine Biosciences
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.
Bioorg Med Chem 16: 5653-64 (2008)
Rensselaer Polytechnic Institute
Identification of acridinyl hydrazides as potent aspartic protease inhibitors.
Bioorg Med Chem Lett 18: 3011-5 (2008)
University Of Karachi
Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity.
Bioorg Med Chem Lett 18: 2896-9 (2008)
Pfizer
A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series.
Bioorg Med Chem Lett 18: 2891-5 (2008)
Universit£
Aza-peptidyl Michael Acceptors. A New Class of Potent and Selective Inhibitors of Asparaginyl Endopeptidases (Legumains) from Evolutionarily Diverse Pathogens.
J Med Chem 51: 2816-32 (2008)
Georgia Institute Of Technology
Alkaloids from the Australian rainforest tree Ochrosia moorei.
J Nat Prod 71: 1063-5 (2008)
Griffith University
Corymbones A and B, phloroglucinols with thyrotropin releasing hormone receptor 2 binding affinity from the flowers of Corymbia peltata.
J Nat Prod 71: 881-3 (2008)
Griffith University
Structural Origin of Selectivity in Class II-Selective Histone Deacetylase Inhibitors.
J Med Chem 51: 2898-906 (2008)
University Of Notre Dame
Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold.
J Med Chem 51: 2863-7 (2008)
University Of Ljubljana
Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
J Med Chem 51: 2758-65 (2008)
Amgen
(3R,5S,E)-7-(4-(4-Fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1H-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic Acid (BMS-644950): A Rationally Designed Orally Efficacious 3-Hydroxy-3-methylglutaryl Coenzyme-A Reductase Inhibitor with Reduced Myotoxicity Potential.
J Med Chem 51: 2722-33 (2008)
Bristol-Myers Squibb
Design and microwave-assisted synthesis of novel macrocyclic peptides active at melanocortin receptors: discovery of potent and selective hMC5R receptor antagonists.
J Med Chem 51: 2701-7 (2008)
University Of Arizona
Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines.
Bioorg Med Chem Lett 18: 2924-9 (2008)
Vernalis (R&D)
Combining docking, molecular dynamics and the linear interaction energy method to predict binding modes and affinities for non-nucleoside inhibitors to HIV-1 reverse transcriptase.
J Med Chem 51: 2648-56 (2008)
Uppsala University
Ring size of somatostatin analogues (ODT-8) modulates receptor selectivity and binding affinity.
J Med Chem 51: 2668-75 (2008)
Salk Institute
Ring size in octreotide amide modulates differently agonist versus antagonist binding affinity and selectivity.
J Med Chem 51: 2676-81 (2008)
Salk Institute
Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
J Med Chem 51: 3005-19 (2008)
Wayne State University
Identification of Plasmodium falciparum spermidine synthase active site binders through structure-based virtual screening.
J Med Chem 51: 2777-86 (2008)
Inovacia
Predicting binding modes from free energy calculations.
J Med Chem 51: 2657-67 (2008)
Uppsala University
Structural and biochemical evidence for a boat-like transition state in beta-mannosidases.
Nat Chem Biol 4: 306-12 (2008)
The Medical School, Newcastle University
Identification of RIP1 kinase as a specific cellular target of necrostatins.
Nat Chem Biol 4: 313-21 (2008)
Tufts University
Spongian diterpenes with thyrotropin releasing hormone receptor 2 binding affinity from Spongia sp.
J Nat Prod 71: 884-6 (2008)
Griffith University
Dihydroxystyrene metabolites from an association of the sponges Poecillastra wondoensis and Jaspis sp.
J Nat Prod 71: 779-83 (2008)
Seoul National University
Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives.
Bioorg Med Chem Lett 18: 2920-3 (2008)
Vernalis (R&D)
Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives.
Bioorg Med Chem Lett 18: 2916-9 (2008)
Vernalis (R&D)
N-Acetylhexosaminidase inhibitory properties of C-1 homologated GlcNAc- and GalNAc-thiazolines.
Bioorg Med Chem Lett 18: 2944-7 (2008)
The State University Of New Jersey
Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation.
Eur J Med Chem 43: 2853-60 (2008)
University Of Namur
Design and synthesis of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates.
Bioorg Med Chem Lett 18: 2905-9 (2008)
Friedrich-Schiller-Universit£T Jena
Conformationally constrained analogues of N'-(4-tert-butylbenzyl)-N-(4-methylsulfonylaminobenzyl)thiourea as TRPV1 antagonists.
Eur J Med Chem 44: 322-31 (2008)
Seoul National University
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?
Eur J Med Chem 43: 2307-15 (2008)
Universit£T Des Saarlandes
Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties.
Bioorg Med Chem 16: 5795-802 (2008)
Kyoto Pharmaceutical University
Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.
Bioorg Med Chem Lett 18: 2967-71 (2008)
Ligand Pharmaceuticals
Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists.
Bioorg Med Chem Lett 18: 2930-4 (2008)
Pfizer
10H-Phenothiazines: a new class of enzyme inhibitors for inflammatory diseases.
Eur J Med Chem 44: 197-202 (2008)
Institute Of Chemical Technology
1,2,3-Triazol-carboxanilides and 1,2,3-triazol-(N-benzyl)-carboxamides as BK-potassium channel activators. XII.
Eur J Med Chem 43: 2618-26 (2008)
Universit£
A novel quantitative structure-activity relationship method to predict the affinities of MT3 melatonin binding site.
Eur J Med Chem 43: 2861-9 (2008)
Lanzhou University
Tailoring the structure of aminobisphosphonates to target plant P5C reductase.
J Agric Food Chem 56: 3193-9 (2008)
University Of Ferrara
Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group.
Bioorg Med Chem 16: 4839-53 (2008)
Georgia Institute Of Technology
Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells.
Bioorg Med Chem Lett 18: 2982-4 (2008)
Waseda University
Podophyllotoxin directly binds a hinge domain in E2 of HPV and inhibits an E2/E7 interaction in vitro.
Bioorg Med Chem 16: 5815-25 (2008)
Tokyo University Of Science
The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.
Bioorg Med Chem Lett 18: 2959-66 (2008)
Merck Research Laboratories
Design and synthesis of calpain inhibitory 6-pyridone 2-carboxamide derivatives.
Eur J Med Chem 44: 1331-4 (2009)
Kyung Hee University
Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors.
Eur J Med Chem 44: 1341-8 (2009)
University Of Bologna
Thioxophosphoranyl aryl- and heteroaryloxiranes as the representants of a new class of metallocarboxypeptidase inhibitors.
Bioorg Med Chem 16: 4823-8 (2008)
Universitat AutòNoma De Barcelona
1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin.
Bioorg Med Chem 16: 4829-38 (2008)
University Of Oslo
Molecular features crucial to the activity of pyrimidine benzamide-based thrombopoietin receptor agonists.
Bioorg Med Chem Lett 18: 3000-6 (2008)
Pfizer
Carboxymethylated pyridoindole antioxidants as aldose reductase inhibitors: Synthesis, activity, partitioning, and molecular modeling.
Bioorg Med Chem 16: 4908-20 (2008)
Slovak Academy Of Sciences
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.
Bioorg Med Chem Lett 18: 2985-9 (2008)
Bristol-Myers Squibb
Diphenidol-related diamines as novel muscarinic M4 receptor antagonists.
Bioorg Med Chem Lett 18: 2972-6 (2008)
University Of Bologna
Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.
Eur J Med Chem 43: 2404-11 (2008)
Ludwig-Maximilians-UniversitäT MüNchen
Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
Bioorg Med Chem 16: 4883-907 (2008)
Pfizer
Synthesis of glutamic acid analogs as potent inhibitors of leukotriene A4 hydrolase.
Bioorg Med Chem 16: 4963-83 (2008)
Berlex Biosciences
5-Sulfonyl-benzimidazoles as selective CB2 agonists.
Bioorg Med Chem Lett 18: 2574-9 (2008)
Johnson & Johnson Pharmaceutical Research & Development
4'-Methyl-4,5'-bithiazole-based correctors of defective delta F508-CFTR cellular processing.
Bioorg Med Chem Lett 18: 2610-4 (2008)
University Of California
Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis.
Bioorg Med Chem Lett 18: 2662-8 (2008)
Weill Medical College Of Cornell University
Synthesis and anti-HIV-1 integrase activities of 3-aroyl-2,3-dihydro-1,1-dioxo-1,4,2-benzodithiazines.
Eur J Med Chem 44: 190-6 (2009)
Medical University Of Gda?Sk
Synthesis of indoleamine 2,3-dioxygenase inhibitory analogues of the sponge alkaloid exiguamine a.
J Med Chem 51: 2634-7 (2008)
University Of British Columbia
Aplysamine 6, an alkaloidal inhibitor of Isoprenylcysteine carboxyl methyltransferase from the sponge Pseudoceratina sp.
J Nat Prod 71: 1066-7 (2008)
Griffith University
Synthesis and pharmacological evaluations of sildenafil analogues for treatment of erectile dysfunction.
J Med Chem 51: 2807-15 (2008)
State University Of Campinas
Natural products, small molecules, and genetics in tuberculosis drug development.
J Med Chem 51: 2606-12 (2008)
National Institute Of Diabetes And Digestive And Kidney Diseases
Natural products as leads to potential drugs: an old process or the new hope for drug discovery?
J Med Chem 51: 2589-99 (2008)
National Cancer Institute-Frederick
Design and Synthesis of 2- and 3-Substituted-3-phenylpropyl Analogs of 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: Role of Amino, Fluoro, Hydroxyl, Methoxyl, Methyl, Methylene, and Oxo Substituents on Affinity f
J Med Chem 51: 2795-806 (2008)
National Taiwan University
Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation.
Proc Natl Acad Sci U S A 105: 5337-42 (2008)
Merck Research Laboratories
Mechanism of inhibition of human immunodeficiency virus type 1 reverse transcriptase by a stavudine analogue, 4'-ethynyl stavudine triphosphate.
Antimicrob Agents Chemother 52: 2035-42 (2008)
Yale University
Design, synthesis and trypanocidal activity of lead compounds based on inhibitors of parasite glycolysis.
Bioorg Med Chem 16: 5050-61 (2008)
University Of Edinburgh
Structure-based discovery of a novel non-peptidic small molecular inhibitor of caspase-3.
Bioorg Med Chem 16: 4854-9 (2008)
Tokyo University Of Science
Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition.
Bioorg Med Chem Lett 18: 2562-6 (2008)
Pfizer
Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists.
J Med Chem 51: 2744-57 (2008)
Amgen
Beta-homo-amino acid scan of angiotensin IV.
J Med Chem 51: 2291-6 (2008)
Vrije Universiteit Brussel
Synthesis and biological evaluation of histone deacetylase inhibitors that are based on FR235222: a cyclic tetrapeptide scaffold.
Bioorg Med Chem Lett 18: 2549-54 (2008)
San Diego State University
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
Bioorg Med Chem Lett 18: 2530-5 (2008)
Sapienza University Of Rome
Herkinorin analogues with differential beta-arrestin-2 interactions.
J Med Chem 51: 2421-31 (2008)
The University Of Iowa
In vivo efficacy of beta-cyclodextrin derivatives against anthrax lethal toxin.
Antimicrob Agents Chemother 52: 2239-41 (2008)
National Institute Of Allergy And Infectious Diseases
Recent advances in selective alpha1-adrenoreceptor antagonists as antihypertensive agents.
Bioorg Med Chem 16: 4759-800 (2008)
Sinhgad College Of Pharmacy
Synthesis and characterization of 5,6,7,8-tetrahydroquinoline C5a receptor antagonists.
Bioorg Med Chem Lett 18: 2544-8 (2008)
Johnson & Johnson Prd
Design and campaign synthesis of pyridine-based histone deacetylase inhibitors.
Bioorg Med Chem Lett 18: 2525-9 (2008)
Astrazeneca
Design and campaign synthesis of piperidine- and thiazole-based histone deacetylase inhibitors.
Bioorg Med Chem Lett 18: 2580-4 (2008)
Astrazeneca
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.
Bioorg Med Chem Lett 18: 2684-90 (2008)
Glaxosmithkline
Tetrazole based amides as growth hormone secretagogues.
Bioorg Med Chem Lett 18: 2536-9 (2008)
Bristol-Myers Squibb Research And Development
New chemotypes for cathepsin K inhibitors.
Bioorg Med Chem Lett 18: 2599-603 (2008)
Novartis Institutes For Biomedical Research
Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct.
Bioorg Med Chem Lett 18: 2567-73 (2008)
Universita Degli Studi Di Firenze
Synthesis of 4'-modified noraristeromycins to clarify the effect of the 4'-hydroxyl groups for inhibitory activity against S-adenosyl-L-homocysteine hydrolase.
Bioorg Med Chem Lett 18: 2615-8 (2008)
Gifu University
Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 3. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists.
Bioorg Med Chem Lett 18: 2725-9 (2008)
F. Hoffmann-La Roche
Pyrano-[2,3b]-pyridines as potassium channel antagonists.
Bioorg Med Chem Lett 18: 2714-8 (2008)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds.
Bioorg Med Chem Lett 18: 2628-32 (2008)
Scripps Florida
2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: optimization via array synthesis.
Bioorg Med Chem Lett 18: 2640-4 (2008)
Bristol-Myers Squibb Pharmaceutical Research Institute
Isoxazolone based inhibitors of p38 MAP kinases.
J Med Chem 51: 2580-4 (2008)
Eberhard Karls University Of Tuebingen
Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3.
Bioorg Med Chem 16: 4954-62 (2008)
Université
PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold.
Bioorg Med Chem Lett 18: 2719-24 (2008)
Affymax
Design and synthesis of bisubstrate inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: overview and perspectives.
Eur J Med Chem 43: 2298-306 (2008)
Chuq-Pavillon Chul And Université
Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.
J Med Chem 51: 2571-4 (2008)
Vrije Universiteit Brussel
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
J Med Chem 51: 2350-3 (2008)
Irbm/Merck Research Laboratories
Identification of promiscuous small molecule activators in high-throughput enzyme activation screens.
J Med Chem 51: 2346-9 (2008)
University Of Illinois
Hymenoic acid, a novel specific inhibitor of human DNA polymerase lambda from a fungus of Hymenochaetaceae sp.
Bioorg Med Chem 16: 5115-22 (2008)
Kobe Gakuin University
Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study.
Bioorg Med Chem 17: 1101-8 (2009)
The Scripps Research Institute
Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.
Bioorg Med Chem Lett 18: 2739-44 (2008)
Bristol-Myers Squibb
Identification of novel cannabinoid CB1 receptor antagonists by using virtual screening with a pharmacophore model.
J Med Chem 51: 2439-46 (2008)
Cns Biological Research
Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor.
J Med Chem 51: 2400-11 (2008)
Okayama University Graduate School Of Medicine
Carbonic anhydrase-II inhibition. what are the true enzyme-inhibitory properties of the sulfamide cognate of topiramate?
J Med Chem 51: 2518-21 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Characterization of chemical libraries for luciferase inhibitory activity.
J Med Chem 51: 2372-86 (2008)
National Human Genome Research Institute
A molecular modeling study of the interaction of 2'-fluoro-substituted analogues of dUMP/FdUMP with thymidylate synthase.
Bioorg Med Chem Lett 18: 2701-8 (2008)
Polish Academy Of Sciences
Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.
Bioorg Med Chem Lett 18: 2691-5 (2008)
Abbott Laboratories
Development of 2-t butyl-N-methyl pyrimidones as potent inhibitors of HIV integrase.
Bioorg Med Chem Lett 18: 2709-13 (2008)
Irbm-Mrl Rome
Design, synthesis and preliminary evaluation of novel pyrrolidine derivatives as matrix metalloproteinase inhibitors.
Eur J Med Chem 43: 2130-9 (2008)
Shandong University
(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists.
J Med Chem 51: 2522-32 (2008)
Egis Pharmaceuticals
Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia.
Bioorg Med Chem Lett 18: 2619-23 (2008)
Korea Research Institute Of Bioscience And Biotechnology
Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold.
Bioorg Med Chem Lett 18: 2696-700 (2008)
Merck Frosst Canada
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
Bioorg Med Chem Lett 18: 2669-74 (2008)
Istituto Di Biostrutture E Bioimmagini-Cnr
Effect of novel N-aryl sulfonamide substituted 3-morpholino arecoline derivatives as muscarinic receptor 1 agonists in Alzheimer's dementia models.
Bioorg Med Chem 16: 5157-63 (2008)
University Of Mysore
N-pyridin-3-yl- and N-quinolin-3-yl-benzamides: modulators of human vanilloid receptor 1 (TRPV1).
Bioorg Med Chem Lett 18: 2730-4 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.
Bioorg Med Chem Lett 18: 2652-7 (2008)
Bristol-Myers Squibb Research And Development
High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate.
Bioorg Med Chem 17: 990-1005 (2009)
Florida Atlantic University
Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors.
Bioorg Med Chem Lett 18: 2311-5 (2008)
Abbott Laboratories
Discovery of novel PRL-3 inhibitors based on the structure-based virtual screening.
Bioorg Med Chem Lett 18: 2250-5 (2008)
Sejong University
Complex sesquiterpenoids with tyrosinase inhibitory activity from the leaves of Chloranthus tianmushanensis.
J Nat Prod 71: 877-80 (2008)
Zhejiang University
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
J Med Chem 51: 2457-67 (2008)
Vrije Universiteit Amsterdam
"Virtual fragment linking": an approach to identify potent binders from low affinity fragment hits.
J Med Chem 51: 2481-91 (2008)
Novartis Institutes For Biomedical Research
N-Alkylated galanthamine derivatives: Potent acetylcholinesterase inhibitors from Leucojum aestivum.
Bioorg Med Chem Lett 18: 2263-6 (2008)
Universitat De Barcelona
Deconstructing cytisine: The syntheses of (+/-)-cyfusine and (+/-)-cyclopropylcyfusine, fused ring analogs of cytisine.
Bioorg Med Chem Lett 18: 2316-9 (2008)
Pfizer
Structure-based dissection of the natural product cyclopentapeptide chitinase inhibitor argifin.
Chem Biol 15: 295-301 (2008)
University Of Dundee
Chemical and biological investigation of N-hydroxy-valdecoxib: An active metabolite of valdecoxib.
Bioorg Med Chem 16: 5322-30 (2008)
Gedeon Richter
Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates.
Bioorg Med Chem Lett 18: 2267-71 (2008)
Universita Degli Studi Di Firenze
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.
Bioorg Med Chem Lett 18: 2288-91 (2008)
Kyowa Hakko Kogyo
Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors.
Bioorg Med Chem Lett 18: 2292-5 (2008)
Keimyung University
Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents.
J Med Chem 51: 2575-9 (2008)
Universit£
Synthesis, in vitro pharmacology, and pharmacokinetic profiles of 2-[1-amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-1-fluorocyclopropanecarboxylic acid and its 6-heptyl ester, a potent mGluR2 antagonist.
Bioorg Med Chem 16: 4359-66 (2008)
Taisho Pharmaceutical
Structure-guided design of C2-symmetric HIV-1 protease inhibitors based on a pyrrolidine scaffold.
J Med Chem 51: 2078-87 (2008)
Philipps-Universit£T Marburg
Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors.
J Med Chem 51: 2447-56 (2008)
Wayne State University
epigenetic multiple ligands: mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (sirtuin) inhibitors.
J Med Chem 51: 2279-90 (2008)
Sapienza University Of Rome
New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin.
J Med Chem 51: 2009-17 (2008)
Universitat De Barcelona
Recent developments of carbonic anhydrase inhibitors as potential anticancer drugs.
J Med Chem 51: 3051-6 (2008)
University Of Namur
Biological activities of novel gyrase inhibitors of the aminocoumarin class.
Antimicrob Agents Chemother 52: 1982-90 (2008)
UniversitäT TüBingen
Pharmacophore identification of Raf-1 kinase inhibitors.
Bioorg Med Chem Lett 18: 2346-50 (2008)
China Pharmaceutical University
Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 18: 2362-7 (2008)
Takeda California
9-cyano-1-azapaullone (cazpaullone), a glycogen synthase kinase-3 (GSK-3) inhibitor activating pancreatic beta cell protection and replication.
J Med Chem 51: 2196-207 (2008)
Technische Universit£T Braunschweig
Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration.
J Med Chem 51: 2147-57 (2008)
The Institute Of Cancer Research
Constrained dansyl derivatives reveal bacterial specificity of highly conserved thymidylate synthases.
Chembiochem 9: 779-90 (2008)
Università
Peptidomimetic 2-cyanopyrrolidines as potent selective cathepsin L inhibitors.
J Enzyme Inhib Med Chem 23: 190-7 (2008)
The M. S. University Of Baroda
Design, synthesis and pharmacological evaluation of hybrid molecules out of quinazolinimines and lipoic acid lead to highly potent and selective butyrylcholinesterase inhibitors with antioxidant properties.
Bioorg Med Chem 16: 4252-61 (2008)
Friedrich-Schiller-UniversitäT Jena
Synthesis, SAR and in vitro evaluation of new cyclic Arg-Gly-Asp pseudopentapeptides containing a s-cis peptide bond as integrin alphavbeta3 and alphavbeta5 ligands.
Bioorg Med Chem 16: 4262-71 (2008)
Department Of Organic Chemistry Ugo Schiff University Of Firenze Via Della Lastruccia 13
Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.
Bioorg Med Chem 16: 4272-85 (2008)
University Of Tokyo
Formation of fluorine-18 labeled diaryl ureas--labeled VEGFR-2/PDGFR dual inhibitors as molecular imaging agents for angiogenesis.
Bioorg Med Chem 16: 4242-51 (2008)
Hadassah Hebrew University Hospital
Inhibitors of DNA polymerase beta: activity and mechanism.
Bioorg Med Chem 16: 4331-40 (2008)
University Of Virginia
Structure-based virtual screening against SARS-3CL(pro) to identify novel non-peptidic hits.
Bioorg Med Chem 16: 4138-49 (2008)
University Of Mississippi
Sugar Chips immobilized with synthetic sulfated disaccharides of heparin/heparan sulfate partial structure.
Bioorg Med Chem Lett 18: 2499-504 (2008)
Kagoshima University
TIE-2/VEGF-R2 SAR and in vitro activity of C3-acyl dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs.
Bioorg Med Chem Lett 18: 2368-72 (2008)
Cephalon
Synthesis of barbiturate-based methionine aminopeptidase-1 inhibitors.
Bioorg Med Chem Lett 18: 2373-6 (2008)
North Dakota State University
Beta-lactam congeners of orlistat as inhibitors of fatty acid synthase.
Bioorg Med Chem Lett 18: 2491-4 (2008)
Texas A&M University
Novel 5-azaindolocarbazoles as cytotoxic agents and Chk1 inhibitors.
Bioorg Med Chem 16: 5303-21 (2008)
Université
Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.
Bioorg Med Chem Lett 18: 2355-61 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Rational design, synthesis and biological evaluation of new 1,5-diarylpyrazole derivatives as CB1 receptor antagonists, structurally related to rimonabant.
Eur J Med Chem 43: 2627-38 (2008)
Università
Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines.
Eur J Med Chem 43: 2665-76 (2008)
Università
Diversity-oriented fluorescence library approach (DOFLA) to the discovery of chymotrypsin sensor.
J Comb Chem 10: 460-5 (2008)
New York University
Sesterterpenoids from the sponge Sarcotragus sp.
J Nat Prod 71: 551-7 (2008)
Seoul National University
Novel prostaglandin d synthase inhibitors generated by fragment-based drug design.
J Med Chem 51: 2178-86 (2008)
Astrazeneca
Lipoxygenase inhibiting and antioxidant iridoids from Buddleja crispa.
J Enzyme Inhib Med Chem 23: 140-3 (2008)
Chinese Academy Of Medical Sciences
Mild and efficient synthesis of new tetraketones as lipoxygenase inhibitors and antioxidants.
J Enzyme Inhib Med Chem 23: 62-9 (2008)
Pharmaceutical Research Centre
In vitro inhibition of cytosolic carbonic anhydrases I and II by some new dihydroxycoumarin compounds.
J Enzyme Inhib Med Chem 23: 32-6 (2008)
Balikesir University Science & Art Faculty
Synthesis and pharmacological characterization at glutamate receptors of the four enantiopure isomers of tricholomic acid.
J Med Chem 51: 2311-5 (2008)
Universit£
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
J Med Chem 51: 1981-90 (2008)
Pfizer
Sidechain-linked inhibitors of HIV-1 protease dimerization.
Bioorg Med Chem 17: 967-76 (2009)
Purdue University
Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies.
Bioorg Med Chem 16: 4304-12 (2008)
Kitasato University
Lead identification of 2-iminobenzimidazole antagonists of the chemokine receptor CXCR3.
Bioorg Med Chem Lett 18: 2414-9 (2008)
Abbott Bioresearch Center
Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists.
Bioorg Med Chem Lett 18: 2385-9 (2008)
Reen Cross
Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation.
Bioorg Med Chem Lett 18: 2399-403 (2008)
Scios
Benzodioxoles: novel cannabinoid-1 receptor inverse agonists for the treatment of obesity.
J Med Chem 51: 2115-27 (2008)
F. Hoffmann-La Roche
5-tert-butyl-N-pyrazol-4-yl-4,5,6,7-tetrahydrobenzo[d]isoxazole-3-carboxamide derivatives as novel potent inhibitors of Mycobacterium tuberculosis pantothenate synthetase: initiating a quest for new antitubercular drugs.
J Med Chem 51: 1999-2002 (2008)
University Of Illinois At Chicago
Expanding the repertoire of small molecule transcriptional activation domains.
Bioorg Med Chem 17: 1034-43 (2009)
University Of Michigan
Tetramic and tetronic acids: an update on new derivatives and biological aspects.
Bioorg Med Chem 16: 4203-21 (2008)
University Of Bayreuth
Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 2: SAR of the amine tether.
Bioorg Med Chem Lett 18: 2395-8 (2008)
Scios
Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 1: SAR of the aryl region.
Bioorg Med Chem Lett 18: 2390-4 (2008)
Scios
Pyrimidine-based inhibitors of CaMKIIdelta.
Bioorg Med Chem Lett 18: 2404-8 (2008)
Scios
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
J Med Chem 51: 2502-11 (2008)
University Of California San Francisco
Conformational analysis and receptor docking of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist.
J Med Chem 51: 2108-14 (2008)
Merck Research Laboratories
Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
J Med Chem 51: 2027-36 (2008)
Fudan University
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 18: 2409-13 (2008)
Merck
Selective cell adhesion inhibitors: Barbituric acid based alpha4beta7--MAdCAM inhibitors.
Bioorg Med Chem Lett 18: 2509-12 (2008)
Millennium Pharmaceuticals
The berkeleyamides, amides from the acid lake fungus Penicillum rubrum.
J Nat Prod 71: 856-60 (2008)
Montana Tech Of The University Of Montana
An updated steroid benchmark set and its application in the discovery of novel nanomolar ligands of sex hormone-binding globulin.
J Med Chem 51: 2047-56 (2008)
University Of British Columbia
Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues.
Bioorg Med Chem 16: 4341-6 (2008)
University Of Queensland
Sulfonamidolactam inhibitors of coagulation factor Xa.
Bioorg Med Chem Lett 18: 2428-33 (2008)
Bristol-Myers Squibb
Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
Eur J Med Chem 43: 2699-716 (2008)
Graduate School Of The Chinese Academy Of Sciences
Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.
Eur J Med Chem 43: 2428-35 (2008)
Graduate School Of The Chinese Academy Of Sciences
Novel inhibitors of 17beta-hydroxysteroid dehydrogenase type 1: templates for design.
Bioorg Med Chem 16: 4438-56 (2008)
University Of Bath
Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.
Bioorg Med Chem Lett 18: 1778-83 (2008)
Neurocrine Biosciences
Targeting gastrin-releasing peptide receptors of prostate cancer cells for photodynamic therapy with a phthalocyanine-bombesin conjugate.
Bioorg Med Chem Lett 18: 2424-7 (2008)
Universit£
Identification of novel series of human CCR1 antagonists.
Bioorg Med Chem Lett 18: 2215-21 (2008)
Tanabe Research Laboratories Usa
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.
J Med Chem 51: 2187-95 (2008)
University Of Oxford
1-(1-Arylethylidene)thiosemicarbazide derivatives: a new class of tyrosinase inhibitors.
Bioorg Med Chem 16: 1096-102 (2008)
Sun Yat-Sen University
The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.
Bioorg Med Chem Lett 18: 1772-7 (2008)
K£Mia
Synthesis of water soluble bis-triazenoquinazolines: an unusual predicted mode of binding to the epidermal growth factor receptor tyrosine kinase.
Chem Biol Drug Des 71: 374-9 (2008)
Mcgill University/Royal Victoria Hospital
Pharmacophore modeling, quantitative structure-activity relationship analysis, and in silico screening reveal potent glycogen synthase kinase-3beta inhibitory activities for cimetidine, hydroxychloroquine, and gemifloxacin.
J Med Chem 51: 2062-77 (2008)
University Of Jordan
Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.
J Med Chem 51: 2158-69 (2008)
Saarland University
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.
J Med Chem 51: 1649-67 (2008)
Amgen
Development of Potent and Selective Phosphinic Peptide Inhibitors of Angiotensin-Converting Enzyme 2.
J Med Chem 51: 2216-2226 (2008)
University Of Athens
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.
J Med Chem 51: 1668-80 (2008)
Amgen
1-(2-Carboxyindol-5-yloxy)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: synthesis, biological activity, metabolic stability, and solubility.
Bioorg Med Chem 16: 3489-500 (2008)
University Of M£Nster
ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds.
Bioorg Med Chem 17: 1079-87 (2009)
Institute Of Molecular Physiology
Synthesis of 1-/2-substituted-[1,2,3]triazolo[4,5-g]phthalazine-4,9-diones and evaluation of their cytotoxicity and topoisomerase II inhibition.
Bioorg Med Chem 16: 4545-50 (2008)
Ewha Womans University
Synthesis, checkpoint kinase 1 inhibitory properties and in vitro antiproliferative activities of new pyrrolocarbazoles.
Bioorg Med Chem 16: 4419-30 (2008)
Universit£
CoMFA analysis of dual/multiple PPAR activators.
Eur J Med Chem 43: 2784-91 (2008)
National Institute Of Pharmaceutical Education And Research
Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases.
J Med Chem 51: 2267-78 (2008)
Cv Therapeutics
Probing distal regions of the A2B adenosine receptor by quantitative structure-activity relationship modeling of known and novel agonists.
J Med Chem 51: 2088-99 (2008)
National Institute Of Diabetes And Digestive And Kidney Diseases
Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.
J Med Chem 51: 1681-94 (2008)
Amgen
X-ray snapshot of the mechanism of inactivation of human neutrophil elastase by 1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives.
J Med Chem 51: 2003-8 (2008)
Wichita State University
Discovery of a New Class of Potent, Selective, and Orally Bioavailable CRTH2 (DP2) Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases.
J Med Chem 51: 2227-2243 (2008)
Merck Serono
Design, synthesis, and biological evaluation of AT1 angiotensin II receptor antagonists based on the pyrazolo[3,4-b]pyridine and related heteroaromatic bicyclic systems.
J Med Chem 51: 2137-46 (2008)
Universit£
Arginine binding motifs: design and synthesis of galactose-derived arginine tweezers as galectin-3 inhibitors.
J Med Chem 51: 2297-301 (2008)
Lund University
Indoleamine 2,3-dioxygenase is the anticancer target for a novel series of potent naphthoquinone-based inhibitors.
J Med Chem 51: 1706-18 (2008)
Bryn Mawr College
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
J Med Chem 51: 1861-73 (2008)
Wyeth Research
Biochemical characterization of SHV-55, an extended-spectrum class A beta-lactamase from Klebsiella pneumoniae.
Antimicrob Agents Chemother 52: 1897-8 (2008)
TBA
The Lys234Arg substitution in the enzyme SHV-72 is a determinant for resistance to clavulanic acid inhibition.
Antimicrob Agents Chemother 52: 1806-11 (2008)
National Institute Of Health Dr. Ricardo Jorge Av. Padre Cruz
Inhibitors of strand transfer that prevent integration and inhibit human T-cell leukemia virus type 1 early replication.
Antimicrob Agents Chemother 52: 3532-41 (2008)
Universit£
Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.
Bioorg Med Chem 16: 3482-8 (2008)
Chemical Genomics Centre Of The Max Planck Society
Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation.
Bioorg Med Chem Lett 18: 2203-5 (2008)
Glaxosmithkline
Synthesis and biological activity of quinolinone and dihydroquinolinone p38 MAP kinase inhibitors.
Bioorg Med Chem Lett 18: 2222-6 (2008)
Merck Research Laboratories
Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-beta Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-beta Receptor Type I Inhibitor as Antitumor Agent.
J Med Chem 51: 2302-2306 (2008)
Eli Lilly
Docking-based 3D-QSAR study for 11beta-HSD1 inhibitors.
Bioorg Med Chem Lett 18: 2479-90 (2008)
Korea Research Institute Of Chemical Technology
Inhibitors of anthrax lethal factor based upon N-oleoyldopamine.
Bioorg Med Chem Lett 18: 2467-70 (2008)
Purdue University
Substrate optimization for monitoring cathepsin C activity in live cells.
Bioorg Med Chem 17: 1064-70 (2009)
Genomics Institute Of The Novartis Research Foundation
Synthesis and neuropharmacological characterization of 2-O-substituted apomorphines.
Bioorg Med Chem 16: 4563-8 (2008)
University Of Debrecen
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (2).
Bioorg Med Chem 16: 4699-714 (2008)
Takeda Pharmaceutical
Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles.
Bioorg Med Chem Lett 18: 2006-12 (2008)
Adolor
2,3-Disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazolines: a novel class of antitumor agents.
Eur J Med Chem 44: 448-52 (2008)
Zhejiang University
Synthesis and aldose reductase inhibitory activity of some new chromonyl-2,4-thiazolidinediones.
Eur J Med Chem 43: 2412-7 (2008)
Ankara University
Degradation-promoters of cellular inhibitor of apoptosis protein 1 based on bestatin and actinonin.
Bioorg Med Chem 16: 4685-98 (2008)
The University Of Tokyo
Catechin gallates are NADP+-competitive inhibitors of glucose-6-phosphate dehydrogenase and other enzymes that employ NADP+ as a coenzyme.
Bioorg Med Chem 16: 3580-6 (2008)
Amorepacific
Computational analysis of the binding affinities of the natural-product cyclopentapeptides argifin and argadin to chitinase B from Serratia marcescens.
Bioorg Med Chem 16: 3565-79 (2008)
Kitasato University
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1).
Bioorg Med Chem 16: 4715-32 (2008)
Takeda Pharmaceutical
A novel synthesis and pharmacological evaluation of a potential dopamine D1/D2 agonist: 1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol.
Bioorg Med Chem 16: 3438-44 (2008)
University Centre For Pharmacy
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
Bioorg Med Chem Lett 18: 1762-7 (2008)
Bristol-Myers Squibb
Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series.
Bioorg Med Chem Lett 18: 1869-73 (2008)
Deltagen Research Laboratories (Former Combichem)
[4-(Phenoxy)pyridin-3-yl]methylamines: a new class of selective noradrenaline reuptake inhibitors.
Bioorg Med Chem Lett 18: 1795-8 (2008)
Pfizer
Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Bioorg Med Chem Lett 18: 1799-803 (2008)
Astrazeneca
Synthesis and biological evaluation of diversely substituted indolin-2-ones.
Eur J Med Chem 43: 2316-22 (2008)
Université
Synthesis of a potent and selective (18)F-labeled delta-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging.
J Med Chem 51: 1817-23 (2008)
Stanford University School Of Medicine
Characterization of Type II Ligands in CYP2C9 and CYP3A4.
J Med Chem 51: 1755-1763 (2008)
Astrazeneca
Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.
J Med Chem 51: 1695-705 (2008)
Amgen
Opioids and efflux transporters. Part 2: P-glycoprotein substrate activity of 3- and 6-substituted morphine analogs.
J Med Chem 51: 2316-20 (2008)
University Of Maryland
Computer-aided discovery of anti-inflammatory thiazolidinones with dual cyclooxygenase/lipoxygenase inhibition.
J Med Chem 51: 1601-9 (2008)
Aristotle University
Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration.
J Med Chem 51: 1546-59 (2008)
Targegen
Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity.
J Med Chem 51: 1904-12 (2008)
Abbott Laboratories
Pivaloyloxymethyl-modified isoprenoid bisphosphonates display enhanced inhibition of cellular geranylgeranylation.
Bioorg Med Chem 16: 3652-60 (2008)
University Of Iowa
Novel azaphilones, kasanosins A and B, which are specific inhibitors of eukaryotic DNA polymerases beta and lambda from Talaromyces sp.
Bioorg Med Chem 16: 4594-9 (2008)
Tokyo University Of Science
Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor.
Bioorg Med Chem Lett 18: 1926-30 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases.
Bioorg Med Chem Lett 18: 1916-21 (2008)
Cephalon
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
Bioorg Med Chem Lett 18: 1814-9 (2008)
Irbm/Merck Research Laboratories
Discovery of selective aminothiazole aurora kinase inhibitors.
ACS Chem Biol 3: 180-92 (2008)
Novartis
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.
J Med Chem 51: 1831-41 (2008)
Centre National de la Recherche Scientifique/INSERM/ULP
2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 2. Reduction of hERG Activity, Observed Species Selectivity, and Structure-Activity Relationships.
J Med Chem 51: 1730-9 (2008)
Neuroscience
2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 1. Structure-Activity Relationships and Optimization of Heterocyclic Substituents.
J Med Chem 51: 1719-29 (2008)
Neuroscience
Discovery of a novel series of biphenyl benzoic acid derivatives as potent and selective human beta3-adrenergic receptor agonists with good oral bioavailability. Part I.
J Med Chem 51: 1925-44 (2008)
Astellas Pharma
Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides.
J Med Chem 51: 1945-53 (2008)
Griffith University
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
J Med Chem 51: 1800-10 (2008)
Friedrich-Alexander University
Synthesis and inhibitory activity of oligosaccharide thiazolines as a class of mechanism-based inhibitors for endo-beta-N-acetylglucosaminidases.
Bioorg Med Chem 16: 4670-5 (2008)
University Of Maryland
Design, synthesis, inhibitory activity, and SAR studies of hydrophobic p-aminosalicylic acid derivatives as neuraminidase inhibitors.
Bioorg Med Chem 16: 3839-47 (2008)
Shandong University
N-1H-benzimidazol-5-ylbenzenesulfonamide derivatives as potent hPXR agonists.
Bioorg Med Chem 16: 3537-49 (2008)
University Of Montpellier
Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena.
Bioorg Med Chem Lett 18: 1804-9 (2008)
Glaxosmithkline
Rhodanine derivatives as novel inhibitors of PDE4.
Bioorg Med Chem Lett 18: 2032-7 (2008)
University Of Paisley
Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1).
Bioorg Med Chem Lett 18: 1859-63 (2008)
Merck Research Laboratories
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
Bioorg Med Chem Lett 18: 1864-8 (2008)
Pharmacopeia
Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues.
J Med Chem 51: 1771-82 (2008)
Universit£
CoMFA and HQSAR studies on 6,7-dimethoxy-4-pyrrolidylquinazoline derivatives as phosphodiesterase10A inhibitors.
Bioorg Med Chem 16: 3675-86 (2008)
St. John'S University
4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.
Bioorg Med Chem Lett 18: 1830-4 (2008)
Amgen
Erigeroflavanone, a flavanone derivative from the flowers of Erigeron annuus with protein glycation and aldose reductase inhibitory activity.
J Nat Prod 71: 713-5 (2008)
Institute Of Oriental Medicine
Latrunculin A and its C-17-O-carbamates inhibit prostate tumor cell invasion and HIF-1 activation in breast tumor cells.
J Nat Prod 71: 396-402 (2008)
University Of Louisana
Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
J Med Chem 51: 1913-24 (2008)
Human Biomolecular Research Institute
The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands.
Bioorg Med Chem 16: 4661-9 (2008)
Purdue University
Benzothiazole based inhibitors of p38alpha MAP kinase.
Bioorg Med Chem Lett 18: 1874-9 (2008)
Bristol-Myers Squibb Research And Development
Synthesis of all stereoisomers of 3-hydroxypipecolic acid and 3-hydroxy-4,5-dehydropipecolic acid and their evaluation as glycosidase inhibitors.
Bioorg Med Chem Lett 18: 1810-3 (2008)
Tohoku Pharmaceutical University
Rapid assembly of diverse and potent allosteric Akt inhibitors.
Bioorg Med Chem Lett 18: 2211-4 (2008)
Merck Research Laboratories
Synthesis of 2-modified aristeromycins and their analogs as potent inhibitors against Plasmodium falciparum S-adenosyl-L-homocysteine hydrolase.
Bioorg Med Chem 16: 3809-15 (2008)
Gifu University
Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain.
Bioorg Med Chem Lett 18: 1825-9 (2008)
Bristol Myers Squibb
Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX.
Bioorg Med Chem Lett 18: 1898-903 (2008)
Universita Degli Studi Di Firenze
Design and structure-activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): tetramic, tetronic acids and dihydropyridin-2-ones.
Bioorg Med Chem Lett 18: 1840-4 (2008)
Novartis Institutes For Biomedical Research
Synthetic homoserine lactone-derived sulfonylureas as inhibitors of Vibrio fischeri quorum sensing regulator.
Bioorg Med Chem 16: 3550-6 (2008)
Insa Lyon
Synthesis and structure-activity relationship studies in peripheral benzodiazepine receptor ligands related to alpidem.
Bioorg Med Chem 16: 3428-37 (2008)
Universit£
Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.
Bioorg Med Chem Lett 18: 1904-9 (2008)
Astrazeneca
Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands.
Bioorg Med Chem Lett 18: 1931-8 (2008)
Neurocrine Biosciences
New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity.
Bioorg Med Chem Lett 18: 1893-7 (2008)
Sulfidris
Use of lantibiotic synthetases for the preparation of bioactive constrained peptides.
Bioorg Med Chem Lett 18: 3025-8 (2008)
University Of Illinois
Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors.
Bioorg Med Chem Lett 18: 2194-7 (2008)
Merck Research Laboratories
Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.
J Med Chem 51: 1824-30 (2008)
University Of Minnesota
Synthesis, Cannabinoid Receptor Affinity, and Molecular Modeling Studies of Substituted 1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides.
J Med Chem 51: 1560-76 (2008)
Sapienza University Of Rome
Synthesis and SAR studies of indole-based MK2 inhibitors.
Bioorg Med Chem Lett 18: 1994-9 (2008)
Boehringer Ingelheim Pharmaceuticals
Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
Bioorg Med Chem Lett 18: 1939-44 (2008)
Bristol-Myers Squibb Research And Development
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.
Bioorg Med Chem Lett 18: 1910-5 (2008)
Bristol-Myers Squibb Pharmaceutical Research And Development
Structure-activity relationships and pharmacokinetic parameters of quinoline acylsulfonamides as potent and selective antagonists of the EP(4) receptor.
Bioorg Med Chem Lett 18: 2048-54 (2008)
Merck Frosst Centre For Therapeutic Research
Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles.
Bioorg Med Chem Lett 18: 2062-6 (2008)
Merck Research Laboratories
Probing FtsZ and tubulin with C8-substituted GTP analogs reveals differences in their nucleotide binding sites.
Chem Biol 15: 189-99 (2008)
University Of Amsterdam
Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors.
J Med Chem 51: 1783-90 (2008)
Universidade De Lisboa
Docking study yields four novel inhibitors of the protooncogene Pim-1 kinase.
J Med Chem 51: 1972-5 (2008)
Vertex Pharmaceuticals
Nitro as a novel zinc-binding group in the inhibition of carboxypeptidase A.
Bioorg Med Chem 16: 3596-601 (2008)
Yanbian University
Discovery of potent cholecystokinin-2 receptor antagonists: elucidation of key pharmacophore elements by X-ray crystallographic and NMR conformational analysis.
Bioorg Med Chem 16: 3917-25 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Constrained NBMPR analogue synthesis, pharmacophore mapping and 3D-QSAR modeling of equilibrative nucleoside transporter 1 (ENT1) inhibitory activity.
Bioorg Med Chem 16: 3848-65 (2008)
University Of Tennessee Health Science Center
Synthesis and neuropharmacological evaluation of 2-aryl- and alkylapomorphines.
Bioorg Med Chem 16: 3773-9 (2008)
University Of Debrecen
Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.
Bioorg Med Chem Lett 18: 1945-51 (2008)
Bristol-Myers Squibb Research And Development
Design, synthesis, and thrombin-inhibitory activity of pyridin-2-ones as P2/P3 core motifs.
Bioorg Med Chem Lett 18: 1972-6 (2008)
Universit£
3-Amino-1,5-benzodiazepinones: potent, state-dependent sodium channel blockers with anti-epileptic activity.
Bioorg Med Chem Lett 18: 1963-6 (2008)
Merck Research Laboratories
Cathepsin B inhibitory activities of phthalates isolated from a marine Pseudomonas strain.
Bioorg Med Chem Lett 18: 2083-8 (2008)
Pukyong National University
Synthesis and biological evaluation of chalcones as inhibitors of the voltage-gated potassium channel Kv1.3.
Bioorg Med Chem Lett 18: 2055-61 (2008)
The Walter And Eliza Hall Institute Of Medical Research
Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors.
Bioorg Med Chem Lett 18: 2097-102 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH).
Bioorg Med Chem Lett 18: 2109-13 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Usimines A-C, bioactive usnic acid derivatives from the Antarctic lichen Stereocaulon alpinum.
J Nat Prod 71: 710-2 (2008)
Silla University
Kinase-likeness and kinase-privileged fragments: toward virtual polypharmacology.
J Med Chem 51: 1214-22 (2008)
Vertex Pharmaceuticals
Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215
J Med Chem 51: 1976-80 (2008)
Bristol-Myers Squibb Research And Development
2-Aryloxy-4-alkylaminopyridines: Discovery of Novel Corticotropin-Releasing Factor 1 Antagonists.
J Med Chem 51: 1385-92 (2008)
Pfizer
6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases.
Proc Natl Acad Sci U S A 105: 2773-8 (2008)
Gsk
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.
Proc Natl Acad Sci U S A 105: 3041-6 (2008)
Plexxikon
Rapid clinical induction of hepatic cytochrome P4502B6 activity by ritonavir.
Antimicrob Agents Chemother 52: 1663-9 (2008)
Washington University
Biphenyl versus phenylpyridazine derivatives: the role of the heterocycle in a series of acyl-CoA:cholesterol acyl transferase inhibitors.
J Med Chem 51: 1474-7 (2008)
Universita Di Milano
Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core.
Bioorg Med Chem 16: 3744-58 (2008)
Leiden University
Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents.
Bioorg Med Chem Lett 18: 1958-62 (2008)
Bristol-Myers Squibb
Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues.
Bioorg Med Chem Lett 18: 2067-72 (2008)
Bristol-Myers Squibb Pharmaceutical Research Institute
2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists.
Bioorg Med Chem Lett 18: 2103-8 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Quinolone 3-carboxylic acid pharmacophore: design of second generation HIV-1 integrase inhibitors.
J Med Chem 51: 1136-44 (2008)
University Of Southern California
Glycosidase profiling with immobilised glycosidase-inhibiting iminoalditols--a proof-of-concept study.
Bioorg Med Chem Lett 18: 1922-5 (2008)
Technische Universit£T Graz
Synthesis, molecular modeling studies and selective inhibitory activity against MAO of N1-propanoyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives.
Eur J Med Chem 43: 2262-7 (2008)
Sapienza University Of Rome
3D-QSAR CoMFA studies on bis-coumarine analogues as urease inhibitors: a strategic design in anti-urease agents.
Bioorg Med Chem 16: 3456-61 (2008)
University Of Karachi
Discovery of a novel class of 1,3-dioxane-2-carboxylic acid derivatives as subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.
Bioorg Med Chem Lett 18: 2128-32 (2008)
Nippon Shinyaku
Rational design of 4-amino-5,6-diaryl-furo[2,3-d]pyrimidines as potent glycogen synthase kinase-3 inhibitors.
Bioorg Med Chem Lett 18: 1967-71 (2008)
Glaxosmithkline
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
J Med Chem 51: 1637-48 (2008)
Amgen
Strongylophorines: natural product inhibitors of hypoxia-inducible factor-1 transcriptional pathway.
J Med Chem 51: 1402-5 (2008)
University Of Utah
Exploring inhibitor binding at the s' subsites of cathepsin L.
J Med Chem 51: 1361-8 (2008)
National Research Council Canada
Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.
J Med Chem 51: 1482-6 (2008)
The University Of Mississippi
N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents.
Bioorg Med Chem Lett 18: 2019-22 (2008)
Merck Research Laboratories
Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein.
Bioorg Med Chem Lett 18: 2023-7 (2008)
Merck Frosst Centre For Therapeutic Research
Adenosine analogues as inhibitors of P2Y12 receptor mediated platelet aggregation.
Bioorg Med Chem Lett 18: 2167-71 (2008)
Inspire Pharmaceuticals
PB183, a sigma receptor ligand, as a potential PET probe for the imaging of prostate adenocarcinoma.
Bioorg Med Chem Lett 18: 1990-3 (2008)
Universit£
Peptide backbone modifications on the C-terminal hexapeptide of neurotensin.
Bioorg Med Chem Lett 18: 2013-8 (2008)
Friedrich-Alexander University
The synthesis of 5-substituted ring E analogs of methyllycaconitine via the Suzuki-Miyaura cross-coupling reaction.
Bioorg Med Chem 16: 3816-24 (2008)
Ohio University
Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3-trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors.
Bioorg Med Chem 16: 3907-16 (2008)
Temple University School Of Medicine
Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARalpha.
Bioorg Med Chem 16: 3800-8 (2008)
Usda-Ars
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
Bioorg Med Chem Lett 18: 2089-92 (2008)
Abbott Laboratories
Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists.
Bioorg Med Chem Lett 18: 2093-6 (2008)
Abbott Bioresearch Center
Discovery and SAR of hydrazide antagonists of the pituitary adenylate cyclase-activating polypeptide (PACAP) receptor type 1 (PAC1-R).
Bioorg Med Chem Lett 18: 2162-6 (2008)
Abbott Laboratories
Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives.
Bioorg Med Chem Lett 18: 2114-21 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Butyrolactone I derivatives from Aspergillus terreus carrying an unusual sulfate moiety.
J Nat Prod 71: 689-92 (2008)
Leibniz-Institute For Natural Product Research And Infection Biology
Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.
J Med Chem 51: 1179-88 (2008)
University Of Zurich
Novel sulfonanilide analogs decrease aromatase activity in breast cancer cells: synthesis, biological evaluation, and ligand-based pharmacophore identification.
J Med Chem 51: 1126-35 (2008)
The Ohio State University
The 1,4-benzodiazepine-2,5-dione small molecule template results in melanocortin receptor agonists with nanomolar potencies.
J Med Chem 51: 1423-31 (2008)
University Of Florida
Monoaryl-substituted salicylaldoximes as ligands for estrogen receptor beta.
J Med Chem 51: 1344-51 (2008)
Universita Di Pisa
Derivatives of 4-Amino-6-hydroxy-2-mercaptopyrimidine as Novel, Potent, and Selective A3 Adenosine Receptor Antagonists.
J Med Chem 51: 1764-70 (2008)
Universita Di Napoli
N-[omega-[4-(2-methoxyphenyl)-1-piperazinyl]alkyl]-2-quinolinamines as high-affinity fluorescent 5-HT1A receptor ligands.
J Med Chem 51: 1492-5 (2008)
Universita Degli Studi Di Bari
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.
J Med Chem 51: 1319-23 (2008)
Wyeth Research
Structures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency.
J Med Chem 51: 1459-63 (2008)
University Of Copenhagen
Structure-activity studies on splitomicin derivatives as sirtuin inhibitors and computational prediction of binding mode.
J Med Chem 51: 1203-13 (2008)
Albert-Ludwigs-University Of Freiburg
DNA gyrase from the albicidin producer Xanthomonas albilineans has multiple-antibiotic-resistance and unusual enzymatic properties.
Antimicrob Agents Chemother 52: 1382-90 (2008)
The University Of Queensland
Design and synthesis of N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamides as aldose reductase inhibitors.
Bioorg Med Chem 16: 3926-32 (2008)
Aristotle University Of Thessaloniki
Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo.
Bioorg Med Chem Lett 18: 2000-5 (2008)
Novartis Institutes For Biomedical Research
Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors.
Bioorg Med Chem Lett 18: 2206-10 (2008)
Array Biopharma
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
J Med Chem 51: 1115-25 (2008)
Institut De Biologie Structurale
A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists.
J Med Chem 51: 1369-76 (2008)
University Of Arizona Tucson
Characterization of the interaction of phorbol esters with the C1 domain of MRCK (myotonic dystrophy kinase-related Cdc42 binding kinase) alpha/beta.
J Biol Chem 283: 10543-9 (2008)
National Cancer Institute-Bethesda
Synthesis, structure and antibacterial activity of novel 1-(5-substituted-3-substituted-4,5-dihydropyrazol-1-yl)ethanone oxime ester derivatives.
Bioorg Med Chem 16: 4075-82 (2008)
Anhui University Of Technology
Preparation and affinity profile of novel nicotinic ligands.
Bioorg Med Chem Lett 18: 2188-93 (2008)
Servier, Chemistry Research Division A
Identification of"toxicophoric" features for predicting drug-induced QT interval prolongation.
Eur J Med Chem 43: 2479-88 (2008)
Universit£
Synthesis of eudistomin D analogues and its effects on adenosine receptors.
Bioorg Med Chem 16: 3825-30 (2008)
Hokkaido University
Individual stereoisomers of phosphinic dipeptide inhibitor of leucine aminopeptidase.
Bioorg Med Chem Lett 18: 1550-4 (2008)
Wroc£?Aw University Of Technology
Novel methylene-linked heterocyclic EP1 receptor antagonists.
Bioorg Med Chem Lett 18: 1592-7 (2008)
Glaxosmithkline
Pyrogallol and its analogs can antagonize bacterial quorum sensing in Vibrio harveyi.
Bioorg Med Chem Lett 18: 1567-72 (2008)
Georgia State University
2,3,5-Substituted tetrahydrofurans: COX-2 inhibitory activities of 5-hydroxymethyl-/carboxyl-2,3-diaryl-tetrahydro-furan-3-ols.
Eur J Med Chem 43: 2792-9 (2008)
Guru Nanak Dev University
Novel non-peptidic and small-sized BACE1 inhibitors.
Bioorg Med Chem Lett 18: 1643-7 (2008)
Kyoto Pharmaceutical University
6-Acetyl-7,7-dimethyl-5,6,7,8-tetrahydropterin is an activator of nitric oxide synthases.
Bioorg Med Chem Lett 18: 1563-6 (2008)
University Of Strathclyde
Synthesis and SAR of 2-Aryloxy-4-alkoxy-pyridines as Potent Orally Active Corticotropin-Releasing Factor 1 Receptor Antagonists.
J Med Chem 51: 1377-84 (2008)
Pfizer
Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes.
J Med Chem 51: 1145-9 (2008)
Bristol-Myers Squibb
3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases.
J Med Chem 51: 1231-41 (2008)
Abbott Laboratories
Structure-activity relationships of C-17 cyano-substituted estratrienes as anticancer agents.
J Med Chem 51: 1295-308 (2008)
University Of Bath
The structure-based design, synthesis and biological evaluation of DNA-binding bisintercalating bisanthrapyrazole anticancer compounds.
Bioorg Med Chem 16: 3959-68 (2008)
University Of Manitoba
Effect of five-membered sugar mimics on mammalian glycogen-degrading enzymes and various glucosidases.
Bioorg Med Chem 16: 2734-40 (2008)
Hokuriku University
Structure-activity relationship of human GLO I inhibitory natural flavonoids and their growth inhibitory effects.
Bioorg Med Chem 16: 3969-75 (2008)
Tokyo University Of Science
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.
Bioorg Med Chem 16: 2741-52 (2008)
Leiden/Amsterdam Center For Drug Research
2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924.
Bioorg Med Chem Lett 18: 1702-7 (2008)
Bristol-Myers Squibb Pharmaceutical Research Institute
QSAR studies on CCR2 antagonists with chiral sensitive hologram descriptors.
Bioorg Med Chem Lett 18: 1323-30 (2008)
National Institute Of Pharmaceutical Education And Research (Niper)
Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents.
J Med Chem 51: 1415-22 (2008)
Universita Degli Studi Di Bari
Carbamoylphosphonate matrix metalloproteinase inhibitors 6: cis-2-aminocyclohexylcarbamoylphosphonic acid, a novel orally active antimetastatic matrix metalloproteinase-2 selective inhibitor--synthesis and pharmacodynamic and pharmacokinetic analysis.
J Med Chem 51: 1406-14 (2008)
The Hebrew University Of Jerusalem
Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines.
J Med Chem 51: 1252-9 (2008)
Universit£
Overcoming undesirable HERG potency of chemokine receptor antagonists using baseline lipophilicity relationships.
J Med Chem 51: 1162-78 (2008)
Astrazeneca
Modeling and synthesis of novel tight-binding inhibitors of cytochrome P450 2C9.
Bioorg Med Chem 16: 4064-74 (2008)
Washington State University
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.
Bioorg Med Chem Lett 18: 1612-6 (2008)
Ewha Womans University
Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity.
Bioorg Med Chem Lett 18: 1725-9 (2008)
Evotec (Uk)
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
Bioorg Med Chem Lett 18: 1617-22 (2008)
Spot-Ea3857
Synthesis and biological evaluation of novel 8-aminomethylated oroxylin A analogues as alpha-glucosidase inhibitors.
Bioorg Med Chem Lett 18: 1659-62 (2008)
Indian Institute Of Chemical Technology
QSAR study of neuraminidase inhibitors based on heuristic method and radial basis function network.
Eur J Med Chem 43: 569-76 (2008)
Lanzhou University
Kinetic, thermodynamic and X-ray structural insights into the interaction of melatonin and analogues with quinone reductase 2.
Biochem J 413: 81-91 (2008)
University Of Illinois At Chicago
Quinazolinones and pyrido[3,4-d]pyrimidin-4-ones as orally active and specific matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis.
J Med Chem 51: 835-41 (2008)
Pfizer
Azetidine based transition state analogue inhibitors of N-ribosyl hydrolases and phosphorylases.
J Med Chem 51: 948-56 (2008)
Industrial Research
Synthesis and dopamine receptor affinities of N-alkyl-11-hydroxy-2-methoxynoraporphines: N-alkyl substituents determine D1 versus D2 receptor selectivity.
J Med Chem 51: 983-7 (2008)
Mclean Hospital
Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an exocyclic hydroxyl group: interaction with dopamine, serotonin, and norepinephrine transporters.
Bioorg Med Chem 16: 2769-78 (2008)
Wayne State University
Synthesis, adenosine receptor binding and 3D-QSAR of 4-substituted 2-(2'-furyl)-1,2,4-triazolo[1,5-a]quinoxalines.
Bioorg Med Chem 16: 2103-13 (2008)
University Of Santiago De Compostela
Structure-activity relationships and CoMFA of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic properties.
Bioorg Med Chem 16: 2829-51 (2008)
Organon Laboratories
Synthesis and pharmacological evaluation of bicyclic SNC80 analogues with separated benzhydryl moiety.
Bioorg Med Chem 16: 2870-85 (2008)
Westf£Lische Wilhelms-Universit£T
Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling.
Bioorg Med Chem 16: 2968-73 (2008)
Johnson & Johnson Pharmaceutical Research And Development
2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A(2A) antagonists with reduced hERG liability.
Bioorg Med Chem Lett 18: 1269-73 (2008)
Neurocrine Biosciences
BACE1 inhibitors: optimization by replacing the P1' residue with non-acidic moiety.
Bioorg Med Chem Lett 18: 1649-53 (2008)
Kyoto Pharmaceutical University
Development of pyridopyrimidines as potent Akt1/2 inhibitors.
Bioorg Med Chem Lett 18: 1274-9 (2008)
Merck Research Laboratories
Structure-activity relationships for the inhibition of recombinant human cytochromes P450 by curcumin analogues.
Eur J Med Chem 43: 1621-31 (2008)
Vrije Universiteit
Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists.
Bioorg Med Chem 16: 2156-70 (2008)
Merck Research Laboratories
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems.
Bioorg Med Chem Lett 18: 901-7 (2008)
Glaxosmithkline
Entry into a new class of protein kinase inhibitors by pseudo ring design.
Bioorg Med Chem Lett 18: 897-900 (2008)
Novartis Institutes For Biomedical Research
Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.
Bioorg Med Chem Lett 18: 1027-30 (2008)
Novartis Institute For Biomedical Research
Histone deacetylase inhibitors: from bench to clinic.
J Med Chem 51: 1505-29 (2008)
Menarini Ricerche
Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.
J Med Chem 51: 937-47 (2008)
The Scripps Research Institute
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors: Part I--discovery of two binding modes.
J Med Chem 51: 725-36 (2008)
Schering-Plough Research Institute
Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.
J Med Chem 51: 1068-72 (2008)
Cephalon
A binary QSAR model for classification of hERG potassium channel blockers.
Bioorg Med Chem 16: 4107-19 (2008)
University Of Vienna
11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists.
Bioorg Med Chem 16: 2753-63 (2008)
Nv Organon
Design, synthesis and biological evaluation of piperazine analogues as CB1 cannabinoid receptor ligands.
Bioorg Med Chem 16: 4035-51 (2008)
Central Research Institute
Inhaled adenosine A(2A) receptor agonists for the treatment of chronic obstructive pulmonary disease.
Bioorg Med Chem Lett 18: 1284-7 (2008)
Pfizer
Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold.
Bioorg Med Chem Lett 18: 1623-7 (2008)
National Health Research Institutes
Identification of a potent new chemotype for the selective inhibition of PDE4.
Bioorg Med Chem Lett 18: 1297-303 (2008)
Nih
Thiol-based angiotensin-converting enzyme 2 inhibitors: P1' modifications for the exploration of the S1' subsite.
Bioorg Med Chem Lett 18: 1681-7 (2008)
Glaxosmithkline
Imidazopyridines: a novel class of hNav1.7 channel blockers.
Bioorg Med Chem Lett 18: 1696-701 (2008)
Merck Research Laboratories
Potent, selective MCH-1 receptor antagonists.
Bioorg Med Chem Lett 18: 1402-6 (2008)
Hoffmann-La Roche
Rare dipeptide and urea derivatives from roots of Moringa oleifera as potential anti-inflammatory and antinociceptive agents.
Eur J Med Chem 44: 432-6 (2008)
Central Drug Research Institute
Synthesis and biological evaluation of pyrazoline analogues with beta-amino acyl group as dipeptidyl peptidase IV inhibitors.
Eur J Med Chem 43: 1889-902 (2008)
Korea Research Institute Of Chemical Technology
The total synthesis of fukiic acid, an HIV-1 integrase inhibitor.
Eur J Med Chem 43: 2268-71 (2008)
Universit£
Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem 16: 4093-106 (2008)
Taisho Pharmaceutical
Synthesis of potent pyrrolidine influenza neuraminidase inhibitors.
Bioorg Med Chem Lett 18: 1692-5 (2008)
Abbott Laboratories
Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.
Bioorg Med Chem Lett 18: 1642-8 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s.
Bioorg Med Chem Lett 18: 1603-6 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3.
Bioorg Med Chem Lett 18: 1573-6 (2008)
Abbott Bioresearch Center
In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.
Bioorg Med Chem Lett 18: 1674-80 (2008)
Sepracor
Constraining the amide bond in N-sulfonylated dipeptide VLA-4 antagonists.
Bioorg Med Chem Lett 18: 1688-91 (2008)
Merck Research Laboratories
Synthesis and structure-activity relationships of heteroaryl substituted-3,4-diamino-3-cyclobut-3-ene-1,2-dione CXCR2/CXCR1 receptor antagonists.
Bioorg Med Chem Lett 18: 1318-22 (2008)
Schering-Plough Research Institute
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.
Bioorg Med Chem Lett 18: 1577-82 (2008)
Bristol-Myers Squibb
Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 1: exploration of 7'-substitution of benzothiadiazine.
Bioorg Med Chem Lett 18: 1413-8 (2008)
Anadys Pharmaceuticals
Discovery of novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling.
Bioorg Med Chem Lett 18: 1340-5 (2008)
Shanghai Institute Of Materia Medica
Evaluation of a series of bicyclic CXCR2 antagonists.
Bioorg Med Chem Lett 18: 798-803 (2008)
Astrazeneca R&D Charnwood
A new class of bradykinin B1 receptor antagonists with high oral bioavailability and minimal PXR activity.
Bioorg Med Chem Lett 18: 682-7 (2008)
Merck Research Laboratories
A highly efficient route to enantiomerically pure l-N-Bz-Pmp(t-Bu)2-OH and incorporation into a peptide-based protein tyrosine phosphatase inhibitor.
Bioorg Med Chem Lett 18: 679-81 (2008)
University Of Southern California
1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity.
Bioorg Med Chem Lett 18: 596-9 (2008)
Pfizer
Acylpyrogallols as inhibitors of antiapoptotic Bcl-2 proteins.
J Med Chem 51: 717-20 (2008)
TBA
Synthesis and screening of a cyclic peptide library: discovery of small-molecule ligands against human prolactin receptor.
Bioorg Med Chem 17: 1026-33 (2009)
The Ohio State University
Alpha,Beta-cyclic-beta-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorg Med Chem Lett 18: 1288-92 (2008)
Bristol-Myers Squibb
Lipophilic modifications to dinucleoside polyphosphates and nucleotides that confer antagonist properties at the platelet P2Y12 receptor.
J Med Chem 51: 1007-25 (2008)
Inspire Pharmaceuticals
Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.
J Med Chem 51: 988-96 (2008)
University Of Messina
Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates.
J Med Chem 51: 713-6 (2008)
TBA
Pyrrolo[2,3-a]carbazoles as potential cyclin dependent kinase 1 (CDK1) Inhibitors. Synthesis, biological evaluation, and binding mode through docking simulations.
J Med Chem 51: 1048-52 (2008)
University Of Patras
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.
J Med Chem 51: 1058-62 (2008)
Istituto Superiore Di Sanita
Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists.
J Med Chem 51: 721-4 (2008)
TBA
Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.
J Med Chem 51: 737-51 (2008)
University Of Oxford
Novel inhibitors of the Gardos channel for the treatment of sickle cell disease.
J Med Chem 51: 976-82 (2008)
Icagen
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.
Proc Natl Acad Sci U S A 105: 2070-5 (2008)
Harvard Medical School
Exploring the potential of 3'-O-carboxy esters of thymidine as inhibitors of ribonuclease A and angiogenin.
Bioorg Med Chem 16: 2819-28 (2008)
Institute Of Technology
1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor.
Bioorg Med Chem 16: 2852-69 (2008)
Universit£
Synthesis and SAR of pyridazinone-substituted phenylalanine amide alpha4 integrin antagonists.
Bioorg Med Chem Lett 18: 1331-5 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Tyramine fragment binding to BACE-1.
Bioorg Med Chem Lett 18: 1304-7 (2008)
F. Hoffmann-La Roche
Design and synthesis of 1,3-diarylurea derivatives as selective cyclooxygenase (COX-2) inhibitors.
Bioorg Med Chem Lett 18: 1336-9 (2008)
Shaheed Beheshti University Of Medical Sciences
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.
Bioorg Med Chem Lett 18: 1312-7 (2008)
Corcept Therapeutics
Selective, high affinity A(2B) adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines.
Bioorg Med Chem Lett 18: 1397-401 (2008)
Cv Therapeutics
Probing the structural and topological requirements for CCR2 antagonism: holographic QSAR for indolopiperidine derivatives.
Bioorg Med Chem Lett 18: 1450-6 (2008)
National Institute Of Pharmaceutical Education And Research (Niper)
Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate.
Bioorg Med Chem 16: 4173-85 (2008)
Universit£
Disruption of Kv1.1 N-type inactivation by novel small molecule inhibitors (disinactivators).
Bioorg Med Chem 16: 3067-75 (2008)
Wyeth Research
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Bioorg Med Chem Lett 18: 923-8 (2008)
Merck Frosst Centre For Therapeutic Research
SAR study of 2,3,4,14b-tetrahydro-1H-dibenzo[b,f]pyrido[1,2-d][1,4]oxazepines as progesterone receptor agonists.
Bioorg Med Chem Lett 18: 1461-7 (2008)
Nv Organon
Small-molecule aggregates inhibit amyloid polymerization.
Nat Chem Biol 4: 197-9 (2008)
University Of California San Francisco
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
Bioorg Med Chem Lett 18: 1530-3 (2008)
Purdue University
Lysianadioic acid, a carboxypeptidase B inhibitor from Lysiana subfalcata.
Bioorg Med Chem Lett 18: 1495-7 (2008)
Griffith University
Synthesis and structure-affinity relationships of novel spirocyclic sigma receptor ligands with furopyrazole structure.
Bioorg Med Chem 16: 2992-3001 (2008)
Westf£Lische Wilhelms-Universit£T M£Nster
Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1-f][1,2,4]triazine-based VEGFR-2 kinase inhibitors.
Bioorg Med Chem Lett 18: 1354-8 (2008)
Bristol-Myers Squibb Research And Development
Pyrazinoindolone inhibitors of MAPKAP-K2.
Bioorg Med Chem Lett 18: 938-41 (2008)
Boehringer Ingelheim Pharmaceuticals
Rhodanine derivatives as selective protease inhibitors against bacterial toxins.
Chem Biol Drug Des 71: 131-9 (2008)
Burnham Institute For Medical Research
N(G)-aminoguanidines from primary amines and the preparation of nitric oxide synthase inhibitors.
J Med Chem 51: 924-31 (2008)
University Of California
Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.
J Med Chem 51: 1026-34 (2008)
The Hebrew University Of Jerusalem
Vesicular monoamine transporter substrate/inhibitor activity of MPTP/MPP+ derivatives: a structure-activity study.
J Med Chem 51: 760-8 (2008)
Wichita State University
Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.
J Med Chem 51: 861-74 (2008)
Irbm-Mrl
Targeting a prokaryotic protein in a eukaryotic pathogen: identification of lead compounds against cryptosporidiosis.
Chem Biol 15: 70-7 (2008)
Brandeis University
Conformational studies of 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists leading to new spirocyclic antagonists.
Bioorg Med Chem Lett 18: 1374-7 (2008)
Merck Research Laboratories
Design, Synthesis, Evaluation, and Crystallographic-Based Structural Studies of HIV-1 Protease Inhibitors with Reduced Response to the V82A Mutation.
J Med Chem 51: 852-60 (2008)
Universidad De Santiago De Compostela
Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic.
J Med Chem 51: 1053-7 (2008)
Uppsala University
Genetic and biochemical characterization of OXA-63, a new class D beta-lactamase from Brachyspira pilosicoli BM4442.
Antimicrob Agents Chemother 52: 1264-8 (2008)
Institut Pasteur
Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent.
Antimicrob Agents Chemother 52: 1302-17 (2008)
Southern Research Institute
High confidence predictions of drug-drug interactions: predicting affinities for cytochrome P450 2C9 with multiple computational methods.
J Med Chem 51: 648-54 (2008)
Washington State University
Novel sst5-selective somatostatin dicarba-analogues: synthesis and conformation-affinity relationships.
J Med Chem 51: 512-20 (2008)
University Of Firenze
Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.
Bioorg Med Chem Lett 18: 1350-3 (2008)
Medical University Of Lodz
Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors.
Bioorg Med Chem Lett 18: 1407-12 (2008)
Merck Frosst Center For Therapeutic Research
Implications for selectivity of 3,4-diarylquinolinones as p38alphaMAP kinase inhibitors.
Bioorg Med Chem Lett 18: 1431-5 (2008)
Eberhard-Karls University
Proline bis-amides as potent dual orexin receptor antagonists.
Bioorg Med Chem Lett 18: 1425-30 (2008)
Merck Research Laboratories
Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.
Bioorg Med Chem Lett 18: 1346-9 (2008)
Neurocrine Bioscience
4-(Heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs as a novel class of histone deacetylase inhibitors.
Bioorg Med Chem Lett 18: 1502-6 (2008)
Methylgene
A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors.
Eur J Med Chem 43: 1603-11 (2008)
National Health Research Institutes
Synthesis and biological evaluation of novel 2,4-diaminoquinazoline derivatives as SMN2 promoter activators for the potential treatment of spinal muscular atrophy.
J Med Chem 51: 449-69 (2008)
Decode Chemistry
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines.
J Med Chem 51: 589-602 (2008)
Merck Research Laboratories
Cdc7 kinase inhibitors: pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships.
J Med Chem 51: 487-501 (2008)
Nerviano Medical Sciences
Rationalizing the activities of diverse cholecystokinin 2 receptor antagonists using molecular field points.
J Med Chem 51: 565-73 (2008)
James Black Foundation
Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies.
J Med Chem 51: 603-11 (2008)
Virginia Commonwealth University
Allosteric modulators of the alpha7 nicotinic acetylcholine receptor.
J Med Chem 51: 701-12 (2008)
Abbott Laboratories
Discovery of novel chemotypes to a G-protein-coupled receptor through ligand-steered homology modeling and structure-based virtual screening.
J Med Chem 51: 581-8 (2008)
Molsoft
Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90.
J Med Chem 51: 373-5 (2008)
Wyeth Research
A new family of H3 receptor antagonists based on the natural product Conessine.
Bioorg Med Chem Lett 18: 1490-4 (2008)
Arena Pharmaceuticals
Anti-HIV-1 entry optimization of novel imidazopiperidine-tropane CCR5 antagonists.
Bioorg Med Chem Lett 18: 1498-501 (2008)
K£Mia
Effect of beta-cyclodextrin charge type on the molecular recognition thermodynamics of reactions with (ferrocenylmethyl)dimethylaminium derivatives.
J Phys Chem B 112: 1445-50 (2008)
Nankai University
New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations.
J Med Chem 51: 689-93 (2008)
University Of Montpellier
Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening.
J Med Chem 51: 625-33 (2008)
National Institute Of Diabetes And Digestive And Kidney Diseases
Conformational cross-talk between alpha2A-adrenergic and mu-opioid receptors controls cell signaling.
Nat Chem Biol 4: 126-31 (2008)
Massachusetts General Hospital
Evaluation of ursolic acid isolated from Ilex paraguariensis and derivatives on aromatase inhibition.
Eur J Med Chem 43: 1865-77 (2008)
Universidade Federal Do Rio Grande Do Sul (Ufrgs)
Synthesis and in silico biological activity evaluation of new N-substituted pyrazolo-oxazin-2-one systems.
Bioorg Med Chem 16: 3059-66 (2008)
University Of Sciences And Technology Houari Boum£Di£Ne
Synthesis and structure-activity relationships of soluble 8-substituted 4-(2-chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of the Wee1 and Chk1 checkpoint kinases.
Bioorg Med Chem Lett 18: 929-33 (2008)
University Of Auckland
Structure-activity relationships of C6-uridine derivatives targeting plasmodia orotidine monophosphate decarboxylase.
J Med Chem 51: 439-48 (2008)
Toronto General Research Institute
Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.
J Med Chem 51: 400-6 (2008)
Neurocrine Biosciences
Total synthesis and evaluation of [18F]MHMZ.
Bioorg Med Chem Lett 18: 1515-9 (2008)
University Of Mainz
Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management.
J Med Chem 51: 392-5 (2008)
Abbott Laboratories
Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor.
J Med Chem 51: 380-3 (2008)
Abbott Laboratories
A quantitative analysis of kinase inhibitor selectivity.
Nat Biotechnol 26: 127-32 (2008)
Ambit Biosciences
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.
Bioorg Med Chem 16: 3049-58 (2008)
Universit£
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Bioorg Med Chem Lett 18: 973-8 (2008)
Merck Research Laboratories
Non-charged thiamine analogs as inhibitors of enzyme transketolase.
Bioorg Med Chem Lett 18: 509-12 (2008)
Array Biopharma
Novel 3-alkoxy-1H-pyrazolo[3,4-d]pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitors.
Bioorg Med Chem Lett 18: 959-62 (2008)
Astrazeneca
Multi-target-directed ligands to combat neurodegenerative diseases.
J Med Chem 51: 347-72 (2008)
University Of Bologna
Synthesis and biological activity of human neuropeptide S analogues modified in position 2.
J Med Chem 51: 655-8 (2008)
University Of Ferrara
Structural diversity and plasticity associated with nucleotides targeting orotidine monophosphate decarboxylase.
J Med Chem 51: 432-8 (2008)
Toronto General Research Institute
Potent memapsin 2 (beta-secretase) inhibitors: design, synthesis, protein-ligand X-ray structure, and in vivo evaluation.
Bioorg Med Chem Lett 18: 1031-6 (2008)
Purdue University
The design, synthesis and structure-activity relationships of 1-aryl-4-aminoalkylisoquinolines: a novel series of CRF-1 receptor antagonists.
Bioorg Med Chem Lett 18: 891-6 (2008)
Neurogen
Indole-2-amide based biochemical antagonist of Dishevelled PDZ domain interaction down-regulates Dishevelled-driven Tcf transcriptional activity.
Bioorg Med Chem Lett 18: 946-9 (2008)
St. Jude Children'S Research Hospital
Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domains.
Bioorg Med Chem Lett 18: 942-5 (2008)
St. Jude Children'S Research Hospital
SAR of carbon-linked, 2-substituted purines: synthesis and characterization of AP23451 as a novel bone-targeted inhibitor of Src tyrosine kinase with in vivo anti-resorptive activity.
Chem Biol Drug Des 71: 97-105 (2008)
Ariad Pharmaceuticals
Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization.
Bioorg Med Chem Lett 18: 2183-7 (2008)
Universit£
1-deoxyrubralactone, a novel specific inhibitor of families X and Y of eukaryotic DNA polymerases from a fungal strain derived from sea algae.
Bioorg Med Chem 16: 2939-44 (2008)
Tokyo University Of Science
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
Bioorg Med Chem 16: 3032-8 (2008)
University Of Ferrara
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systems.
Bioorg Med Chem Lett 18: 908-12 (2008)
Glaxosmithkline
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.
Bioorg Med Chem Lett 18: 885-90 (2008)
Vanderbilt Institute Of Chemical Biology
Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents.
Bioorg Med Chem Lett 18: 1037-41 (2008)
Amgen
Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase.
Bioorg Med Chem Lett 18: 464-8 (2008)
Bristol-Myers Squibb
Structural similarities between thiamin-binding protein and thiaminase-I suggest a common ancestor.
Biochemistry 47: 1346-57 (2008)
Cornell University
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.
J Med Chem 51: 407-16 (2008)
Abbott Laboratories
Positive and negative modulation of group I metabotropic glutamate receptors.
J Med Chem 51: 634-47 (2008)
Institute Of Organic Synthesis
Inhibition of adenosine deaminase by analogues of adenosine and inosine, incorporating a common heterocyclic base, 4(7)-amino-6(5)H-imidazo[4,5-d]pyridazin-7(4)one.
J Med Chem 51: 694-8 (2008)
University Of Maryland Baltimore County
Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB.
J Med Chem 51: 545-52 (2008)
University Of California San Francisco
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
Bioorg Med Chem Lett 18: 1022-6 (2008)
Gsk
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).
Bioorg Med Chem Lett 18: 1011-6 (2008)
Glaxosmithkline
Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.
Bioorg Med Chem 16: 3218-23 (2008)
Harvard Medical School
BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.
Bioorg Med Chem Lett 18: 1017-21 (2008)
Glaxosmithkline
Hybrid angiogenesis inhibitors: synthesis and biological evaluation of bifunctional compounds based on 1-deoxynojirimycin and aryl-1,2,3-triazoles.
Bioorg Med Chem Lett 18: 954-8 (2008)
University College Dublin
Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors.
Bioorg Med Chem 16: 3245-54 (2008)
Monash University
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.
Bioorg Med Chem Lett 18: 983-8 (2008)
Clinic Of Nuclear Medicine
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.
Bioorg Med Chem 16: 3125-40 (2008)
Takeda Pharmaceutical
Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists.
Bioorg Med Chem Lett 18: 994-8 (2008)
Merck Research Laboratories
Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor.
Bioorg Med Chem Lett 18: 1120-3 (2008)
Gilead Sciences
Alkaloids from stems and leaves of Stemona japonica and their insecticidal activities.
J Nat Prod 71: 112-6 (2008)
Chinese Academy Of Sciences
Pim2 inhibitors from the Papua New Guinean plant Cupaniopsis macropetala.
J Nat Prod 71: 451-2 (2008)
Griffith University
Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator.
J Med Chem 51: 183-6 (2008)
Astex Therapeutics
SAR-oriented discovery of peroxisome proliferator-activated receptor pan agonist with a 4-adamantylphenyl group as a hydrophobic tail.
Bioorg Med Chem Lett 18: 1110-5 (2008)
University Of Tokyo
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.
Bioorg Med Chem Lett 18: 1063-6 (2008)
Wyeth Research
Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst 1 receptor.
Bioorg Med Chem Lett 18: 979-82 (2008)
Novartis Institutes For Biomedical Research
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
Antimicrob Agents Chemother 52: 901-8 (2008)
Glaxosmithkline
1-Aminoindanes as novel motif with potential atypical antipsychotic properties.
Bioorg Med Chem Lett 18: 489-93 (2008)
Pfizer
Synthetic study of VLA-4/VCAM-1 inhibitors: synthesis and structure-activity relationship of piperazinylphenylalanine derivatives.
Bioorg Med Chem Lett 18: 1053-7 (2008)
Kyowa Hakko Kogyo
Design and synthesis of 4-[(s-triazin-2-ylamino)methyl]-N-(2-aminophenyl)-benzamides and their analogues as a novel class of histone deacetylase inhibitors.
Bioorg Med Chem Lett 18: 1067-71 (2008)
Methylgene
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part II: Acyclic replacements for the (3S)-3-benzylpiperidine in a series of potent CCR3 antagonists.
Bioorg Med Chem Lett 18: 586-95 (2008)
Bristol-Myers Squibb
Targeting ACE and ECE with dual acting inhibitors.
Bioorg Med Chem Lett 18: 1058-62 (2008)
Universit£
Discovery of novel orally active ureido NPY Y5 receptor antagonists.
Bioorg Med Chem Lett 18: 1146-50 (2008)
Schering-Plough Research Institute
Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.
Bioorg Med Chem Lett 18: 474-8 (2008)
Bristol-Myers Squibb R & D
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
J Med Chem 51: 282-97 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Novel 2-(4-methylsulfonylphenyl)pyrimidine derivatives as highly potent and specific COX-2 inhibitors.
Bioorg Med Chem 16: 2183-99 (2008)
Faes Farma
High-content single-cell drug screening with phosphospecific flow cytometry.
Nat Chem Biol 4: 132-42 (2008)
Stanford University
Synthesis of benzamide derivatives as TRPV1 antagonists.
Bioorg Med Chem Lett 18: 1072-8 (2008)
Pfizer
Hepatoselectivity of statins: design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors.
Bioorg Med Chem Lett 18: 1151-6 (2008)
Pfizer
Synthesis and structure-activity relationships of thiadiazole-derivatives as potent and orally active peroxisome proliferator-activated receptors alpha/delta dual agonists.
Bioorg Med Chem 16: 3321-41 (2008)
Johnson & Johnson Pharmaceutical Research And Development
3D-QSAR models on clinically relevant K103N mutant HIV-1 reverse transcriptase obtained from two strategic considerations.
Bioorg Med Chem Lett 18: 1181-94 (2008)
Korea Institute Of Science And Technology
An oxazole-based small-molecule Stat3 inhibitor modulates Stat3 stability and processing and induces antitumor cell effects.
ACS Chem Biol 2: 787-98 (2007)
University Of Central Florida College Of Medicine
URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices.
Chem Biol 14: 1357-65 (2007)
University Of California Irvine
Diazen-1-ium-1,2-diolated and nitrooxyethyl nitric oxide donor ester prodrugs of anti-inflammatory (E)-2-(aryl)-3-(4-methanesulfonylphenyl)acrylic acids: synthesis, cyclooxygenase inhibition, and nitric oxide release studies.
Bioorg Med Chem 16: 3302-8 (2008)
University Of Alberta
Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase.
Bioorg Med Chem 16: 3283-90 (2008)
Universidad De Buenos Aires
Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: part 2. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists.
Bioorg Med Chem Lett 18: 1091-5 (2008)
F. Hoffmann-La Roche
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.
Bioorg Med Chem Lett 18: 576-85 (2008)
Bristol-Myers Squibb
Noreupenifeldin, a tropolone from an unidentified ascomycete.
J Nat Prod 71: 457-9 (2008)
Merck Research Laboratories
2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-one-based HIV-1 integrase inhibitors.
J Med Chem 51: 251-9 (2008)
National Cancer Institute-Frederick
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.
J Med Chem 51: 305-13 (2008)
Arena Pharmaceuticals
Biochemical and structural evaluation of highly selective 2-arylbenzoxazole-based transthyretin amyloidogenesis inhibitors.
J Med Chem 51: 260-70 (2008)
The Scripps Research Institute
Comparison of the structural properties of the active site cavities of human and rat monoamine oxidase A and B in their soluble and membrane-bound forms.
Biochemistry 47: 526-36 (2008)
Emory University
New inhibitors of ABCG2 identified by high-throughput screening.
Mol Cancer Ther 6: 3271-8 (2007)
Saic-Frederick
NF-kappaB-inhibiting naphthopyrones from the Fijian echinoderm Comanthus parvicirrus.
J Nat Prod 71: 106-11 (2008)
University Of Aberdeen
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
J Med Chem 51: 187-95 (2008)
University Of Arizona
Structural basis for the high all-trans-retinaldehyde reductase activity of the tumor marker AKR1B10.
Proc Natl Acad Sci U S A 104: 20764-9 (2007)
Universitat Aut£Noma De Barcelona
Thiahomoisocitrate: a highly potent inhibitor of homoisocitrate dehydrogenase involved in the alpha-aminoadipate pathway.
Bioorg Med Chem 16: 3372-6 (2008)
Tokyo Institute Of Technology
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 1. Design, synthesis, and lead identification.
Bioorg Med Chem Lett 18: 1135-9 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Selective mapping of chemical space for Pseudomonas aeruginosa deacetylase LpxC inhibitory potential.
Chem Biol Drug Des 71: 45-56 (2008)
National Institute Of Pharmaceutical Education And Research
Synthesis and in vivo evaluation of halogenated N,N-dimethyl-2-(2'-amino-4'-hydroxymethylphenylthio)benzylamine derivatives as PET serotonin transporter ligands.
J Med Chem 51: 271-81 (2008)
Emory University
Novel quinazolinone derivatives as 5-HT7 receptor ligands.
Bioorg Med Chem 16: 2570-8 (2008)
Institute Of Science And Technology
Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists.
Bioorg Med Chem 16: 3309-20 (2008)
Astellas Pharma
Stereospecific synthesis and bio-activity of novel beta(3)-adrenoceptor agonists and inverse agonists.
Bioorg Med Chem 16: 2473-88 (2008)
Universit£
Prodrug thiamine analogs as inhibitors of the enzyme transketolase.
Bioorg Med Chem Lett 18: 505-8 (2008)
Array Biopharma
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).
Bioorg Med Chem Lett 18: 554-9 (2008)
Merck
Discovery of a novel class of selective human CB1 inverse agonists.
Bioorg Med Chem Lett 18: 1199-206 (2008)
Vernalis (R&D)
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents.
Bioorg Med Chem Lett 18: 1140-5 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Protected aminooxyprolines for expedited library synthesis: application to Tsg101-directed proline-oxime containing peptides.
Bioorg Med Chem Lett 18: 1096-101 (2008)
Nih
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
Bioorg Med Chem Lett 18: 469-73 (2008)
Purdue University
N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.
Bioorg Med Chem Lett 18: 1172-6 (2008)
Amgen
Synthetic ligands that activate and inhibit a quorum-sensing regulator in Pseudomonas aeruginosa.
Bioorg Med Chem Lett 18: 3072-5 (2008)
University Of Wisconsin-Madison
N(delta)-Methylated L-arginine derivatives and their effects on the nitric oxide generating system.
Bioorg Med Chem 16: 2305-12 (2008)
Christian-Albrechts-University Of Kiel
Omega-(2-Naphthyloxy) amino alkanes as a novel class of anti-hyperglycemic and lipid lowering agents.
Bioorg Med Chem 16: 2489-98 (2008)
Central Drug Research Institute
Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors.
Bioorg Med Chem 16: 2448-62 (2008)
University Of Bonn
Synthesis and biological evaluation of bengacarboline derivatives.
Bioorg Med Chem Lett 18: 1212-6 (2008)
Universit£
Syntheses of tetrahydrothiophenes and tetrahydrofurans and studies of their derivatives as melanocortin-4 receptor ligands.
Bioorg Med Chem Lett 18: 1124-30 (2008)
Neurocrine Biosciences
CODES, a novel procedure for ligand-based virtual screening: PDE7 inhibitors as an application example.
Eur J Med Chem 43: 1349-59 (2008)
Polymer Functionalization Group (Ictp, Csic)
Structure and function of PA4872 from Pseudomonas aeruginosa, a novel class of oxaloacetate decarboxylase from the PEP mutase/isocitrate lyase superfamily.
Biochemistry 47: 167-82 (2008)
University Of Maryland Biotechnology Institute
Bornyl (3,4,5-trihydroxy)-cinnamate--an optimized human neutrophil elastase inhibitor designed by free energy calculations.
Bioorg Med Chem 16: 2385-90 (2008)
Albert-Ludwigs-University Of Freiburg
Parallel synthesis of a series of potentially brain penetrant aminoalkyl benzoimidazoles.
Bioorg Med Chem 16: 2313-28 (2008)
Siena Biotech
Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids.
Bioorg Med Chem 16: 2558-69 (2008)
Birla Institute Of Technology And Science
Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents.
Bioorg Med Chem Lett 18: 1207-11 (2008)
Universit&Aagrov
Thiol-based angiotensin-converting enzyme 2 inhibitors: P1 modifications for the exploration of the S1 subsite.
Bioorg Med Chem Lett 18: 732-7 (2008)
Glaxosmithkline
Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor.
Bioorg Med Chem Lett 18: 571-5 (2008)
Institute Of Science And Technology
Synthesis and biological activity of novel peptide mimetics as melanocortin receptor agonists.
Bioorg Med Chem Lett 18: 1223-8 (2008)
Nanyang Technological University
Synthesis and evaluation of N-methyl and S-methyl 11C-labeled 6-methylthio-2-(4'-N,N-dimethylamino)phenylimidazo[1,2-a]pyridines as radioligands for imaging beta-amyloid plaques in Alzheimer's disease.
J Med Chem 51: 148-58 (2008)
National Institute Of Mental Health
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Proc Natl Acad Sci U S A 104: 19936-41 (2007)
Harvard Medical School
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Proc Natl Acad Sci U S A 104: 20523-8 (2007)
University Of Oxford
Hemopressin is an inverse agonist of CB1 cannabinoid receptors.
Proc Natl Acad Sci U S A 104: 20588-93 (2007)
Proteimax Biotechnology
Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.
Bioorg Med Chem 16: 2243-60 (2008)
Takeda Pharmaceutical
1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists.
Bioorg Med Chem 16: 2419-30 (2008)
Universit£
Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide.
Bioorg Med Chem Lett 18: 614-8 (2008)
Universit£
Conformationally constrained diketopimelic acid analogues as inhibitors of dihydrodipicolinate synthase.
Bioorg Med Chem Lett 18: 460-3 (2008)
University Of Melbourne
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Bioorg Med Chem Lett 18: 355-9 (2008)
Abbott Laboratories
Reaching for high-hanging fruit in drug discovery at protein-protein interfaces.
Nature 450: 1001-1009 (2007)
University Of California San Francisco
Further structure-activity relationships study of hybrid 7-{[2-(4-phenylpiperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol analogues: identification of a high-affinity D3-preferring agonist with potent in vivo activity with long duration of action.
J Med Chem 51: 101-17 (2008)
Wayne State University
Design, synthesis, and biological evaluation of classical and nonclassical 2-amino-4-oxo-5-substituted-6-methylpyrrolo[3,2-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors.
J Med Chem 51: 68-76 (2008)
Duquesne University
New celecoxib derivatives as anti-inflammatory agents.
J Med Chem 51: 142-7 (2008)
Gedeon Richter
Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes.
J Med Chem 51: 46-56 (2008)
Kyoto University
Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic acid (PF-3052334) as a candidate for the treatment of hypercholesterolemia.
J Med Chem 51: 31-45 (2008)
Pfizer
Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-Benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues.
J Med Chem 51: 57-67 (2008)
Seoul National University
Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.
J Med Chem 51: 4-16 (2008)
Novartis Pharmaceuticals
Substituted benzylaminoalkylindoles with preference for the sigma2 binding site.
Eur J Med Chem 43: 2073-81 (2008)
University Of Trieste
New QSAR combined strategy for the design of A1 adenosine receptor agonists.
Bioorg Med Chem 16: 1658-75 (2008)
Central University Of Las Villas
Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist.
Bioorg Med Chem 16: 2635-44 (2008)
Kyushu University
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.
Bioorg Med Chem Lett 18: 767-71 (2008)
Wyeth Research
Design and synthesis of novel potent and selective integrin alphanubeta3 antagonists--novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates.
Bioorg Med Chem Lett 18: 527-31 (2008)
Basf
A set of phosphatase-inert"molecular rulers" to probe for bivalent mannose 6-phosphate ligand-receptor interactions.
Bioorg Med Chem Lett 18: 3085-9 (2008)
University Of Nebraska
Novel ofloxacin derivatives: synthesis, antimycobacterial and toxicological evaluation.
Bioorg Med Chem Lett 18: 1229-36 (2008)
Birla Institute Of Technology And Science
New insights into the first oxidative phenol coupling reaction during vancomycin biosynthesis.
Bioorg Med Chem Lett 18: 3081-4 (2008)
University Of Z£Rich
Inhibition of dipeptidyl peptidase-IV (DPP-IV) by atorvastatin.
Bioorg Med Chem Lett 18: 479-84 (2008)
St. John'S University
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.
Bioorg Med Chem Lett 18: 560-4 (2008)
Incyte
Design, synthesis, and biological evaluation of human sialidase inhibitors. Part 1: selective inhibitors of lysosomal sialidase (NEU1).
Bioorg Med Chem Lett 18: 532-7 (2008)
Gifu University
Development of CXCR3 antagonists. Part 4: discovery of 2-amino-(4-tropinyl)quinolines.
Bioorg Med Chem Lett 18: 629-33 (2008)
Ucb Pharma
Novel bradykinin-1 antagonists containing a (1,2,3,4-tetrahydro-isoquinolin-1-yl)acetic acid scaffold.
Eur J Med Chem 43: 1552-8 (2008)
University Of Szeged
Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo.
J Med Chem 51: 17-30 (2008)
National Institute Of Mental Health
Conformational comparisons of a series of tachykinin peptide analogs.
J Med Chem 50: 6501-6 (2007)
Mississippi State University
Selective COX-2 inhibitors. Part 2: synthesis and biological evaluation of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamides.
Bioorg Med Chem 16: 2697-706 (2008)
Taipei Medical University
Conception of myeloperoxidase inhibitors derived from flufenamic acid by computational docking and structure modification.
Bioorg Med Chem 16: 1702-20 (2008)
Universit£
Substituted oxazolidinones as novel NPC1L1 ligands for the inhibition of cholesterol absorption.
Bioorg Med Chem Lett 18: 546-53 (2008)
Pfizer
Design and optimization of imidazole derivatives as potent CXCR3 antagonists.
Bioorg Med Chem Lett 18: 608-13 (2008)
Amgen
Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
J Med Chem 51: 173-7 (2008)
Biological Research Center Of The Hungarian Academy Of Sciences
Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure.
Bioorg Med Chem 16: 1992-2010 (2008)
Saarland University
Protein phosphatase inhibitory activity of tautomycin photoaffinity probes evaluated at femto-molar level.
Bioorg Med Chem 16: 1747-55 (2008)
Nagoya University
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
Bioorg Med Chem Lett 18: 688-93 (2008)
Amgen
Sulfonamide derivatives of bridgehead substituted bicyclo[4.2.1]nonanes as gamma-secretase inhibitors.
Bioorg Med Chem Lett 18: 375-9 (2008)
Merck Sharp And Dohme Research Laboratories
A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Bioorg Med Chem Lett 18: 674-8 (2008)
Astrazeneca
Alpha,beta-cyclic-beta-benzamido hydroxamic acids: novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-alpha converting enzyme (TACE).
Bioorg Med Chem Lett 18: 694-9 (2008)
Bristol-Myers Squibb Research And Development
1-Toluene-sulfonyl-3-[(3'-hydroxy-5'-substituted)-gamma-butyrolactone]-indoles: synthesis, COX-2 inhibition and anti-cancer activities.
Bioorg Med Chem Lett 18: 85-9 (2008)
Guru Nanak Dev University
Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.
Bioorg Med Chem Lett 18: 716-20 (2008)
Merck Research Laboratories
Design and synthesis of a siderophore conjugate as a potent PSMA inhibitor and potential diagnostic agent for prostate cancer.
Bioorg Med Chem 16: 1648-57 (2008)
University Of Notre Dame
Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.
Bioorg Med Chem Lett 18: 39-43 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists.
Bioorg Med Chem Lett 18: 710-5 (2008)
Glaxosmithkline
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
Bioorg Med Chem Lett 18: 726-31 (2008)
Merck Research Laboratories
Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor.
Bioorg Med Chem Lett 18: 210-4 (2008)
University Of Pennsylvania
Molecular basis of cyclin-CDK-CKI regulation by reversible binding of an inositol pyrophosphate.
Nat Chem Biol 4: 25-32 (2007)
Harvard University
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.
Nat Chem Biol 4: 42-50 (2007)
Dvanderbilt Program In Drug Discovery
Structure, inhibitor, and regulatory mechanism of Lyp, a lymphoid-specific tyrosine phosphatase implicated in autoimmune diseases.
Proc Natl Acad Sci U S A 104: 19767-72 (2007)
Indiana University School Of Medicine
Structure-based design and synthesis of novel macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds as potent inhibitors of protein kinase CK2 and their anticancer activities.
Bioorg Med Chem Lett 18: 619-23 (2008)
Polaris Pharmaceuticals
Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes.
Bioorg Med Chem Lett 18: 624-8 (2008)
University Of California
Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.
Bioorg Med Chem Lett 18: 634-9 (2008)
Bristol-Myers Squibb Research And Development
(Phenylpiperazinyl)cyclohexylureas: discovery of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
Bioorg Med Chem Lett 18: 640-4 (2008)
Johnson & Johnson Pharmaceutical Research And Development
Antitumor studies -- part 2: structure-activity relationship study for flavin analogs including investigations on their in vitro antitumor assay and docking simulation into protein tyrosine kinase.
Eur J Med Chem 43: 1376-89 (2008)
Okayama University
Iromycins from Streptomyces sp. and from synthesis: new inhibitors of the mitochondrial electron transport chain.
Bioorg Med Chem 16: 1738-46 (2008)
Georg-August-Universit£T G£Ttingen
Novel heterocycle-substituted pyrimidines as inhibitors of NF-kappaB transcription regulation related to TNF-alpha cytokine release.
Bioorg Med Chem Lett 18: 653-6 (2008)
Seoul National University
Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones.
Bioorg Med Chem Lett 18: 44-8 (2008)
Vertex Pharmaceuticals
Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs).
Bioorg Med Chem 16: 2011-33 (2008)
University Of Freiburg
(2S,2'R)-analogue of LG190178 is a major active isomer.
Bioorg Med Chem Lett 18: 120-3 (2008)
National Institute Of Health Sciences
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.
Bioorg Med Chem Lett 18: 49-53 (2008)
Merck
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs.
Bioorg Med Chem Lett 18: 23-7 (2008)
Glaxosmithkline
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Bioorg Med Chem Lett 18: 749-54 (2008)
Bristol-Myers Squibb Research And Development
The synthesis of bivalent 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)-8-heterobicyclo[3.2.1]octanes as probes for proximal binding sites on the dopamine and serotonin transporters.
Bioorg Med Chem 16: 1832-41 (2008)
Organix
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Bioorg Med Chem 16: 1562-95 (2008)
Johnson & Johnson Pharmaceutical Research & Development
Ohioensins F and G: protein tyrosine phosphatase 1B inhibitory benzonaphthoxanthenones from the Antarctic moss Polytrichastrum alpinum.
Bioorg Med Chem Lett 18: 772-5 (2008)
Silla University
Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs.
Bioorg Med Chem Lett 18: 28-33 (2008)
Glaxosmithkline
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.
Bioorg Med Chem Lett 18: 738-43 (2008)
Korea Research Institute Of Chemical Technology
4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.
J Med Chem 50: 6706-17 (2007)
Glaxosmithkline
N-(substituted-anilinoethyl)amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands.
J Med Chem 50: 6618-26 (2007)
Universit£
2-(2'-((dimethylamino)methyl)-4'-(fluoroalkoxy)-phenylthio)benzenamine derivatives as serotonin transporter imaging agents.
J Med Chem 50: 6673-84 (2007)
University Of Pennsylvania
Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.
J Med Chem 50: 6638-46 (2007)
University Of Antwerp
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes.
J Med Chem 50: 6450-3 (2007)
Boehringer Ingelheim Pharma
A p-[18F]fluoroethoxyphenyl bicyclic nucleoside analogue as a potential positron emission tomography imaging agent for varicella-zoster virus thymidine kinase gene expression.
J Med Chem 50: 6627-37 (2007)
Institute For Medical Research
Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease.
J Med Chem 50: 6446-9 (2007)
Bologna University
Scouting human A3 adenosine receptor antagonist binding mode using a molecular simplification approach: from triazoloquinoxaline to a pyrimidine skeleton as a key study.
J Med Chem 50: 6596-606 (2007)
Università
Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes.
Nature 450: 712-716 (2007)
Sirtris Pharmaceuticals
N6-1,3-diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: synthesis and biological evaluation as allosteric modulators of A2A adenosine receptors.
Eur J Med Chem 43: 1639-47 (2008)
Università
Bioactivities of a series of phosphodiesterase type 5 (PDE-5) inhibitors as modelled by MIA-QSAR.
Eur J Med Chem 43: 1632-8 (2008)
Universidade Federal De Lavras-Ufla
Chlorocyclinones A-D, chlorinated angucyclinones from Streptomyces sp. strongly antagonizing rosiglitazone-induced PPAR-gamma activation.
J Nat Prod 70: 1934-8 (2007)
Boehringer Ingelheim Pharma
Potent inhibition of human apurinic/apyrimidinic endonuclease 1 by arylstibonic acids.
Mol Pharmacol 73: 669-77 (2008)
The Johns Hopkins University
Protein protein interaction inhibition (2P2I) combining high throughput and virtual screening: Application to the HIV-1 Nef protein.
Proc Natl Acad Sci U S A 104: 19256-61 (2007)
Centre National De La Recherche Scientifique
N6-substituted C5'-modified adenosines as A1 adenosine receptor agonists.
Bioorg Med Chem 16: 1861-73 (2008)
Monash University (Parkville Campus)
New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.
Bioorg Med Chem 16: 1474-80 (2008)
Upres Ea 4021 Biomol�Cules Et Th�Rapies Anti-Tumorales
Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII.
Bioorg Med Chem Lett 18: 836-41 (2008)
Ecole Nationale Sup£Rieure De Chimie De Montpellier
Design and synthesis of a fluorescent muscarinic antagonist.
Bioorg Med Chem Lett 18: 825-7 (2008)
Pfizer
Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis.
Proc Natl Acad Sci U S A 104: 19512-7 (2007)
Mcgill University
Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group.
Bioorg Med Chem 16: 1613-31 (2008)
Ono Pharmaceutical
2-Aminoresorcinol is a potent alpha-glucosidase inhibitor.
Bioorg Med Chem Lett 18: 812-5 (2008)
Hokkaido University
Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38alpha MAP kinase inhibitors with excellent in vivo antiinflammatory properties.
Bioorg Med Chem Lett 18: 179-83 (2008)
Eli Lilly
Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.
Bioorg Med Chem Lett 18: 821-4 (2008)
Emd-Serono Research Institute
Design, synthesis, and biological activity of piperidine diamine derivatives as factor Xa inhibitor.
Bioorg Med Chem Lett 18: 782-7 (2008)
Daiichi Sankyo
Calcitonin gene-related peptide (CGRP) receptor antagonists: investigations of a pyridinone template.
Bioorg Med Chem Lett 18: 755-8 (2008)
Merck Research Laboratories
Alkaloids with human delta-opioid receptor binding affinity from the Australian rainforest tree Peripentadenia mearsii.
J Nat Prod 70: 1946-50 (2007)
Griffith University
Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
J Med Chem 50: 6607-17 (2007)
University Of California San Diego
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.
J Med Chem 50: 6519-34 (2007)
Glaxosmithkline
Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylases for cancer treatment.
J Med Chem 50: 6685-91 (2007)
University Of Minnesota
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
J Med Chem 50: 6443-5 (2007)
Eli Lilly
Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity.
J Med Chem 50: 6493-500 (2007)
Northeastern University
An efficient tool for identifying inhibitors based on 3D-QSAR and docking using feature-shape pharmacophore of biologically active conformation--a case study with CDK2/cyclinA.
Eur J Med Chem 43: 2807-18 (2008)
Institute Of Chemical Biology (Csir)
Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.
Bioorg Med Chem Lett 18: 66-71 (2008)
Incyte
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.
Bioorg Med Chem Lett 18: 159-63 (2008)
Incyte
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
Bioorg Med Chem 16: 1966-82 (2008)
Astellas Pharma
Estradiol and estrone C-16 derivatives as inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: blocking of ER+ breast cancer cell proliferation induced by estrone.
Bioorg Med Chem 16: 1849-60 (2008)
Chuq-Pavillon Chul And Universit£
An antidepressant that extends lifespan in adult Caenorhabditis elegans.
Nature 450: 553-556 (2007)
Howard Hughes Medical Institute
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.
Proc Natl Acad Sci U S A 104: 19244-9 (2007)
Ligand Pharmaceuticals
Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 18: 129-36 (2008)
Neurocrine Biosciences
Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives.
Bioorg Med Chem Lett 18: 147-51 (2008)
Ucb Pharma
Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors.
Bioorg Med Chem Lett 18: 241-6 (2008)
Bristol-Myers Squibb
The discovery of GSK221149A: a potent and selective oxytocin antagonist.
Bioorg Med Chem Lett 18: 90-4 (2008)
Glaxosmithkline
Picomolar inhibitors as transition-state probes of 5'-methylthioadenosine nucleosidases.
ACS Chem Biol 2: 725-34 (2007)
Albert Einstein College Of Medicine
Synthesis and structure-activity relationships of N-(3-phenylpropyl)-N'-benzylpiperazines: Potent ligands for sigma1 and sigma2 receptors.
Bioorg Med Chem 16: 755-61 (2008)
University Of Missouri-Columbia
Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.
Bioorg Med Chem Lett 17: 6723-8 (2008)
Merck Research Laboratories
Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
Bioorg Med Chem Lett 17: 6744-9 (2008)
Eli Lilly
A novel series of highly selective inhibitors of MMP-3.
Bioorg Med Chem Lett 17: 6750-3 (2008)
Pfizer
Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists.
Bioorg Med Chem Lett 17: 6773-8 (2008)
Johnson & Johnson
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
Bioorg Med Chem Lett 17: 6816-20 (2008)
Merck Frosst Centre For Therapeutic Research
Synthesis and evaluation of novel heterocyclic MMP inhibitors.
Bioorg Med Chem Lett 17: 6864-70 (2008)
North Dakota State University
Synthesis and solid-phase purification of anthranilic sulfonamides as CCK-2 ligands.
Bioorg Med Chem Lett 17: 6905-9 (2007)
Johnson & Johnson Pharmaceutical Research And Development
New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain.
J Med Chem 50: 6554-69 (2007)
Sapienza University Of Rome
Structure of the deacetylase LpxC bound to the antibiotic CHIR-090: Time-dependent inhibition and specificity in ligand binding.
Proc Natl Acad Sci U S A 104: 18433-8 (2007)
Duke University Medical Center
Antiplasmodial activity of [(aryl)arylsulfanylmethyl]Pyridine.
Antimicrob Agents Chemother 52: 705-15 (2008)
Central Drug Research Institute
Probing lipid- and drug-binding domains with fluorescent dyes.
Bioorg Med Chem 16: 1162-73 (2008)
European Molecular Biology Laboratory
A photoswitchable ITAM peptidomimetic: synthesis and real time surface plasmon resonance (SPR) analysis of the effects of cis-trans isomerization on binding.
Bioorg Med Chem 16: 1393-9 (2008)
Utrecht University
Synthesis of 4,5,6,7-tetrahydrothieno[3,2-c]pyridines and comparison with their isosteric 1,2,3,4-tetrahydroisoquinolines as inhibitors of phenylethanolamine N-methyltransferase.
Bioorg Med Chem 16: 542-59 (2008)
The University Of Kansas
Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation.
Bioorg Med Chem Lett 18: 329-35 (2008)
Columbia University
Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17.
Bioorg Med Chem Lett 18: 267-73 (2008)
Saarland University
Discovery of a series of aminopiperidines as novel iNOS inhibitors.
Bioorg Med Chem Lett 18: 336-43 (2008)
Adolor
Design and synthesis of 4-quinolinone 2-carboxamides as calpain inhibitors.
Bioorg Med Chem Lett 18: 205-9 (2008)
Kyung Hee University
QSAR analysis of 1,3-diaryl-4,5,6,7-tetrahydro-2H-isoindole derivatives as selective COX-2 inhibitors.
Eur J Med Chem 43: 1559-69 (2008)
Dr Hs Gour University
Phosphoramidate derivatives of hydroxysteroids as inhibitors of prostate-specific membrane antigen.
Bioorg Med Chem Lett 18: 281-4 (2008)
Washington State University
Nitrogen-appended N-alkylsulfonamides as inhibitors of gamma-secretase.
Bioorg Med Chem Lett 18: 175-8 (2008)
Bristol-Myers Squibb
Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.
Bioorg Med Chem Lett 18: 414-7 (2008)
Schering-Plough Research Institute
Development of dimeric modulators for anti-apoptotic Bcl-2 proteins.
Bioorg Med Chem Lett 18: 236-40 (2008)
University Of Minnesota Minneapolis
4-Aminopyridine derivatives with anticholinesterase and antiamnesic activity.
Bioorg Med Chem Lett 18: 309-12 (2008)
Sapienza University Of Rome
Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.
Bioorg Med Chem Lett 18: 386-90 (2008)
Abbott Laboratories
Identification of novel inhibitors of bacterial surface enzyme Staphylococcus aureus Sortase A.
Bioorg Med Chem Lett 18: 380-5 (2008)
University Of Alabama At Birmingham
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration.
Bioorg Med Chem Lett 18: 262-6 (2008)
F. Hoffmann-La Roche
Synthesis of fluorine substituted pyrazolopyrimidines as potential leads for the development of PET-imaging agents for the GABAA receptors.
Bioorg Med Chem 16: 1184-94 (2008)
Abx Advanced Biochemical Compounds
Influence of sulfur oxidation state and steric bulk upon trifluoromethyl ketone (TFK) binding kinetics to carboxylesterases and fatty acid amide hydrolase (FAAH).
Bioorg Med Chem 16: 2114-30 (2008)
University Of California
Synthesis and cyclooxygenase inhibitory activities of linear 1-(methanesulfonylphenyl or benzenesulfonamido)-2-(pyridyl)acetylene regioisomers.
Bioorg Med Chem 16: 1948-56 (2008)
University Of Alberta
Trisubstituted 1,2,4-triazoles as ligands for the ghrelin receptor: on the significance of the orientation and substitution at position 3.
Bioorg Med Chem Lett 18: 164-8 (2008)
University Of Montpellier
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
Bioorg Med Chem Lett 18: 54-9 (2008)
Wyeth Pharmaceuticals
Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth.
Chem Biol 14: 1283-93 (2007)
Vanderbilt University
Inverse in silico screening for identification of kinase inhibitor targets.
Chem Biol 14: 1207-14 (2007)
University Of Munich
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.
J Med Chem 51: 196-218 (2008)
Vernalis (R&D)
From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling.
J Med Chem 50: 6295-8 (2007)
F. Hoffmann-La Roche
Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach.
J Med Chem 50: 6291-4 (2007)
F. Hoffmann-La Roche
Derrubone, an inhibitor of the Hsp90 protein folding machinery.
J Nat Prod 70: 2014-8 (2007)
The University Of Kansas
Synthesis of natural product-inspired inhibitors of Mycobacterium tuberculosis mycothiol-associated enzymes: the first inhibitors of GlcNAc-Ins deacetylase.
J Med Chem 50: 6326-36 (2007)
National Institute Of Diabetes And Digestive And Kidney Diseases
Imine derivatives as new potent and selective CB2 cannabinoid receptor agonists with an analgesic action.
Bioorg Med Chem 16: 1111-24 (2008)
Taisho Pharmaceutical
Novel GSK-3beta inhibitors from sequential virtual screening.
Bioorg Med Chem 16: 636-43 (2008)
Korea Institute Of Science And Technology
Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors.
Bioorg Med Chem Lett 18: 366-70 (2008)
Kyoto Pharmaceutical University
Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists.
Bioorg Med Chem Lett 18: 223-7 (2008)
University Of Bonn
3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists.
Bioorg Med Chem Lett 18: 228-31 (2008)
Schering-Plough Research Institute
7-Azaindole derivatives as potential partial nicotinic agonists.
Bioorg Med Chem Lett 18: 188-93 (2008)
Solvay Pharmaceuticals
Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode.
Bioorg Med Chem Lett 18: 318-23 (2008)
Gsk
Synthesis, binding properties and receptor docking of 4-halo-6-[2-(4-arylpiperazin-1-yl)ethyl]-1H-benzimidazoles, mixed ligands of D2 and 5-HT1A receptors.
Eur J Med Chem 43: 1696-705 (2008)
University Of Belgrade
Selectivity-determining residues in Plk1.
Chem Biol Drug Des 70: 540-6 (2007)
Pfizer
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