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Developing dual functional allosteric modulators of GABA(A) receptors.
Bioorg Med Chem 18: 8374-82 (2010)
Astrazeneca Pharmaceuticals
Virtual screening against nuclear factor¿B (NF-¿B) of a focus library: Identification of bioactive furocoumarin derivatives inhibiting NF-¿B dependent biological functions involved in cystic fibrosis.
Bioorg Med Chem 18: 8341-9 (2010)
Biopharmanet
Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands.
Bioorg Med Chem 18: 8356-64 (2010)
University Of New Orleans
4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series.
J Med Chem 53: 7918-31 (2010)
Universite£? Lille-Nord De France
Characterization of nicotinamidases: steady state kinetic parameters, classwide inhibition by nicotinaldehydes, and catalytic mechanism.
Biochemistry 49: 10421-39 (2010)
Cornell University
Novela3ß4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation.
J Med Chem 53: 8187-91 (2010)
Sri International
Bicyclic substituted hydroxyphenylmethanones as novel inhibitors of 17ß-hydroxysteroid dehydrogenase type 1 (17ß-HSD1) for the treatment of estrogen-dependent diseases.
J Med Chem 53: 8176-86 (2010)
Saarland University
Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2.
Bioorg Med Chem Lett 20: 6989-92 (2010)
Glaxosmithkline
Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors.
Bioorg Med Chem Lett 20: 6960-5 (2010)
F. Hoffmann-La Roche
Synthesis and biological evaluation of N-substituted-3,5-diphenyl-2-pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors.
Eur J Med Chem 45: 6135-8 (2010)
Sapienza University Of Rome
Furan-2,5-dimethylene-tethered bis-imidacloprid insecticide conferring high potency.
J Agric Food Chem 58: 11832-6 (2010)
Gifu University
In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease.
J Med Chem 53: 8104-15 (2010)
Johnson & Johnson Pharmaceutical Research And Development
Discovery and synthesis of novel luteolin derivatives as DAT agonists.
Bioorg Med Chem 18: 7842-8 (2010)
Zhengzhou University
Towards a stable noeuromycin analog with a D-manno configuration: synthesis and glycosidase inhibition of D-manno-like tri- and tetrahydroxylated azepanes.
Bioorg Med Chem 20: 641-9 (2012)
Umr Cnrs 7201
N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 inhibitors. Part 1.
Bioorg Med Chem Lett 20: 6983-8 (2010)
Glaxosmithkline
Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.
Bioorg Med Chem Lett 20: 7037-41 (2010)
Array Biopharma
Receptor agonists of macrophage migration inhibitory factor.
Bioorg Med Chem Lett 20: 7033-6 (2010)
Yale University
Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists.
Bioorg Med Chem Lett 20: 6969-74 (2010)
F. Hoffmann-La Roche
N-substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators.
Bioorg Med Chem Lett 20: 7116-9 (2010)
Glaxosmithkline
Indazole derivatives as novel bradykinin B1 receptor antagonists.
Bioorg Med Chem Lett 20: 7011-4 (2010)
Merck Research Laboratories
The synthesis and SAR of novel diarylsulfone 11ß-HSD1 inhibitors.
Bioorg Med Chem Lett 20: 7071-5 (2010)
Amgen
2-Azetidinone--a new profile of various pharmacological activities.
Eur J Med Chem 45: 5541-60 (2010)
Barkatullah University
Probing the active-site requirements of human intestinal N-terminal maltase-glucoamylase: Synthesis and enzyme inhibitory activities of a six-membered ring nitrogen analogue of kotalanol and its de-O-sulfonated derivative.
Bioorg Med Chem 18: 7794-8 (2010)
Simon Fraser University
Sulfonamide derivatives of styrylheterocycles as a potent inhibitor of COX-2-mediated prostaglandin E2 production.
Bioorg Med Chem Lett 20: 6938-41 (2010)
Seoul National University
Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents.
Eur J Med Chem 45: 6027-38 (2010)
Alexandria University
Identification of clinically used drugs that activate pregnane X receptors.
Drug Metab Dispos 39: 151-9 (2010)
National Institutes Of Health Chemical Genomics Center
Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols.
Bioorg Med Chem 18: 8005-15 (2010)
Institut FüR Pharmazeutische Und Medizinische Chemie Der WestfäLischen Wilhelms-UniversitäT MüNster
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.
Bioorg Med Chem 18: 7816-25 (2010)
Abbott Laboratories
Synthesis and SAR studies of chiral non-racemic dexoxadrol analogues as uncompetitive NMDA receptor antagonists.
Bioorg Med Chem 18: 7855-67 (2010)
Institut FüR Pharmazeutische Und Medizinische Chemie Der WestfäLischen Wilhelms-UniversitäT MüNster
5-benzyloxytryptamine as an antagonist of TRPM8.
Bioorg Med Chem Lett 20: 7076-9 (2010)
Renovis
Identification of potent ITK inhibitors through focused compound library design including structural information.
Bioorg Med Chem Lett 20: 6998-7003 (2010)
Nycomed
Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs).
Eur J Med Chem 45: 5919-25 (2010)
Protera
Citrusosides A-D and furanocoumarins with cholinesterase inhibitory activity from the fruit peels of Citrus hystrix.
J Nat Prod 73: 1879-83 (2010)
Ramkhamhaeng University
Synthesis and biological evaluation of oleanolic acid derivatives as inhibitors of protein tyrosine phosphatase 1B.
J Nat Prod 73: 1743-50 (2010)
Xihua University
Probing the active site of the deoxynucleotide N-hydrolase Rcl encoded by the rat gene c6orf108.
J Biol Chem 285: 41806-14 (2010)
Institut Pasteur
Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents.
Bioorg Med Chem 18: 7826-35 (2010)
Federal University Of Pernambuco
5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists.
Bioorg Med Chem Lett 20: 7015-9 (2010)
Amri
Highly brominated metabolites from marine red alga Laurencia similis inhibit protein tyrosine phosphatase 1B.
Bioorg Med Chem Lett 20: 7152-4 (2010)
Jilin University
Design and synthesis of tetrahydropyridothieno[2,3-d]pyrimidine scaffold based epidermal growth factor receptor (EGFR) kinase inhibitors: the role of side chain chirality and Michael acceptor group for maximal potency.
J Med Chem 53: 7316-26 (2010)
National Health Research Institutes
Ipomotaosides A-D, resin glycosides from the aerial parts of Ipomoea batatas and their inhibitory activity against COX-1 and COX-2.
J Nat Prod 73: 1763-6 (2010)
Tokushima Bunri University
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.
J Med Chem 53: 7874-8 (2010)
Pfizer
Identification of a Natural Product Antagonist against the Botulinum Neurotoxin Light Chain Protease.
ACS Med Chem Lett 1: 268-272 (2010)
TBA
Exploration of the active site of neuronal nitric oxide synthase by the design and synthesis of pyrrolidinomethyl 2-aminopyridine derivatives.
J Med Chem 53: 7804-24 (2010)
Northwestern University
Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones.
J Med Chem 53: 7699-708 (2010)
University Of Massachusetts Medical School
Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.
J Med Chem 53: 7573-86 (2010)
University Of North Carolina At Chapel Hill
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
J Med Chem 53: 7879-82 (2010)
Kumamoto University
Triterpenoidal alkaloids from Buxus natalensis and their acetylcholinesterase inhibitory activity.
J Nat Prod 73: 1858-62 (2010)
The University Of Winnipeg
Pyrimidinylmethylphenyl glucoside as novel C-aryl glucoside SGLT2 inhibitors.
Bioorg Med Chem Lett 20: 7046-9 (2010)
Green Cross
Tetrahydrocarboline analogs as MCH-1 antagonists.
Bioorg Med Chem Lett 20: 7024-8 (2010)
Amri
Ligand-based virtual screening and ADME-tox guided approach to identify triazolo-quinoxalines as folate cycle inhibitors.
Bioorg Med Chem 18: 7773-85 (2010)
Università
5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.
Bioorg Med Chem Lett 20: 7092-6 (2010)
Glaxosmithkline
Antimalarial histone deacetylase inhibitors containing cinnamate or NSAID components.
Bioorg Med Chem Lett 20: 7080-4 (2010)
The University Of Queensland
Design, synthesis and inhibitory activity against Mycobacterium tuberculosis thymidine monophosphate kinase of acyclic nucleoside analogues with a distal imidazoquinolinone.
Eur J Med Chem 45: 5910-8 (2010)
Instituto De Qu£Mica M£Dica (Csic)
Synthesis and structure-activity relationships of tyrosine-based inhibitors of autotaxin (ATX).
Bioorg Med Chem Lett 20: 7132-6 (2010)
University Of Virginia
Small molecule inhibitors of hantavirus infection.
Bioorg Med Chem Lett 20: 7085-91 (2010)
University Of New Mexico School Of Medicine
Substituted spiro [2.3'] oxindolespiro [3.2¿]-5,6-dimethoxy-indane-1¿-one-pyrrolidine analogue as inhibitors of acetylcholinesterase.
Bioorg Med Chem Lett 20: 7064-6 (2010)
Universiti Sains Malaysia
Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity.
Bioorg Med Chem Lett 20: 7020-3 (2010)
Amri
Design, synthesis and SAR of a novel series of benzimidazoles as potent NPY Y5 antagonists.
Bioorg Med Chem Lett 20: 7120-3 (2010)
Glaxosmithkline
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
J Med Chem 53: 7564-72 (2010)
Bristol-Myers Squibb
Synthesis, biological evaluation, and molecular docking studies of 2-chloropyridine derivatives possessing 1,3,4-oxadiazole moiety as potential antitumor agents.
Bioorg Med Chem 18: 7836-41 (2010)
Nanjing University
The binding ofß-d-glucopyranosyl-thiosemicarbazone derivatives to glycogen phosphorylase: A new class of inhibitors.
Bioorg Med Chem 18: 7911-22 (2010)
National Hellenic Research Foundation
Structural insights into the hot spot amino acid residues of mushroom tyrosinase for the bindings of thujaplicins.
Bioorg Med Chem 18: 8112-8 (2010)
Institute For Theoretical Medicine
Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors.
Bioorg Med Chem 18: 7849-54 (2010)
Academia Sinica
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists.
Bioorg Med Chem Lett 20: 7137-41 (2010)
Johnson & Johnson Pharmaceutical Research And Development
Inhibitors selective for HDAC6 in enzymes and cells.
Bioorg Med Chem Lett 20: 7067-70 (2010)
The University Of Queensland
A targeted low molecular weight near-infrared fluorescent probe for prostate cancer.
Bioorg Med Chem Lett 20: 7124-6 (2010)
Washington State University
Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.
J Med Chem 53: 7869-73 (2010)
Abbott Laboratories
Design, synthesis, crystal structures, and antimicrobial activity of sulfonamide boronic acids asß-lactamase inhibitors.
J Med Chem 53: 7852-63 (2010)
University Of California San Francisco
Synthesis and evaluation of 5-substituted 9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as check point 1 kinase inhibitors.
Bioorg Med Chem 18: 7878-89 (2010)
Hokkaido University
1-Bromo-3-(1',1'-dimethylalkyl)-1-deoxy-¿(8)-tetrahydrocannabinols: New selective ligands for the cannabinoid CB(2) receptor.
Bioorg Med Chem 18: 7809-15 (2010)
Clemson University
Molecular modeling study on potent and selective adenosine A(3) receptor agonists.
Bioorg Med Chem 18: 7923-30 (2010)
University Of Camerino
Anticonvulsant activity of 2,4(1H)-diarylimidazoles in mice and rats acute seizure models.
Bioorg Med Chem 18: 7957-65 (2010)
Università
4-Phenylcoumarins from Mesua elegans with acetylcholinesterase inhibitory activity.
Bioorg Med Chem 18: 7873-7 (2010)
University Of Malaya
Design, synthesis and biological evaluation of quinoline amide derivatives as novel VEGFR-2 inhibitors.
Bioorg Med Chem Lett 20: 6653-6 (2010)
Nanjing University
Synthesis and biological evaluation of [D-lysine]8cyclosporin A analogs as potential anti-HCV agents.
Bioorg Med Chem Lett 20: 6542-6 (2010)
Scynexis
Triazolyl tryptoline derivatives asß-secretase inhibitors.
Bioorg Med Chem Lett 20: 6572-6 (2010)
Mahidol University
Detection of Rap1A as a yessotoxin binding protein from blood cell membranes.
Bioorg Med Chem Lett 20: 6443-6 (2010)
Osaka University
Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands.
Eur J Med Chem 45: 5878-86 (2010)
Sapienza University Of Rome
Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.
J Med Chem 53: 7778-95 (2010)
Glaxosmithkline
First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis.
J Med Chem 53: 7715-30 (2010)
Genkyotex
Synthesis and SAR comparative studies of 2-allyl-4-methoxy-1-alkoxybenzenes as 15-lipoxygenase inhibitors.
J Enzyme Inhib Med Chem 26: 238-44 (2011)
Mashhad University Of Medical Sciences
The inhibition study of human UDP-glucuronosyltransferases with cytochrome P450 selective substrates and inhibitors.
J Enzyme Inhib Med Chem 26: 386-93 (2011)
Guangzhou Institutes Of Biomedicine And Health, Chinese Academy Of Sciences
Synthesis and biological evaluation of polyhydroxy benzophenone as mushroom tyrosinase inhibitors.
J Enzyme Inhib Med Chem 26: 449-52 (2011)
Sun Yat-Sen University
Isolation and characterization of minor analogues of silvestrol and other constituents from a large-scale re-collection of Aglaia foveolata.
J Nat Prod 73: 1873-8 (2010)
The Ohio State University
Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin.
Bioorg Med Chem 18: 8092-105 (2010)
Seoul National University
Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.
Bioorg Med Chem 18: 7890-9 (2010)
Dipartimento Di Scienze Farmaceutiche
A diverse series of substituted benzenesulfonamides as aldose reductase inhibitors with antioxidant activity: design, synthesis, and in vitro activity.
J Med Chem 53: 7756-66 (2010)
Aristotle University Of Thessaloniki
Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization.
J Med Chem 53: 7682-98 (2010)
The Institute Of Cancer Research
Synthesis and molecular modelling studies of prenylated pyrazolines as MAO-B inhibitors.
Bioorg Med Chem Lett 20: 6479-82 (2010)
Sapienza University Of Rome
Synthesis anda1-adrenoceptor antagonist activity of tamsulosin analogues.
Eur J Med Chem 45: 5800-7 (2010)
Universit£
BACE1 inhibitory activities of enantiomerically pure, variously substituted N-(3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropyl) arylsulfonamides.
Bioorg Med Chem 18: 7991-6 (2010)
University Of Pisa
Design, synthesis and bioevaluation of dihydropyrazolo[3,4-b]pyridine and benzo[4,5]imidazo[1,2-a]pyrimidine compounds as dual KSP and Aurora-A kinase inhibitors for anti-cancer agents.
Bioorg Med Chem 18: 8035-43 (2010)
China Pharmaceutical University
Biflavonoids from Torreya nucifera displaying SARS-CoV 3CL(pro) inhibition.
Bioorg Med Chem 18: 7940-7 (2010)
Korea Research Institute Of Bioscience And Biotechnology
Design, syntheses and 3D-QSAR studies of novel N-phenyl pyrrolidin-2-ones and N-phenyl-1H-pyrrol-2-ones as protoporphyrinogen oxidase inhibitors.
Bioorg Med Chem 18: 7948-56 (2010)
Central China Normal University
Structure-activity relationships for inhibition of inosine monophosphate dehydrogenase and differentiation induction of K562 cells among the mycophenolic acid derivatives.
Bioorg Med Chem 18: 8106-11 (2010)
Hokkaido University
Tri- and tetrasubstituted imidazoles as p38a mitogen-activated protein kinase inhibitors.
Bioorg Med Chem Lett 20: 6671-5 (2010)
Eberhard-Karls University Of TüBingen
Kojyl thioether derivatives having both tyrosinase inhibitory and anti-inflammatory properties.
Bioorg Med Chem Lett 20: 6569-71 (2010)
Amorepacific
New stilbenoid with inhibitory activity on viral neuraminidases from Erythrina addisoniae.
Bioorg Med Chem Lett 20: 6430-4 (2010)
Chosun University
Substituted pyrazoles as novel sEH antagonist: investigation of key binding interactions within the catalytic domain.
Bioorg Med Chem Lett 20: 6379-83 (2010)
Boehringer Ingelheim Pharmaceuticals
Design, syntheses, and SAR of 2,8-diazaspiro[4.5]decanones as T-type calcium channel antagonists.
Bioorg Med Chem Lett 20: 6375-8 (2010)
Icagen
An in situ oxidation strategy towards overcoming hERG affinity.
Bioorg Med Chem Lett 20: 6400-4 (2010)
Pfizer
Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor.
Bioorg Med Chem Lett 20: 6370-4 (2010)
Glaxosmithkline
Inhibition of Bfl-1 with N-aryl maleimides.
Bioorg Med Chem Lett 20: 6560-4 (2010)
Human Biomolecular Research Institute
Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7.
Bioorg Med Chem Lett 20: 6384-6 (2010)
University Of Kansas
N-Substituted acetamidines and 2-methylimidazole derivatives as selective inhibitors of neuronal nitric oxide synthase.
Bioorg Med Chem Lett 20: 6495-9 (2010)
Università
Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.
Bioorg Med Chem Lett 20: 6610-5 (2010)
Baylor University
Design, synthesis, and structure-activity relationship studies of N-arylsulfonyl morpholines as¿-secretase inhibitors.
Bioorg Med Chem Lett 20: 6606-9 (2010)
Merck Research Lab.
2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists.
Bioorg Med Chem Lett 20: 6405-7 (2010)
Glaxosmithkline
2-Aryl benzimidazoles: human SCD1-specific stearoyl coenzyme-A desaturase inhibitors.
Bioorg Med Chem Lett 20: 6366-9 (2010)
Merck Frosst Centre For Therapeutic Research
Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment.
Bioorg Med Chem Lett 20: 6387-93 (2010)
Merck Frosst Centre For Therapeutic Research
Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity.
Bioorg Med Chem Lett 20: 6524-32 (2010)
Merck Research Laboratories
Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.
Bioorg Med Chem Lett 20: 6439-42 (2010)
Green Cross
Building a MCHR1 homology model provides insight into the receptor-antagonist contacts that are important for the development of new anti-obesity agents.
Bioorg Med Chem 18: 7365-79 (2010)
Universidad De Navarra
4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors.
Bioorg Med Chem Lett 20: 6489-94 (2010)
Nerviano Medical Sciences
Development of novel inhibitors targeting HIF-1a towards anticancer drug discovery.
Bioorg Med Chem Lett 20: 6426-9 (2010)
Piramal Life Sciences
1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties.
Bioorg Med Chem Lett 20: 7142-6 (2010)
Johnson & Johnson Pharmaceutical Research And Development
The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity.
Bioorg Med Chem Lett 20: 6394-9 (2010)
Ansaris
Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution.
Bioorg Med Chem Lett 20: 6483-8 (2010)
Vernalis (R&D)
Synthesis and pharmacological activity of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acids as selective ET(A) antagonists.
Bioorg Med Chem Lett 20: 6840-4 (2010)
St. John'S University
Synthesis of novel chiral¿2-isoxazoline derivatives related to ABT-418 and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes.
Eur J Med Chem 45: 5594-601 (2010)
Universit£
5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists.
J Med Chem 53: 7639-46 (2010)
Wyeth Research
Identification of non-peptide malignant brain tumor (MBT) repeat antagonists by virtual screening of commercially available compounds.
J Med Chem 53: 7625-31 (2010)
University Of North Carolina At Chapel Hill
Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) part 2: identification of a novel, potent, and selective series of benzimidazole-quinolinone iNOS/nNO
J Med Chem 53: 7739-55 (2010)
Kalypsys
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.
J Med Chem 53: 7549-63 (2010)
Aska Pharmaceutical
Mammea E/BB, an isoprenylated dihydroxycoumarin protonophore that potently uncouples mitochondrial electron transport, disrupts hypoxic signaling in tumor cells.
J Nat Prod 73: 1868-72 (2010)
University Of Mississippi
Rational design, synthesis, and evaluation of new selective inhibitors of microbial class II (zinc dependent) fructose bis-phosphate aldolases.
J Med Chem 53: 7836-42 (2010)
Paris-Sud University
Indapamide-like benzenesulfonamides as inhibitors of carbonic anhydrases I, II, VII, and XIII.
Bioorg Med Chem 18: 7357-64 (2010)
Institute Of Biotechnology
3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP3 receptor antagonists.
Bioorg Med Chem Lett 20: 6744-7 (2010)
Glaxosmithkline
Molecular docking and QSAR study on steroidal compounds as aromatase inhibitors.
Eur J Med Chem 45: 5612-20 (2010)
Tianjin University Of Science And Technology
Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow's neuroprotective therapies against neurodegenerative diseases.
Eur J Med Chem 45: 6152-8 (2010)
Instituto De Qu£Mica M£Dica
Novel alkyl- and arylcarbamate derivatives with N-benzylpiperidine and N-benzylpiperazine moieties as cholinesterases inhibitors.
Eur J Med Chem 45: 5602-11 (2010)
Jagiellonian University Medical College
Novel 1',1'-chain substituted hexahydrocannabinols: 9ß-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol (AM2389) a highly potent cannabinoid receptor 1 (CB1) agonist.
J Med Chem 53: 6996-7010 (2010)
Northeastern University
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
J Med Chem 53: 6779-810 (2010)
Aristotle University Of Thessaloniki
Fruitful adrenergica(2C)-agonism/a(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
J Med Chem 53: 7825-35 (2010)
Universita` Di Camerino
Mechanistic studies of the inactivation of TEM-1 and P99 by NXL104, a novel non-beta-lactam beta-lactamase inhibitor.
Antimicrob Agents Chemother 54: 5132-8 (2010)
Novexel
Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factorß receptor I (TGFßRI).
J Med Chem 53: 7287-95 (2010)
Boehringer Ingelheim Pharma
Structural and biochemical characterization of Mycobacterium tuberculosis CYP142: evidence for multiple cholesterol 27-hydroxylase activities in a human pathogen.
J Biol Chem 285: 38270-82 (2010)
Manchester Interdisciplinary Biocentre
Fluorescent-tagged sp2-iminosugars with potentß-glucosidase inhibitory activity.
Bioorg Med Chem 18: 7439-45 (2010)
Universidad De Sevilla
3D QSAR study, synthesis, and in vitro evaluation of (+)-5-FBVM as potential PET radioligand for the vesicular acetylcholine transporter (VAChT).
Bioorg Med Chem 18: 7659-67 (2010)
University Of Tours
4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII.
Bioorg Med Chem 18: 7413-21 (2010)
Vilnius University
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.
Bioorg Med Chem Lett 20: 6538-41 (2010)
Amri
Massive screening yields novel and selective Trypanosoma cruzi triosephosphate isomerase dimer-interface-irreversible inhibitors with anti-trypanosomal activity.
Eur J Med Chem 45: 5767-72 (2010)
Universidad De La Rep£Blica
Novel selective anti-androgens with a diphenylpentane skeleton.
Bioorg Med Chem Lett 20: 6661-6 (2010)
The University Of Tokyo
Bromophenols as Candida albicans isocitrate lyase inhibitors.
Bioorg Med Chem Lett 20: 6644-8 (2010)
Seoul National University
Synthesis and evaluation of bivalent, peptidomimetic antagonists of theavß3 integrins.
Bioorg Med Chem Lett 20: 6577-80 (2010)
The Methodist Hospital Research Institute
Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT(1A) receptors.
Bioorg Med Chem Lett 20: 6628-32 (2010)
Università
Design of more potent squalene synthase inhibitors with multiple activities.
Bioorg Med Chem 18: 7402-12 (2010)
University Of Athens
Design, synthesis, and subtype selectivity of 3,6-disubstitutedß-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Bioorg Med Chem 18: 7548-64 (2010)
University Of Wisconsin-Milwaukee
Discovery of a vorapaxar analog with increased aqueous solubility.
Bioorg Med Chem Lett 20: 6676-9 (2010)
Merck Research Laboratories
Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.
Bioorg Med Chem Lett 20: 6592-6 (2010)
Ansaris
Convenient synthesis and biological profile of 5-amino-substituted 1,2,4-oxadiazole derivatives.
Eur J Med Chem 45: 5635-45 (2010)
Democritus University Of Thrace
C-Methylated Flavonoids from Cleistocalyx operculatus and Their Inhibitory Effects on Novel Influenza A (H1N1) Neuraminidase.
J Nat Prod 73: 1636-42 (2010)
Chosun University
Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.
Bioorg Med Chem Lett 20: 6657-60 (2010)
Chroma Therapeutics
Synthesis, biological evaluation and docking studies of 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives.
Eur J Med Chem 45: 5678-84 (2010)
University Of Lille
An o-aminoanilide analogue of 1a,25-dihydroxyvitamin D(3) functions as a strong vitamin D receptor antagonist.
J Med Chem 53: 7461-5 (2010)
Mcgill University
Targeted mutations of Bacillus anthracis dihydrofolate reductase condense complex structure-activity relationships.
J Med Chem 53: 7327-36 (2010)
University Of Connecticut
Design, solid-phase synthesis, and biological evaluation of novel 1,5-diarylpyrrole-3-carboxamides as carbonic anhydrase IX inhibitors.
Bioorg Med Chem 18: 7392-401 (2010)
University Of Lille
Identification of 9-fluoro substituted (-)-cytisine derivatives as ligands with high affinity for nicotinic receptors.
Bioorg Med Chem Lett 20: 6667-70 (2010)
Ensicaen-Université
Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.
Bioorg Med Chem Lett 20: 6597-605 (2010)
Pfizer
Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase.
Bioorg Med Chem Lett 20: 6649-52 (2010)
Sun Yat-Sen University
(Z)-3-butylidenephthalide from Ligusticum porteri , ana-glucosidase inhibitor.
J Nat Prod 74: 314-20 (2011)
Universidad Nacional Auto£?Noma De Me£?Xico
Kinetics and inhibition of nicotinamidase from Mycobacterium tuberculosis.
Biochemistry 49: 9613-9 (2010)
Albert Einstein College Of Medicine
Synthesis and biological evaluation of radio-iodinated benzimidazoles as SPECT imaging agents for NR2B subtype of NMDA receptor.
Bioorg Med Chem 18: 7497-506 (2010)
Hamamatsu University School Of Medicine
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Bioorg Med Chem 18: 7675-99 (2010)
Pfizer
5,6,7,8-Tetrahydropyrido[4,3-d]pyrimidines as novel class of potent and highly selective CaMKII inhibitors.
Bioorg Med Chem Lett 20: 6696-8 (2010)
Dainippon Sumitomo Pharma
Carbocycles related to oseltamivir as influenza virus group-1-specific neuraminidase inhibitors. Binding to N1 enzymes in the context of virus-like particles.
J Med Chem 53: 7377-91 (2010)
Simon Fraser University
Novel agonists and antagonists for human protease activated receptor 2.
J Med Chem 53: 7428-40 (2010)
The University Of Queensland
Assessment of structurally diverse philanthotoxin analogues for inhibitory activity on ionotropic glutamate receptor subtypes: discovery of nanomolar, nonselective, and use-dependent antagonists.
J Med Chem 53: 7441-51 (2010)
University Of Copenhagen
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.
J Med Chem 53: 7296-315 (2010)
Nerviano Medical Sciences
Design, synthesis, radiolabeling, and in vivo evaluation of carbon-11 labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a potential positron emission tomography tracer for the dopamine D(4) receptors.
J Med Chem 53: 7344-55 (2010)
Universita` Degli Studi Di Bari A Moro
Selective inhibition of BET bromodomains.
Nature 468: 1067-73 (2010)
University Of Oxford
Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors.
Bioorg Med Chem 18: 7580-5 (2010)
Ewha Womans University
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.
Bioorg Med Chem Lett 20: 6587-91 (2010)
Abbott Laboratories
3D-QSAR and docking studies on pyrazolo[4,3-h]qinazoline-3-carboxamides as cyclin-dependent kinase 2 (CDK2) inhibitors.
Bioorg Med Chem Lett 20: 6764-72 (2010)
Jinan University
Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold.
Bioorg Med Chem Lett 20: 6754-7 (2010)
Merck And
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.
Eur J Med Chem 45: 5420-7 (2010)
Konkuk University
9-Dihydroerythromycin ethers as motilin agonists--developing structure-activity relationships for potency and safety.
Bioorg Med Chem 18: 7651-8 (2010)
Kosan Biosciences
Discovery of 2-aminoimidazopyridine adenosine A(2A) receptor antagonists.
Bioorg Med Chem Lett 20: 6845-9 (2010)
Ligand Pharmaceuticals
Discovery of potent and selective inhibitors of human reticulocyte 15-lipoxygenase-1.
J Med Chem 53: 7392-404 (2010)
National Human Genome Research Institute
Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1.
Bioorg Med Chem Lett 20: 6725-9 (2010)
Vitae Pharmaceuticals
Development of the next generation of HIV-1 integrase inhibitors: pyrazolone as a novel inhibitor scaffold.
Bioorg Med Chem Lett 20: 6854-7 (2010)
University Of Southern California
Antidotes to anthrax lethal factor intoxication. Part 1: Discovery of potent lethal factor inhibitors with in vivo efficacy.
Bioorg Med Chem Lett 20: 6850-3 (2010)
Panthera Biopharma
Synthesis and characterisation of two novel proton transfer compounds and their inhibition studies on carbonic anhydrase isoenzymes.
J Enzyme Inhib Med Chem 26: 104-14 (2011)
Dumlupinar University
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
J Med Chem 53: 7167-79 (2010)
Friedrich-Alexander University
Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.
J Med Chem 53: 7146-55 (2010)
Dana-Farber Cancer Institute
Design and synthesis of prolylcarboxypeptidase (PrCP) inhibitors to validate PrCP as a potential target for obesity.
J Med Chem 53: 7251-63 (2010)
Merck Research Laboratories
Structure-activity relationship study of first selective inhibitor of excitatory amino acid transporter subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101).
J Med Chem 53: 7180-91 (2010)
University Of Copenhagen
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity fora(1)-adrenoceptors.
J Med Chem 53: 7021-34 (2010)
University Of Copenhagen
2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections.
Bioorg Med Chem 18: 7475-85 (2010)
University Of London
Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series.
Bioorg Med Chem Lett 20: 6802-7 (2010)
Roche Palo Alto
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Bioorg Med Chem Lett 20: 6812-5 (2010)
Abbott Laboratories
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Bioorg Med Chem Lett 20: 6739-43 (2010)
Merck Research Laboratories
Aldehyde oxidase: an enzyme of emerging importance in drug discovery.
J Med Chem 53: 8441-60 (2010)
Pfizer
Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11ß-hydroxysteroid dehydrogenase 2 inhibitors.
Bioorg Med Chem 18: 7522-41 (2010)
University Of Natural Resources And Applied Life Sciences
Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.
Bioorg Med Chem Lett 20: 6797-801 (2010)
Pfizer
Novel CGRP receptor antagonists from central amide replacements causing a reversal of preferred chirality.
Bioorg Med Chem Lett 20: 6827-30 (2010)
Merck
Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.
Bioorg Med Chem Lett 20: 6735-8 (2010)
F. Hoffmann-La Roche
Novel thiazolidinedione derivatives with anti-obesity effects: dual action as PTP1B inhibitors and PPAR-¿ activators.
Bioorg Med Chem Lett 20: 6758-63 (2010)
Inha University
Expansion of SAR studies on triaryl bis sulfone cannabinoid CB2 receptor ligands.
Bioorg Med Chem Lett 20: 6785-9 (2010)
Merck Research Laboratories
Molecular docking and structure-activity relationship studies on benzothiazole based non-peptidic BACE-1 inhibitors.
Bioorg Med Chem Lett 20: 6203-7 (2010)
Singapore Polytechnic
Indole alkaloids from Ervatamia hainanensis with potent acetylcholinesterase inhibition activities.
Bioorg Med Chem Lett 20: 6185-7 (2010)
Zhejiang University
Design and synthesis of KNT-127, ad-opioid receptor agonist effective by systemic administration.
Bioorg Med Chem Lett 20: 6302-5 (2010)
Kitasato University
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
Bioorg Med Chem Lett 20: 6306-9 (2010)
Stony Brook University
Inhibitors of the tyrosine kinase EphB4. Part 3: identification of non-benzodioxole-based kinase inhibitors.
Bioorg Med Chem Lett 20: 6242-5 (2010)
Astrazeneca
Discovery and optimization of a new class of potent and non-chiral indole-3-carboxamide-based renin inhibitors.
Bioorg Med Chem Lett 20: 6268-72 (2010)
Sanofi-Aventis Deutschland
Structure-based optimization and biological evaluation of human 20a-hydroxysteroid dehydrogenase (AKR1C1) salicylic acid-based inhibitors.
Eur J Med Chem 45: 5309-17 (2010)
Monash University (Parkville Campus)
Anti-AIDS agents 84. Synthesis and anti-human immunodeficiency virus (HIV) activity of 2'-monomethyl-4-methyl- and 1'-thia-4-methyl-(3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) analogs.
Bioorg Med Chem 18: 7203-11 (2010)
Fudan University
Quantitative structure-activity relationship studies of threo-methylphenidate analogs.
Bioorg Med Chem 18: 7221-38 (2010)
Institute Of Technology
New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold.
Bioorg Med Chem Lett 20: 6213-6 (2010)
University Of Lille
Discovery of a series of potent, orally activea,a-disubstituted piperidine NK(1) antagonists.
Bioorg Med Chem Lett 20: 6313-5 (2010)
Merck Research Laboratories
A FLT3-inhibitory constituent from the rhizomes of Anemarrhena asphodeloides.
J Enzyme Inhib Med Chem 26: 445-8 (2011)
Gyeongsang National University
Synthesis and biological evaluation of bivalent ligands for the cannabinoid 1 receptor.
J Med Chem 53: 7048-60 (2010)
Research Triangle Institute
Development of molecular probes for the human 5-HT(6) receptor.
J Med Chem 53: 7095-106 (2010)
Universidad Complutense De Madrid
Improvement of water-solubility of biarylcarboxylic acid peroxisome proliferator-activated receptor (PPAR)d-selective partial agonists by disruption of molecular planarity/symmetry.
Bioorg Med Chem 18: 7164-73 (2010)
The University Of Tokyo
Design, synthesis, biological evaluation, and modeling of a non-carbohydrate antagonist of the myelin-associated glycoprotein.
Bioorg Med Chem 18: 7239-51 (2010)
University Of Basel
Indole- and benzothiophene-based histamine H3 antagonists.
Bioorg Med Chem Lett 20: 6226-30 (2010)
Johnson & Johnson Pharmaceutical Research & Development
Piperidine-based renin inhibitors: upper chain optimization.
Bioorg Med Chem Lett 20: 6291-6 (2010)
Actelion Pharmaceuticals
'Click' assembly of selective inhibitors for MAO-A.
Bioorg Med Chem Lett 20: 6222-5 (2010)
Zhejiang University
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.
Bioorg Med Chem Lett 20: 6237-41 (2010)
Merck Research Laboratories
Design and optimization of new piperidines as renin inhibitors.
Bioorg Med Chem Lett 20: 6286-90 (2010)
Actelion Pharmaceuticals
Positive allosteric modulators of thea-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor.
J Med Chem 53: 7271-9 (2010)
Merck Research Laboratories
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.
J Med Chem 53: 7219-28 (2010)
Friedrich-Alexander University
Exploration of the amine terminus in a novel series of 1,2,4-triazolo-3-yl-azabicyclo[3.1.0]hexanes as selective dopamine D3 receptor antagonists.
J Med Chem 53: 7129-39 (2010)
Glaxosmithkline
Discovery of small molecule inhibitors of the PH domain leucine-rich repeat protein phosphatase (PHLPP) by chemical and virtual screening.
J Med Chem 53: 6899-911 (2010)
University Of California San Diego
An Optimized Immunoaffinity Fluorescent Method for Natural Product Target Elucidation.
J Nat Prod 73: 1659-66 (2010)
University Of California
N-phenyl-N'-[4-(5H-pyrrolo[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as novel inhibitors of VEGFR and FGFR kinases.
Bioorg Med Chem 18: 7150-63 (2010)
Takeda Pharmaceutical
Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.
Bioorg Med Chem Lett 20: 5988-93 (2010)
The Institute Of Cancer Research
Paraoxon, 4-nitrophenyl phosphate and acetate are substrates ofa- but not ofß-,¿- and¿-carbonic anhydrases.
Bioorg Med Chem Lett 20: 6208-12 (2010)
Università
Peripheral but crucial: a hydrophobic pocket (Tyr(706), Leu(337), and Met(336)) for potent and selective inhibition of neuronal nitric oxide synthase.
Bioorg Med Chem Lett 20: 6258-61 (2010)
Northwestern University
Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.
Bioorg Med Chem 18: 7260-73 (2010)
Takeda Pharmaceutical
Investigation of 4-piperidinols as novel H3 antagonists.
Bioorg Med Chem Lett 20: 6246-9 (2010)
Athersys
Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors.
Bioorg Med Chem Lett 20: 6273-6 (2010)
Bristol-Myers Squibb Research And Development
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.
Bioorg Med Chem Lett 20: 6231-6 (2010)
Elan Pharmaceuticals
Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors.
Bioorg Med Chem Lett 20: 6129-32 (2010)
Industrial Technology Research Institute
Discovery of pyrrolopyridazines as novel DGAT1 inhibitors.
Bioorg Med Chem Lett 20: 6030-3 (2010)
Amgen
Thienopyrimidines asß3-adrenoceptor agonists: hit-to-lead optimization.
Bioorg Med Chem Lett 20: 6108-15 (2010)
4Sc
Synthesis and biological evaluation of a series of aromatic bisphosphonates.
Bioorg Med Chem 18: 7212-20 (2010)
University Of Iowa
Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.
Bioorg Med Chem Lett 20: 5984-7 (2010)
Hoffmann-La Roche
Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities.
Bioorg Med Chem Lett 20: 6088-92 (2010)
Merck Research Laboratories
Validated predictive QSAR modeling of N-aryl-oxazolidinone-5-carboxamides for anti-HIV protease activity.
Bioorg Med Chem Lett 20: 6082-7 (2010)
Jadavpur University
Isoform-selective inhibition of chrysin towards human cytochrome P450 1A2. Kinetics analysis, molecular docking, and molecular dynamics simulations.
Bioorg Med Chem Lett 20: 6008-12 (2010)
Sun Yat-Sen University
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
Toxicol Sci 118: 485-500 (2010)
Amgen
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
Bioorg Med Chem Lett 20: 6020-3 (2010)
Roche R&D Center China
Synthesis, antioxidant activities and urease inhibition of some new 1,2,4-triazole and 1,3,4-thiadiazole derivatives.
Eur J Med Chem 45: 5200-7 (2010)
Quaid-I-Azam University
Characterization of Acetylcholinesterase Inhibitory Constituents from Annona glabra Assisted by HPLC Microfractionation.
J Nat Prod 73: 1632-5 (2010)
National Taiwan University
Expanding the diversity of allosteric bcr-abl inhibitors.
J Med Chem 53: 6934-46 (2010)
Harvard Medical School
Surface plasmon resonance biosensor based fragment screening using acetylcholine binding protein identifies ligand efficiency hot spots (LE hot spots) by deconstruction of nicotinic acetylcholine receptora7 ligands.
J Med Chem 53: 7192-201 (2010)
Vu University Amsterdam
A novel competitive class of α-glucosidase inhibitors: (E)-1-phenyl-3-(4-styrylphenyl)urea derivatives.
Chembiochem 11: 2125-31 (2010)
Gyeongsang National University
20-Aminosteroids as a novel class of selective and complete androgen receptor antagonists and inhibitors of prostate cancer cell growth.
Bioorg Med Chem 18: 6960-9 (2010)
UniversitäT Leipzig
Design, synthesis, and binding of homologated truncated 4'-thioadenosine derivatives at the human A3 adenosine receptors.
Bioorg Med Chem 18: 7015-21 (2010)
Ewha Womans University
Synthesis and biological activity of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines as phosphodiesterase type 4 inhibitors.
J Med Chem 53: 6912-22 (2010)
RhôNe-Poulenc Rorer
Optimised expression and spectral analysis of the target enzyme CYP51 from Penicillium digitatum with possible new DMI fungicides.
Pest Manag Sci 66: 1344-50 (2010)
Central China Normal University
Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
Antimicrob Agents Chemother 54: 4611-8 (2010)
Boehringer Ingelheim (Canada)
OGA inhibition by GlcNAc-selenazoline.
Bioorg Med Chem 18: 7058-64 (2010)
Daegu University
A stereo-controlled synthesis of 2,4-dimethyl-4-hydroxy-16-phenylhexadecanoic acid 1,4-lactone and its PPAR activities.
Bioorg Med Chem Lett 20: 6017-9 (2010)
Seoul National University
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.
Bioorg Med Chem Lett 20: 6048-51 (2010)
Genentech
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.
Bioorg Med Chem Lett 20: 6034-9 (2010)
Elan Pharmaceuticals
Structural basis for binding of cyclic 2-oxoglutarate analogues to factor-inhibiting hypoxia-inducible factor.
Bioorg Med Chem Lett 20: 6125-8 (2010)
University Of Oxford
Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (Sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) asa4ß2-nicotinic acetylcholine receptor-selective partial agonists.
J Med Chem 53: 6973-85 (2010)
University Of Illinois At Chicago
Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents.
J Med Chem 53: 6867-88 (2010)
Yale University
Insights from selective non-phosphinic inhibitors of MMP-12 tailored to fit with an S1' loop canonical conformation.
J Biol Chem 285: 35900-9 (2010)
Commissariat À
Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.
Bioorg Med Chem 18: 6977-86 (2010)
Novartis Institutes For Biomedical Research
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.
Bioorg Med Chem Lett 20: 6067-71 (2010)
Abbott Laboratories
A novel series of positive modulators of the AMPA receptor: structure-based lead optimization.
Bioorg Med Chem Lett 20: 6072-5 (2010)
Merck Research Laboratories
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.
Bioorg Med Chem Lett 20: 6064-6 (2010)
Kyoto University
Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease.
Bioorg Med Chem Lett 20: 6093-5 (2010)
Charles University
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.
Bioorg Med Chem 18: 7113-20 (2010)
Nerviano Medical Sciences Oncology
Fatty acid synthase inhibitors of phenolic constituents isolated from Garcinia mangostana.
Bioorg Med Chem Lett 20: 6045-7 (2010)
Chinese Academy Of Sciences
4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors.
Bioorg Med Chem Lett 20: 6096-9 (2010)
Pfizer
Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase.
Eur J Med Chem 45: 5140-9 (2010)
Instituto De ParasitologíA Y Biomedicina LóPez-Neyra
Synthesis and characterization of a iodine-125-labeled pyrrolo[1,2-a]thieno[3,2-e]pyrazine and evaluation as a potential 5-HT4R SPECT tracer.
Eur J Med Chem 45: 5465-7 (2010)
Universit£
Spiroindolones, a potent compound class for the treatment of malaria.
Science 329: 1175-80 (2010)
Swiss Tropical And Public Health Institute
Synthesis, anti-fungal and 1,3-ß-D-glucan synthase inhibitory activities of caffeic and quinic acid derivatives.
Bioorg Med Chem 18: 7009-14 (2010)
Inner Mongolia University
Search for influence of spatial properties on affinity ata1-adrenoceptor subtypes for phenylpiperazine derivatives of phenytoin.
Bioorg Med Chem Lett 20: 6152-6 (2010)
Jagiellonian University Medical College
Synthesis and biological evaluation of a novel series of bis-salicylaldehydes as mushroom tyrosinase inhibitors.
Bioorg Med Chem Lett 20: 6138-40 (2010)
Universit£
Discovery and structure-activity relationship of a novel spirocarbamate series of NPY Y5 antagonists.
Bioorg Med Chem Lett 20: 6103-7 (2010)
Glaxosmithkline
Elucidation of the active conformation of the amino terminus of receptor-bound secretin using intramolecular disulfide bond constraints.
Bioorg Med Chem Lett 20: 6040-4 (2010)
Mayo Clinic
Homology modeling and molecular dynamics of CYP1A1 and CYP2B1 to explore the metabolism of aryl derivatives by docking and experimental assays.
Eur J Med Chem 45: 4845-55 (2010)
Instituto PolitéCnico Nacional
Identification of selective norbornane-type aspartate analogue inhibitors of the glutamate transporter 1 (GLT-1) from the chemical universe generated database (GDB).
J Med Chem 53: 7236-50 (2010)
University Of Berne
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.
J Med Chem 53: 7035-47 (2010)
National Institute Of Mental Health
1-Aryl-3-(1-acylpiperidin-4-yl)urea inhibitors of human and murine soluble epoxide hydrolase: structure-activity relationships, pharmacokinetics, and reduction of inflammatory pain.
J Med Chem 53: 7067-75 (2010)
Department Of Entomology And University Of California Davis Cancer Center
Synthesis and biochemical characterization of a series of 17a-perfluoroalkylated estradiols as selective ligands for estrogen receptora.
J Med Chem 53: 6947-53 (2010)
Charles University In Prague
Discovery of pyrrolopyrimidine inhibitors of Akt.
Bioorg Med Chem Lett 20: 5607-12 (2010)
Array Biopharma
Synthesis and evaluation of indole, pyrazole, chromone and pyrimidine based conjugates for tumor growth inhibitory activities--development of highly efficacious cytotoxic agents.
Eur J Med Chem 45: 4968-82 (2010)
Guru Nanak Dev University
Click-chemistry-derived triazole ligands of arginine-glycine-aspartate (RGD) integrins with a broad capacity to inhibit adhesion of melanoma cells and both in vitro and in vivo angiogenesis.
J Med Chem 53: 7119-28 (2010)
University Of Florence
Amino derivatives of indole as potent inhibitors of isoprenylcysteine carboxyl methyltransferase.
J Med Chem 53: 6838-50 (2010)
National University Of Singapore
Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5.
J Med Chem 53: 7107-18 (2010)
Sepracor
Rigid analogues of thea2-adrenergic blocker atipamezole: small changes, big consequences.
J Med Chem 53: 6986-95 (2010)
Pierre Fabre Research Center
Identification of an endothelin-converting enzyme-2-specific fluorigenic substrate and development of an in vitro and ex vivo enzymatic assay.
J Biol Chem 285: 34390-400 (2010)
Pharmaleads
Hyperbolic mixed-type inhibition of acetylcholinesterase by tetracyclic thienopyrimidines.
J Enzyme Inhib Med Chem 26: 350-8 (2011)
University Of Bonn
Analogues of morphanthridine and the tear gas dibenz[b,f][1,4]oxazepine (CR) as extremely potent activators of the human transient receptor potential ankyrin 1 (TRPA1) channel.
J Med Chem 53: 7011-20 (2010)
Johnson & Johnson Pharmaceutical Research & Development
Topsentinols, 24-isopropyl steroids from the marine sponge Topsentia sp.
J Nat Prod 73: 1597-600 (2010)
University Of Hawaii At Manoa
Bioactivity-guided isolation of 1,2,3,4,6-Penta-O-galloyl-D-glucopyranose from Paeonia lactiflora roots as a PTP1B inhibitor.
J Nat Prod 73: 1578-81 (2010)
University Of Vienna
6,7-Dihydroxy-4-phenylcoumarin as inhibitor of aldose reductase 2.
Bioorg Med Chem Lett 20: 5630-3 (2010)
University Of Toyama
Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.
Biochemistry 49: 8488-98 (2010)
Pfizer
Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophore.
J Med Chem 53: 7902-17 (2010)
Duquesne University
Inhalation by design: novel ultra-long-actingß(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
J Med Chem 53: 6640-52 (2010)
Pfizer
Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38a MAP kinase inhibitor for the treatment of inflammatory diseases.
J Med Chem 53: 6629-39 (2010)
Bristol-Myers Squibb Research And Development
Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(aryloyl)phenyl methyl sulfones.
J Med Chem 53: 6560-71 (2010)
Universitat De Barcelona
Delphinidin, a dietary anthocyanidin in berry fruits, inhibits human glyoxalase I.
Bioorg Med Chem 18: 7029-33 (2010)
Tokyo University Of Science
Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novela1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, anda1d computational study.
Bioorg Med Chem 18: 7065-77 (2010)
Universit£
Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators.
Bioorg Med Chem Lett 20: 5617-22 (2010)
Vanderbilt University Medical Center
6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics.
Bioorg Med Chem Lett 20: 5666-9 (2010)
Pfizer
The synthesis, structure and activity evaluation of pyrogallol and catechol derivatives as Helicobacter pylori urease inhibitors.
Eur J Med Chem 45: 5064-70 (2010)
Jishou University
Synthesis and evaluation of novel stearoyl-CoA desaturase 1 inhibitors: 1'-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-3,4-dihydrospiro[chromene-2,4'-piperidine] analogs.
Eur J Med Chem 45: 4788-96 (2010)
Daiichi Sankyo
Synthesis, characterization, oxidative degradation, antibacterial activity and acetylcholinesterase/butyrylcholinesterase inhibitory effects of some new phosphorus(V) hydrazides.
Eur J Med Chem 45: 5130-9 (2010)
Tarbiat Modares University
Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI.
Bioorg Med Chem 18: 7085-91 (2010)
Universit£
9-Dihydroerythromycins as non-antibiotic motilin receptor agonists.
Bioorg Med Chem Lett 20: 5658-61 (2010)
Kosan Biosciences
Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.
Bioorg Med Chem Lett 20: 5718-21 (2010)
Kalypsys
Synthesis and biological evaluation of C-2 halogenated analogs of salvinorin A.
Bioorg Med Chem Lett 20: 5749-52 (2010)
Harvard Medical School
Probing the active-site requirements of human intestinal N-terminal maltase glucoamylase: the effect of replacing the sulfate moiety by a methyl ether in ponkoranol, a naturally occurringa-glucosidase inhibitor.
Bioorg Med Chem Lett 20: 5686-9 (2010)
Simon Fraser University
Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase.
Bioorg Med Chem Lett 20: 5781-6 (2010)
Mcgill University
Discovery of potent and selective histamine H3 receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold.
Bioorg Med Chem Lett 20: 5713-7 (2010)
F. Hoffmann-La Roche
Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.
Bioorg Med Chem Lett 20: 5690-4 (2010)
Niddk
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.
Bioorg Med Chem Lett 20: 5874-8 (2010)
Neurocrine Biosciences
Novel indoline-1- or 3,4-dihydroquinoline-1(2H)-substituted carbothiohydrazides as TPO receptor agonists.
Bioorg Med Chem Lett 20: 5670-2 (2010)
Shanghai Hengrui Pharmaceuticals
Synthesis and biological evaluation of novel coumarin-based inhibitors of Cdc25 phosphatases.
Bioorg Med Chem Lett 20: 5827-30 (2010)
Université
Synthesis and molecular docking study of novel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential antitumor agents.
Bioorg Med Chem Lett 20: 5705-8 (2010)
Anhui University Of Technology
Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region.
Bioorg Med Chem Lett 20: 5793-8 (2010)
Deciphera Pharmaceuticals
Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors.
Eur J Med Chem 45: 4953-62 (2010)
East China University Of Science And Technology
Development of a new epidermal growth factor receptor positron emission tomography imaging agent based on the 3-cyanoquinoline core: synthesis and biological evaluation.
Bioorg Med Chem 18: 6634-45 (2010)
Imperial College
Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line.
Bioorg Med Chem Lett 20: 5722-5 (2010)
Institute Of Science And Technology
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.
Bioorg Med Chem Lett 20: 5869-73 (2010)
Pfizer
Application of fragment-based drug discovery to membrane proteins: identification of ligands of the integral membrane enzyme DsbB.
Chem Biol 17: 881-91 (2010)
Leiden University
Functional studies of Plasmodium falciparum dipeptidyl aminopeptidase I using small molecule inhibitors and active site probes.
Chem Biol 17: 808-19 (2010)
Stanford School Of Medicine
Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers.
J Med Chem 53: 6773-7 (2010)
Laboratory Of Design, Synthesis, And Study Of Biologically Active Heterocycles (Heterobiolab)
Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor.
J Med Chem 53: 6706-19 (2010)
Vanderbilt University Medical Center
Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics.
J Med Chem 53: 6681-98 (2010)
Boehringer Ingelheim Pharmaceuticals
Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38a MAP kinase inhibitors.
Bioorg Med Chem Lett 20: 5864-8 (2010)
Bristol-Myers Squibb Pharmaceutical Research Institute
3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators.
Bioorg Med Chem Lett 20: 5922-4 (2010)
Vanderbilt University
Direct renin inhibitors as a new therapy for hypertension.
J Med Chem 53: 7490-520 (2010)
Novartis Pharmaceuticals
Potent and fully noncompetitive peptidomimetic inhibitor of multidrug resistance P-glycoprotein.
J Med Chem 53: 6720-9 (2010)
Umr 5086 Cnrs
A focused library of protein tyrosine phosphatase inhibitors.
J Med Chem 53: 6768-72 (2010)
Brown University
Small-molecule inhibitors of NADPH oxidase 4.
J Med Chem 53: 6758-62 (2010)
Vichem Chemie Research
Design and synthesis of biphenyl derivatives as mushroom tyrosinase inhibitors.
Bioorg Med Chem 18: 6708-14 (2010)
Jinan University
Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor.
Bioorg Med Chem Lett 20: 5925-32 (2010)
Merck Research Laboratories
QSAR prediction of D2 receptor antagonistic activity of 6-methoxy benzamides.
Eur J Med Chem 45: 4856-62 (2010)
University Of Mazandaran
Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles.
Bioorg Med Chem 18: 6865-73 (2010)
Clermont Université
Replacement of the Lys linker with an Arg linker resulting in improved melanoma uptake and reduced renal uptake of Tc-99m-labeled Arg-Gly-Asp-conjugated alpha-melanocyte stimulating hormone hybrid peptide.
Bioorg Med Chem 18: 6695-700 (2010)
University Of New Mexico
Optimization of N-benzyl-benzoxazol-2-ones as receptor antagonists of macrophage migration inhibitory factor (MIF).
Bioorg Med Chem Lett 20: 5811-4 (2010)
Yale University
The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part III: the three microdose candidates.
Bioorg Med Chem Lett 20: 7164-8 (2010)
Pfizer
Identification and optimization of substituted 5-aminopyrazoles as potent and selective adenosine A1 receptor antagonists.
Bioorg Med Chem Lett 20: 5891-4 (2010)
Bayer Schering Pharma
Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers.
Bioorg Med Chem Lett 20: 5879-82 (2010)
Johann Wolfgang Goethe University
Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors.
Bioorg Med Chem Lett 20: 5807-10 (2010)
Institute Of Microbial Chemistry
CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist.
Bioorg Med Chem Lett 20: 5853-8 (2010)
Tokyo Medical And Dental University
Identification of a new biaryl scaffold generating potent renin inhibitors.
Bioorg Med Chem Lett 20: 5822-6 (2010)
Merck Frosst Center For Therapeutic Research
3D-QSAR pharmacophore modeling and in silico screening of new Bcl-xl inhibitors.
Eur J Med Chem 45: 4774-82 (2010)
Universit£
Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2: azoles: effective metal chelators.
Bioorg Med Chem Lett 20: 5909-12 (2010)
Avexa
Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1.
Bioorg Med Chem Lett 20: 5847-52 (2010)
Astrazeneca Pharmaceuticals
Synthesis and biological evaluation of indomethacin analogs possessing a N-difluoromethyl-1,2-dihydropyrid-2-one ring system: a search for novel cyclooxygenase and lipoxygenase inhibitors.
Bioorg Med Chem Lett 20: 5776-80 (2010)
University Of Alberta
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO).
Bioorg Med Chem Lett 20: 5799-802 (2010)
University Of Sydney
Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: selection of the scaffold.
Bioorg Med Chem Lett 20: 5913-7 (2010)
Avexa
Discovery of a class of calcium sensing receptor positive allosteric modulators; 1-(benzothiazol-2-yl)-1-phenylethanols.
Bioorg Med Chem Lett 20: 5918-21 (2010)
Acadia Pharmaceuticals
Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.
Bioorg Med Chem Lett 20: 5883-6 (2010)
Johann Wolfgang Goethe University
Discovery of quinolines as selective glucocorticoid receptor agonists.
Bioorg Med Chem Lett 20: 5835-8 (2010)
Bayer Schering Pharma
Orally active MMP-1 sparinga-tetrahydropyranyl anda-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
J Med Chem 53: 6653-80 (2010)
Pfizer
Studies on ligand binding to histidine triad nucleotide binding protein 1.
Bioorg Med Chem 18: 6756-62 (2010)
University Of Maryland
Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists.
Bioorg Med Chem Lett 20: 5443-8 (2010)
Dr. Reddy'S Laboratories
Prenylflavonoids from Glycyrrhiza uralensis and their protein tyrosine phosphatase-1B inhibitory activities.
Bioorg Med Chem Lett 20: 5398-401 (2010)
Toho University
Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.
Bioorg Med Chem Lett 20: 5567-71 (2010)
Korea Institute Of Science And Technology
Iminoheterocycles as gamma-secretase modulators.
Bioorg Med Chem Lett 20: 5380-4 (2010)
Merck Research Laboratories
Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity.
Bioorg Med Chem Lett 20: 5426-30 (2010)
F. Hoffmann-La Roche
Computational analysis of ligand recognition sites of homo- and heteropentameric 5-HT3 receptors.
Eur J Med Chem 45: 4746-60 (2010)
University Of Modena And Reggio Emilia
Synthesis, characterization and antiglaucoma activity of some novel pyrazole derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide.
Eur J Med Chem 45: 4769-73 (2010)
Dumlupinar University
Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.
J Med Chem 53: 6618-28 (2010)
Spanish National Cancer Research Centre (Cnio)
Identification and hit-to-lead optimization of a novel class of CB1 antagonists.
Bioorg Med Chem Lett 20: 5449-53 (2010)
Ligand Pharmaceuticals
SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.
Bioorg Med Chem Lett 20: 5405-10 (2010)
Astrazeneca Pharmaceuticals
Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists.
Bioorg Med Chem Lett 20: 5394-7 (2010)
Ligand Pharmaceuticals
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.
Bioorg Med Chem Lett 20: 5431-3 (2010)
University Of Copenhagen
Discovery of 2-[1-(4-chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury.
J Med Chem 53: 6003-17 (2010)
Pfizer
Fragment-based drug discovery applied to Hsp90. Discovery of two lead series with high ligand efficiency.
J Med Chem 53: 5942-55 (2010)
Astex Therapeutics
Investigations on the 4-quinolone-3-carboxylic acid motif. 3. Synthesis, structure-affinity relationships, and pharmacological characterization of 6-substituted 4-quinolone-3-carboxamides as highly selective cannabinoid-2 receptor ligands.
J Med Chem 53: 5915-28 (2010)
Universit£
Novel benzimidazole inhibitors bind to a unique site in the kinesin spindle protein motor domain.
Biochemistry 49: 8350-8 (2010)
Merck Research Laboratories
Design and synthesis of potent"sulfur-free" transition state analogue inhibitors of 5'-methylthioadenosine nucleosidase and 5'-methylthioadenosine phosphorylase.
J Med Chem 53: 6730-46 (2010)
Industrial Research
Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
J Med Chem 53: 6572-83 (2010)
National Health Research Institutes
FRET-based sensors for the human M1-, M3-, and M5-acetylcholine receptors.
Bioorg Med Chem 19: 1048-54 (2011)
University Of Wuerzburg
Identification of small molecule compounds with higher binding affinity to guanine deaminase (cypin) than guanine.
Bioorg Med Chem 18: 6748-55 (2010)
The State University Of New Jersey
Synthesis, stereochemical separation, and biological evaluation of selective inhibitors of human MAO-B: 1-(4-arylthiazol-2-yl)-2-(3-methylcyclohexylidene)hydrazines.
J Med Chem 53: 6516-20 (2010)
Sapienza University Of Rome
Discovery of pyridazinopyridinones as potent and selective p38 mitogen-activated protein kinase inhibitors.
J Med Chem 53: 6398-411 (2010)
Amgen
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery.
Nat Chem Biol 6: 660-6 (2010)
Novartis Institutes For Biomedical Research
Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists.
Bioorg Med Chem 18: 6763-70 (2010)
Purdue University
The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part 2: the second clinical candidate having a shorter and favorable human half-life.
Bioorg Med Chem Lett 20: 7159-63 (2010)
Pfizer
Substituted biaryl oxazoles, imidazoles, and thiazoles as sodium channel blockers.
Bioorg Med Chem Lett 20: 5536-40 (2010)
Merck Research Laboratories
The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists.
Bioorg Med Chem Lett 20: 5434-8 (2010)
Glaxosmithkline
The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors.
Bioorg Med Chem Lett 20: 5502-5 (2010)
Merck Frosst Centre For Therapeutic Research
Substituted biaryl pyrazoles as sodium channel blockers.
Bioorg Med Chem Lett 20: 5480-3 (2010)
Merck Research Laboratories
Synthesis of polyhydroxylated aromatics having amidation of piperazine nitrogen as HIV-1 integrase inhibitor.
Bioorg Med Chem Lett 20: 5469-71 (2010)
Beijing University Of Technology
Rose Bengal analogs and vesicular glutamate transporters (VGLUTs).
Bioorg Med Chem 18: 6922-33 (2010)
University Of Paris
Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells.
Bioorg Med Chem 18: 6785-95 (2010)
University Of Rostock
Synthesis and evaluation of amides surrogates of dopamine D3 receptor ligands.
Bioorg Med Chem Lett 20: 5376-9 (2010)
Université
The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core.
Bioorg Med Chem Lett 20: 5544-7 (2010)
Amgen
Novel pyrrolidine heterocycles as CCR1 antagonists.
Bioorg Med Chem Lett 20: 5477-9 (2010)
Ligand Pharmaceuticals
1,2,3-triazole analogs of combretastatin A-4 as potential microtubule-binding agents.
Bioorg Med Chem 18: 6874-85 (2010)
University Of Oslo
Peptidic HIV integrase inhibitors derived from HIV gene products: structure-activity relationship studies.
Bioorg Med Chem 18: 6771-5 (2010)
Tokyo Medical And Dental University
Synthesis of new series of quinoxaline based MAO-inhibitors and docking studies.
Eur J Med Chem 45: 4479-89 (2010)
Alexandria University
Synthesis and biological activity of N-substituted aminocarbonyl-1,3-dioxolanes as VLA-4 antagonists.
Bioorg Med Chem Lett 20: 5514-20 (2010)
New Drug Discovery Research
p-Trifluoromethyldiazirinyl-etomidate: a potent photoreactive general anesthetic derivative of etomidate that is selective for ligand-gated cationic ion channels.
J Med Chem 53: 6432-44 (2010)
Massachusetts General Hospital
Synthesis of new 3-aryl-4,5-dihydropyrazole-1-carbothioamide derivatives. An investigation on their ability to inhibit monoamine oxidase.
Eur J Med Chem 45: 4490-8 (2010)
Dipartimento Farmaco Chimico Tecnologico
Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein.
Biochemistry 49: 8143-54 (2010)
Beactica
Identification and development of novel inhibitors of Toxoplasma gondii enoyl reductase.
J Med Chem 53: 6287-300 (2010)
University Of Illinois At Chicago
Affinity of ceftobiprole for penicillin-binding protein 2b in Streptococcus pneumoniae strains with various susceptibilities to penicillin.
Antimicrob Agents Chemother 54: 4510-2 (2010)
Johnson & Johnson Pharmaceutical Research & Development
Xanthones with neuraminidase inhibitory activity from the seedcases of Garcinia mangostana.
Bioorg Med Chem 18: 6258-64 (2010)
Graduate School Of Gyeongsang National University
Selective inhibition of methoxyflavonoids on human CYP1B1 activity.
Bioorg Med Chem 18: 6310-5 (2010)
University Of Shizuoka
Identification of a naturally occurring rexinoid, honokiol, that activates the retinoid X receptor.
J Nat Prod 73: 1332-6 (2010)
Aichi Gakuin University
[3-azabicyclo[3.1.0]hex-1-yl]phenyl-benzenesulfonamides as selective dopamine D3 antagonists.
Bioorg Med Chem Lett 20: 5491-4 (2010)
Glaxosmithkline
N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B.
Bioorg Med Chem Lett 20: 5488-90 (2010)
Csiro Molecular And Health Technologies
Identification of a novel NR2B-selective NMDA receptor antagonist using a virtual screening approach.
Bioorg Med Chem Lett 20: 5552-8 (2010)
Universit£
Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.
Bioorg Med Chem Lett 20: 5541-3 (2010)
University Of WüRzburg
Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2.
Eur J Med Chem 45: 4594-600 (2010)
Sapienza University Of Rome
Synthesis, biological evaluation, and docking studies of novel heterocyclic diaryl compounds as selective COX-2 inhibitors.
Bioorg Med Chem 18: 6367-76 (2010)
Gazi University
Design, synthesis, and biological evaluation of new monoamine reuptake inhibitors with potential therapeutic utility in depression and pain.
Bioorg Med Chem Lett 20: 5559-66 (2010)
Roche Palo Alto
Three-dimensional quantitative structure-activity relationship CoMSIA/CoMFA and LeapFrog studies on novel series of bicyclo [4.1.0] heptanes derivatives as melanin-concentrating hormone receptor R1 antagonists.
Eur J Med Chem 45: 4509-22 (2010)
Universidad De Cartagena
QSAR study of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2 using LS-SVM and GRNN based on principal components.
Eur J Med Chem 45: 4499-508 (2010)
Kermanshah University Of Medical Sciences
Design, synthesis and biological evaluation of new (E)- and (Z)-1,2,3-triaryl-2-propen-1-ones as selective COX-2 inhibitors.
Eur J Med Chem 45: 4013-7 (2010)
Shahid Beheshti University Of Medical Sciences
Synthesis, in vitro activity, and three-dimensional quantitative structure-activity relationship of novel hydrazine inhibitors of human vascular adhesion protein-1.
J Med Chem 53: 6301-15 (2010)
Fi-40014 University Of Jyvaskyla
Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors.
J Med Chem 53: 6326-36 (2010)
Georgia Institute Of Technology
Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain.
J Med Chem 53: 6445-56 (2010)
Meiji Seika Kaisha
Discovery of canagliflozin, a novel C-glucoside with thiophene ring, as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitus.
J Med Chem 53: 6355-60 (2010)
Mitsubishi Tanabe Pharma
N(G)-Acyl-argininamides as NPY Y(1) receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity.
Bioorg Med Chem 18: 6292-304 (2010)
UniversitäT Regensburg
Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists.
Bioorg Med Chem Lett 20: 4992-8 (2010)
Abbott Healthcare Products
S-benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase.
Bioorg Med Chem Lett 20: 5126-9 (2010)
University Of Shizuoka
Development of potent glucagon-like peptide-1 agonists with high enzyme stability via introduction of multiple lactam bridges.
J Med Chem 53: 6412-20 (2010)
University Of Texas At Dallas
Antiviral agents 2. Synthesis of trimeric naphthoquinone analogues of conocurvone and their antiviral evaluation against HIV.
Bioorg Med Chem 18: 6442-50 (2010)
Monash University (Parkville Campus)
Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.
Bioorg Med Chem Lett 20: 5035-8 (2010)
Kitasato University
Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists).
Bioorg Med Chem Lett 20: 5161-4 (2010)
Novartis Institutes For Biomedical Research
The synthesis and structure-activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H3 antagonists.
Bioorg Med Chem Lett 20: 5004-8 (2010)
Merck Research Laboratories
Homology modeling and atomic level binding study of GABA(A) receptor with novel enaminone amides.
Eur J Med Chem 45: 3595-600 (2010)
Wuhan Institute Of Technology
Synthesis and resolution of cis-(+/-)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl)cyclopropanecarboxylate [(+/-)-PPCC)]: new sigma receptor ligands with neuroprotective effect.
J Med Chem 53: 5881-5 (2010)
University Of Catania
Design of potent inhibitors of human RAD51 recombinase based on BRC motifs of BRCA2 protein: modeling and experimental validation of a chimera peptide.
J Med Chem 53: 5782-91 (2010)
Centre National De La Recherche Scientifique & Universite De Nantes
Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.
J Med Chem 53: 5749-58 (2010)
Saarland University
Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.
J Med Chem 53: 5727-37 (2010)
The Scripps Research Institute
Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia.
J Med Chem 53: 5696-706 (2010)
Arena Pharmaceuticals
Crystal structure-based selective targeting of the pyridoxal 5'-phosphate dependent enzyme kynurenine aminotransferase II for cognitive enhancement.
J Med Chem 53: 5684-9 (2010)
University Of Piemonte Orientale Amedeo Avogadro
Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors.
J Med Chem 53: 5629-38 (2010)
Nagoya City University
Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.
J Med Chem 53: 5620-8 (2010)
Bristol-Myers Squibb
An efficient approach to the discovery of potent inhibitors against glycosyltransferases.
J Med Chem 53: 5607-19 (2010)
Hokkaido University
Biological diversity from a structurally diverse library: systematically scanning conformational space using a pyranose scaffold.
J Med Chem 53: 5576-86 (2010)
Alchemia
Development and characterization of new inhibitors of the human and mouse hematopoietic prostaglandin D(2) synthases.
J Med Chem 53: 5536-48 (2010)
The University Of Queensland
Identification of the first low-molecular-weight inhibitors of matriptase-2.
J Med Chem 53: 5523-35 (2010)
University Of Bonn
A novel water-soluble gossypol derivative increases chemotherapeutic sensitivity and promotes growth inhibition in colon cancer.
J Med Chem 53: 5502-10 (2010)
Institute Of Health Sciences
Quinazolin-4-one derivatives: A novel class of noncompetitive NR2C/D subunit-selective N-methyl-D-aspartate receptor antagonists.
J Med Chem 53: 5476-90 (2010)
Emory University
Phenylsulfonylfuroxans as modulators of multidrug-resistance-associated protein-1 and P-glycoprotein.
J Med Chem 53: 5467-75 (2010)
Universita Degli Studi Di Torino
Identification of potent and selective amidobipyridyl inhibitors of protein kinase D.
J Med Chem 53: 5422-38 (2010)
Novartis Institutes For Biomedical Research
Identification of orally available naphthyridine protein kinase D inhibitors.
J Med Chem 53: 5400-21 (2010)
Novartis Institutes For Biomedical Research
Novel carbamates as orally active acetylcholinesterase inhibitors found to improve scopolamine-induced cognition impairment: pharmacophore-based virtual screening, synthesis, and pharmacology.
J Med Chem 53: 6490-505 (2010)
Central Drug Research Institute
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
J Med Chem 53: 6386-97 (2010)
H. Lundbeck
Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
J Med Chem 53: 6361-7 (2010)
University Of Michigan
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.
J Med Chem 53: 6368-77 (2010)
Amgen
Identification of novel inhibitors of 1-aminocyclopropane-1-carboxylic acid synthase by chemical screening in Arabidopsis thaliana.
J Biol Chem 285: 33445-56 (2010)
National Defense Medical Center
Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities.
J Med Chem 53: 6089-99 (2010)
Hokkaido University
Discovery of pyrrole-indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile.
J Med Chem 53: 5929-41 (2010)
Development Center For Biotechnology
Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 2, optimization for blood pressure reduction in spontaneously hypertensive rats.
Bioorg Med Chem Lett 20: 5153-6 (2010)
Boehringer Ingelheim Pharmaceuticals
Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase.
Bioorg Med Chem Lett 20: 5027-30 (2010)
Bristol-Myers Squibb Research And Development
Synthesis and biological evaluation of oxoindolin-3-ylidene ethyl benzothiohydrazides as non-peptide TPO mimics.
Bioorg Med Chem Lett 20: 5062-4 (2010)
Shanghai Hengrui Pharmaceuticals
Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.
Bioorg Med Chem Lett 20: 5113-8 (2010)
Daiichi Sankyo
SAR studies of non-zinc-chelating MMP-13 inhibitors: improving selectivity and metabolic stability.
Bioorg Med Chem Lett 20: 5039-43 (2010)
Boehringer Ingelheim Pharmaceuticals
Synthesis and biochemical evaluation of a range of (4-substituted phenyl)sulfonate derivatives of 4-hydroxybenzyl imidazole-based compounds as potent inhibitors of 17alpha-hydroxylase/17,20-lyase (P45017alpha) derived from rat testicular microsomes.
Bioorg Med Chem Lett 20: 5345-8 (2010)
University Of The West Of Scotland
Design, synthesis, and pharmacological effects of structurally simple ligands for MT(1) and MT(2) melatonin receptors.
Bioorg Med Chem 18: 6496-511 (2010)
Universit£
New effective inhibitors of the Abelson kinase.
Bioorg Med Chem 18: 6316-21 (2010)
Iowa State University
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents.
Bioorg Med Chem Lett 20: 5334-6 (2010)
Chinese Academy Of Sciences
Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.
Bioorg Med Chem Lett 20: 5069-73 (2010)
Glaxosmithkline
Synthesis of selenophene derivatives as novel CHK1 inhibitors.
Bioorg Med Chem Lett 20: 5065-8 (2010)
Development Center For Biotechnology
Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists.
Bioorg Med Chem Lett 20: 5044-9 (2010)
Glaxosmithkline
Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV.
Bioorg Med Chem Lett 20: 5050-3 (2010)
Universit£
Inhibition of interleukin-1beta converting enzyme (ICE or caspase 1) by aspartyl acyloxyalkyl ketones and aspartyl amidooxyalkyl ketones.
Bioorg Med Chem Lett 20: 5089-94 (2010)
Pfizer
Development of 2-pyrrolidinyl-N-methyl pyrimidones as potent and orally bioavailable HIV integrase inhibitors.
Bioorg Med Chem Lett 20: 5031-4 (2010)
Irbm-Mrl
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Bioorg Med Chem Lett 20: 5170-4 (2010)
Merck Research Laboratories
Inhibition of monoamine oxidase by indole and benzofuran derivatives.
Eur J Med Chem 45: 4458-66 (2010)
North-West University
Discovery of 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-1H-pyrazol-3-yl)-5-tert-butyl-1,3,4-thiadiazole (GCC2680) as a potent, selective and orally efficacious cannabinoid-1 receptor antagonist.
Bioorg Med Chem 18: 6377-88 (2010)
Green Cross
Discovery of achiral inhibitors of the hepatitis C virus NS3 protease based on 2(1H)-pyrazinones.
Bioorg Med Chem 18: 6512-25 (2010)
Uppsala University
Design, synthesis and anticholinesterase activity of a novel series of 1-benzyl-4-((6-alkoxy-3-oxobenzofuran-2(3H)-ylidene) methyl) pyridinium derivatives.
Bioorg Med Chem 18: 6360-6 (2010)
Tehran University Of Medical Sciences
Structure-based design, synthesis, and biological evaluation of lipophilic-tailed monocationic inhibitors of neuronal nitric oxide synthase.
Bioorg Med Chem 18: 6526-37 (2010)
Northwestern University
Addressing time-dependent CYP 3A4 inhibition observed in a novel series of substituted amino propanamide renin inhibitors, a case study.
Bioorg Med Chem Lett 20: 5074-9 (2010)
Merck Frosst Centre For Therapeutic Research
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
Bioorg Med Chem Lett 20: 5080-4 (2010)
Glaxosmithkline
Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration.
Bioorg Med Chem Lett 20: 5133-8 (2010)
Astrazeneca R&D Boston
Structure-activity relationships for a novel series of citalopram (1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile) analogues at monoamine transporters.
J Med Chem 53: 6112-21 (2010)
National Institute On Drug Abuse-Intramural Research Program
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.
J Med Chem 53: 5979-6002 (2010)
Pfizer
Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists.
J Med Chem 53: 5970-8 (2010)
Pfizer
Comparison of the activity of non-steroidal ecdysone agonists between dipteran and lepidopteran insects, using cell-based EcR reporter assays.
Pest Manag Sci 66: 1215-29 (2010)
Ghent University
Effects of 7-O substitutions on estrogenic and anti-estrogenic activities of daidzein analogues in MCF-7 breast cancer cells.
J Med Chem 53: 6153-63 (2010)
Xavier University Of Louisiana
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
J Med Chem 53: 6100-11 (2010)
Georgia Institute Of Technology
Medicinal chemistry as a conduit for the modulation of quorum sensing.
J Med Chem 53: 7467-89 (2010)
The Scripps Research Institute
NMR spectroscopy and computational analysis of interaction between Serratia marcescens chitinase B and a dipeptide derived from natural-product cyclopentapeptide chitinase inhibitor argifin.
Bioorg Med Chem 18: 5835-44 (2010)
Kitasato University
Design, synthesis, and biological evaluation of prenylated chalcones as 5-LOX inhibitors.
Bioorg Med Chem 18: 5807-15 (2010)
University Of Hyderabad
Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.
Bioorg Med Chem 18: 6934-52 (2010)
The Institute Of Cancer Research
Synthesis of a series of novel 2,4,5-trisubstituted selenazole compounds as potential PLTP inhibitors.
Bioorg Med Chem Lett 20: 5123-5 (2010)
Beijing Institute Of Pharmacology And Toxicology
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).
Bioorg Med Chem Lett 20: 5175-8 (2010)
Vanderbilt University Medical Center
Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists.
Bioorg Med Chem Lett 20: 5165-9 (2010)
Evotec (Uk)
Fluorescent retinoid X receptor ligands for fluorescence polarization assay.
Bioorg Med Chem Lett 20: 5143-6 (2010)
Okayama University
Discovery of cannabinoid-1 receptor antagonists by virtual screening.
Bioorg Med Chem Lett 20: 5130-2 (2010)
Korea Research Institute Of Chemical Technology
Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors.
J Med Chem 53: 6188-97 (2010)
University Of Firenze
Identification and characterization of acidic mammalian chitinase inhibitors.
J Med Chem 53: 6122-8 (2010)
Pfizer
Discovery and mechanistic study of a class of protein arginine methylation inhibitors.
J Med Chem 53: 6028-39 (2010)
Georgia State University
Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1a prolyl hydroxylases-1, -2, and -3 with altered selectivity.
J Comb Chem 12: 676-86 (2010)
Amgen
Aryl phosphoramidates of 5-phospho erythronohydroxamic acid, a new class of potent trypanocidal compounds.
J Med Chem 53: 6071-8 (2010)
University Of Dundee
Structural and thermodynamic analyses of α-L-fucosidase inhibitors.
Chembiochem 11: 1971-4 (2010)
University Of York
Biaryl substituted hydantoin compounds as TACE inhibitors.
Bioorg Med Chem Lett 20: 5286-9 (2010)
Merck Research Laboratories
A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists.
Bioorg Med Chem Lett 20: 4749-52 (2010)
Pfizer
Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site.
Bioorg Med Chem Lett 20: 4819-24 (2010)
K£Mia
Synthesis and antiproliferative evaluation of certain indeno[1,2-c]quinoline derivatives. Part 2.
J Med Chem 53: 6164-79 (2010)
Kaohsiung Medical University
Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as sigma-1 receptor ligands.
J Med Chem 53: 6228-39 (2010)
University Of Sydney
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
Antimicrob Agents Chemother 54: 4451-63 (2010)
Pfizer
Expression, purification, and characterization of Aspergillus fumigatus sterol 14-alpha demethylase (CYP51) isoenzymes A and B.
Antimicrob Agents Chemother 54: 4225-34 (2010)
Swansea University
Synthesis and T-type calcium channel blocking activity of novel diphenylpiperazine compounds, and evaluation of in vivo analgesic activity.
Bioorg Med Chem 18: 5938-44 (2010)
Ewha Womans University
Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.
Bioorg Med Chem Lett 20: 5241-4 (2010)
H. Lundbeck
A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements.
Bioorg Med Chem Lett 20: 5258-61 (2010)
University Of Delaware
New halogenated 3-phenylcoumarins as potent and selective MAO-B inhibitors.
Bioorg Med Chem Lett 20: 5157-60 (2010)
Universidad De Santiago De Compostela
Multipotent drugs with cholinergic and neuroprotective properties for the treatment of Alzheimer and neuronal vascular diseases. I. Synthesis, biological assessment, and molecular modeling of simple and readily available 2-aminopyridine-, and 2-chloropyridine-3,5-dicarbonitriles.
Bioorg Med Chem 18: 5861-72 (2010)
Laboratorio De Radicales Libres Y QuíMica Computacional (Iqog, Csic)
Characterization of new PPARgamma agonists: benzimidazole derivatives-importance of positions 5 and 6, and computational studies on the binding mode.
Bioorg Med Chem 18: 5885-95 (2010)
Freie UniversitäT Berlin
Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1).
Bioorg Med Chem Lett 20: 5184-90 (2010)
Pfizer
Fragment-based discovery and optimization of BACE1 inhibitors.
Bioorg Med Chem Lett 20: 5329-33 (2010)
Evotec
Modification at the acidic domain of RXR agonists has little effect on permissive RXR-heterodimer activation.
Bioorg Med Chem Lett 20: 5139-42 (2010)
Okayama University
Synthesis and in vitro binding studies of piperazine-alkyl-naphthamides: impact of homology and sulphonamide/carboxamide bioisosteric replacement on the affinity for 5-HT1A, alpha2A, D4.2, D3 and D2L receptors.
Bioorg Med Chem Lett 20: 5199-202 (2010)
University Of LièGe
Improved inhibition of the histone acetyltransferase PCAF by an anacardic acid derivative.
Bioorg Med Chem 18: 5826-34 (2010)
Groningen Research Institute Of Pharmacy
Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: a novel series of atypical antipsychotic agents.
Bioorg Med Chem Lett 20: 5221-4 (2010)
Korea Research Institute Of Chemical Technology
Synthesis and CYP24A1 inhibitory activity of (E)-2-(2-substituted benzylidene)- and 2-(2-substituted benzyl)-6-methoxy-tetralones.
Eur J Med Chem 45: 4427-34 (2010)
Cardiff University
Natural and semisynthetic azaphilones as a new scaffold for Hsp90 inhibitors.
Bioorg Med Chem 18: 6031-43 (2010)
Universit£
Structure-activity studies on acetylcholinesterase inhibition in the lycorine series of Amaryllidaceae alkaloids.
Bioorg Med Chem Lett 20: 5290-4 (2010)
Mcmaster University
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.
Bioorg Med Chem Lett 20: 5302-7 (2010)
Novartis Institutes For Biomedical Research
Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists.
Bioorg Med Chem Lett 20: 5269-73 (2010)
Sunesis Pharmaceuticals
Triaryl (Z)-olefins suitable for radiolabeling with carbon-11 or fluorine-18 radionuclides for positron emission tomography imaging of cyclooxygenase-2 expression in pathological disease.
Bioorg Med Chem Lett 20: 5245-50 (2010)
University Of Alberta
X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors.
Bioorg Med Chem Lett 20: 5217-20 (2010)
Roche Palo Alto
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.
Bioorg Med Chem Lett 20: 5203-6 (2010)
Université
Design, synthesis, and biological evaluation of ketoprofen analogs as potent cyclooxygenase-2 inhibitors.
Bioorg Med Chem 18: 5855-60 (2010)
Shahid Beheshti University Of Medical Sciences
Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylase based on a cinnamic hydroxamic acid core structure.
Bioorg Med Chem 18: 5950-64 (2010)
University Of Minnesota
Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.
Bioorg Med Chem Lett 20: 5313-9 (2010)
F. Hoffmann-La Roche
Novel Notch-sparing gamma-secretase inhibitors derived from a peroxisome proliferator-activated receptor agonist library.
Bioorg Med Chem Lett 20: 5282-5 (2010)
Okayama University Graduate School Of Medicine
Identification of novel monoamine oxidase B inhibitors by structure-based virtual screening.
Bioorg Med Chem Lett 20: 5295-8 (2010)
Northeastern Ohio Universities
The GABA(A) receptor as a target for photochromic molecules.
Bioorg Med Chem 18: 7731-8 (2010)
University Of Massachusetts
Synthesis of aryl-heteroaryl ureas (AHUs) based on 4-aminoquinoline and their evaluation against the insulin-like growth factor receptor (IGF-1R).
Bioorg Med Chem 18: 5995-6005 (2010)
San Francisco State University
4-Anilino-6-phenyl-quinoline inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2).
Bioorg Med Chem Lett 20: 4738-40 (2010)
Astrazeneca R & D Lund
Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant.
Bioorg Med Chem Lett 20: 4757-61 (2010)
Merck Research Laboratories
An integrative in silico methodology for the identification of modulators of macrophage migration inhibitory factor (MIF) tautomerase activity.
Bioorg Med Chem 18: 5425-40 (2010)
Brain Mind Institute
Functional profiling of p53-binding sites in Hdm2 and Hdmx using a genetic selection system.
Bioorg Med Chem 18: 6099-108 (2010)
Purdue University
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
Bioorg Med Chem Lett 20: 4816-8 (2010)
Pfizer
Discovery of novel alpha7 nicotinic receptor antagonists.
Bioorg Med Chem Lett 20: 4825-30 (2010)
Intra-Cellular Therapies
Exploring benzcyclo derivatives as potent aromatase inhibitors using ligand-based modeling studies.
Eur J Med Chem 45: 4307-15 (2010)
University Of Calcutta
Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold.
Eur J Med Chem 45: 4280-7 (2010)
Wichita State University
Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay.
Eur J Med Chem 45: 4316-30 (2010)
University Of Jordan
A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity.
Bioorg Med Chem 18: 6089-98 (2010)
The University Of Adelaide
Synthesis of novel 3,5-diaryl pyrazole derivatives using combinatorial chemistry as inhibitors of tyrosinase as well as potent anticancer, anti-inflammatory agents.
Bioorg Med Chem 18: 6149-55 (2010)
Solapur University
Structure and activity relationships of tartrate-based TACE inhibitors.
Bioorg Med Chem Lett 20: 4812-5 (2010)
Merck Research Laboratories
Refinement of the pharmacophore of 3,4-dihydroquinazoline-2(1H)-thiones for their anti-melanogenesis activity.
Bioorg Med Chem Lett 20: 4771-3 (2010)
Chungnam National University
An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction.
Bioorg Med Chem Lett 20: 4901-5 (2010)
Evotec (Uk)
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Bioorg Med Chem Lett 20: 4911-7 (2010)
Phenex Pharmaceuticals
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
Bioorg Med Chem 18: 6024-30 (2010)
University Of Cagliari
Synthesis of pyridazine and thiazole analogs as SGLT2 inhibitors.
Bioorg Med Chem 18: 6069-79 (2010)
Green Cross
Further optimization of novel pyrrole 3-carboxamides for targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.
Bioorg Med Chem 18: 6156-69 (2010)
Green Cross
Novel aminopeptidase N (APN/CD13) inhibitors derived from 3-phenylalanyl-N'-substituted-2,6-piperidinedione.
Bioorg Med Chem 18: 5981-7 (2010)
Shandong University
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3.
Bioorg Med Chem Lett 20: 4774-8 (2010)
Daiichi Sankyo
Integrated ligand and structure based studies of flavonoids as fatty acid biosynthesis inhibitors of Plasmodium falciparum.
Bioorg Med Chem Lett 20: 4779-81 (2010)
Csir-Central Drug Research Institute
3-D-QSAR and docking studies on the neuronal choline transporter.
Bioorg Med Chem Lett 20: 4870-7 (2010)
Northeastern Ohio Universities Colleges Of Medicine And Pharmacy
Design and synthesis of novel isoxazole-based HDAC inhibitors.
Eur J Med Chem 45: 4331-8 (2010)
Università
Structural combination of established 5-HT(2A) receptor ligands: new aspects of the binding mode.
Chem Biol Drug Des 76: 361-6 (2010)
University Of Mainz
New bioactive halenaquinone derivatives from South Pacific marine sponges of the genus Xestospongia.
Bioorg Med Chem 18: 6006-11 (2010)
National Museum Of Natural History
Syntheses and pharmacological characterization of novel thiazole derivatives as potential mGluR5 PET ligands.
Bioorg Med Chem 18: 6044-54 (2010)
Eth Zurich (Swiss Federal Institute Of Technology)
Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X(7) antagonists.
Bioorg Med Chem Lett 20: 4951-4 (2010)
Glaxosmithkline
Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.
Bioorg Med Chem Lett 20: 4789-94 (2010)
Elan Pharmaceuticals
Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.
Bioorg Med Chem Lett 20: 4800-4 (2010)
Millennium Pharmaceuticals
Design, synthesis, and structure-activity relationship study of conformationally constrained analogs of indole-3-carboxamides as novel CB1 cannabinoid receptor agonists.
Bioorg Med Chem Lett 20: 4918-21 (2010)
Schering-Plough Research Institute
Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution.
Bioorg Med Chem Lett 20: 4836-9 (2010)
Kyoto Pharmaceutical University
New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action.
Bioorg Med Chem 18: 5510-8 (2010)
Universit£
N(epsilon)-Modified lysine containing inhibitors for SIRT1 and SIRT2.
Bioorg Med Chem 18: 5616-25 (2010)
University Of Eastern Finland
Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists.
Bioorg Med Chem Lett 20: 4741-4 (2010)
Glaxosmithkline
Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.
Bioorg Med Chem Lett 20: 4795-9 (2010)
Millennium Pharmaceuticals
Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
Bioorg Med Chem 18: 4687-93 (2011)
National Institute On Aging
Identification of a sulfonamide series of CCR2 antagonists.
Bioorg Med Chem Lett 20: 3961-4 (2010)
Glaxosmithkline
Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents.
Bioorg Med Chem 18: 4606-14 (2011)
Nanjing University
Inhibition of prolyl oligopeptidase with a synthetic unnatural dipeptide.
Bioorg Med Chem 18: 4775-82 (2011)
The University Of Warwick
Design and synthesis of novel hydroxyalkylaminomethylchromones for their IL-5 inhibitory activity.
Bioorg Med Chem 18: 4625-9 (2011)
Chungnam National University
Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases.
Bioorg Med Chem Lett 20: 3863-7 (2010)
Walter Reed Army Institute Of Research
Cell cycle arrest and cytochrome c-mediated apoptotic induction by MCS-5A is associated with up-regulation of p16(INK4a) in HL-60 cells.
Bioorg Med Chem Lett 20: 3880-4 (2010)
Kyunggi-Do
Inhibition of ABCG2-mediated drug efflux by naphthopyrones from marine crinoids.
Bioorg Med Chem Lett 20: 3848-50 (2010)
Nci-Frederick
Design and synthesis of benzoazepin-2-one analogs as allosteric binders targeting the PIF pocket of PDK1.
Bioorg Med Chem Lett 20: 3897-902 (2010)
Genomics Institute Of The Novartis Research Foundation
Synthesis and evaluation of some novel dibenzo[b,d]furan carboxylic acids as potential anti-diabetic agents.
Eur J Med Chem 45: 3709-18 (2010)
Glenmark Research Center
Fragment-based discovery of novel thymidylate synthase leads by NMR screening and group epitope mapping.
Chem Biol Drug Des 76: 218-33 (2010)
University Of Washington
Chemical validation of phosphodiesterase C as a chemotherapeutic target in Trypanosoma cruzi, the etiological agent of Chagas' disease.
Antimicrob Agents Chemother 54: 3738-45 (2010)
University Of Georgia
Mutation of Phe91 to Asn in human carbonic anhydrase I unexpectedly enhanced both catalytic activity and affinity for sulfonamide inhibitors.
Bioorg Med Chem 18: 5498-503 (2010)
Balikesir University
Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers.
Bioorg Med Chem Lett 20: 4219-22 (2010)
Institute Of Science And Technology
Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors.
Bioorg Med Chem Lett 20: 4156-8 (2010)
Takeda California
Structure-based optimization of potent PDK1 inhibitors.
Bioorg Med Chem Lett 20: 4095-9 (2010)
Nerviano Medical Sciences
Subtype-selectivity of metal-dependent methionine aminopeptidase inhibitors.
Bioorg Med Chem Lett 20: 4038-44 (2010)
Universit£T Heidelberg
The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796.
Bioorg Med Chem 18: 5738-48 (2010)
The University Of Arizona
Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha.
Bioorg Med Chem 18: 5593-601 (2010)
Instituto PolitéCnico Nacional 2508
Synthesis and pharmacology of 1-methoxy analogs of CP-47,497.
Bioorg Med Chem 18: 5475-82 (2010)
Clemson University
Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists.
Bioorg Med Chem 18: 5519-27 (2010)
Zhejiang University
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.
Bioorg Med Chem Lett 20: 4940-4 (2010)
Trinity College
Synthesis of potent chemical inhibitors of dynamin GTPase.
Bioorg Med Chem Lett 20: 4858-64 (2010)
Gwangju Institute Of Science And Technology
Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.
Bioorg Med Chem Lett 20: 4895-900 (2010)
Merck Research Laboratories
Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer's disease.
Bioorg Med Chem 18: 5610-5 (2010)
Zhejiang University
Substrate specificity and inhibitory study of human airway trypsin-like protease.
Bioorg Med Chem 18: 5504-9 (2010)
Faculty Of Chemistry Gdansk University
Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors.
Bioorg Med Chem Lett 20: 4885-91 (2010)
Pfizer
Smoothened antagonists for hair inhibition.
Bioorg Med Chem Lett 20: 4932-5 (2010)
Pfizer
Synthesis, binding and bioactivity of gamma-methylene gamma-lactam ecdysone receptor ligands: advantages of QSAR models for flexible receptors.
Bioorg Med Chem 18: 5647-60 (2010)
Csiro Molecular And Health Technologies
A newly synthesized, potent tyrosinase inhibitor: 5-(6-hydroxy-2-naphthyl)-1,2,3-benzenetriol.
Bioorg Med Chem Lett 20: 4882-4 (2010)
Pusan National University
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
J Med Chem 53: 5491-501 (2010)
University Of Arizona
Investigations on the 2-thiazolylhydrazyne scaffold: synthesis and molecular modeling of selective human monoamine oxidase inhibitors.
Bioorg Med Chem 18: 5715-23 (2010)
Sapienza University Of Rome
Elucidation of the topography of the thapsigargin binding site in the sarco-endoplasmic calcium ATPase.
Bioorg Med Chem 18: 5634-46 (2010)
University Of Copenhagen
GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.
Bioorg Med Chem Lett 20: 4472-4 (2010)
Merck Research Laboratories
LuxR-dependent quorum sensing: computer aided discovery of new inhibitors structurally unrelated to N-acylhomoserine lactones.
Bioorg Med Chem Lett 20: 4355-8 (2010)
Insa
Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists.
Bioorg Med Chem Lett 20: 4371-5 (2010)
Gedeon Richter
Pyrido[2,3-b]pyrazines, discovery of TRPV1 antagonists with reduced potential for the formation of reactive metabolites.
Bioorg Med Chem Lett 20: 4359-63 (2010)
Neurogen
Peptide deformylase inhibitors with retro-amide scaffold: synthesis and structure-activity relationships.
Bioorg Med Chem Lett 20: 4317-9 (2010)
Seoul National University
Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif.
Bioorg Med Chem Lett 20: 4364-6 (2010)
University Of Dundee
Tricyclic imidazole antagonists of the Neuropeptide S Receptor.
Bioorg Med Chem Lett 20: 4704-8 (2010)
Merck Research Laboratories
The discovery of potent inhibitors of aldosterone synthase that exhibit selectivity over 11-beta-hydroxylase.
Bioorg Med Chem Lett 20: 4324-7 (2010)
Novartis Institutes For Biomedical Research
Probing the binding site of curcumin in Escherichia coli and Bacillus subtilis FtsZ--a structural insight to unveil antibacterial activity of curcumin.
Eur J Med Chem 45: 4209-14 (2010)
National Institute Of Pharmaceutical Education And Research
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
J Med Chem 53: 5844-57 (2010)
University Of North Carolina At Chapel Hill
Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator.
J Med Chem 53: 5801-12 (2010)
Glaxosmithkline
Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.
Bioorg Med Chem Lett 20: 4201-5 (2010)
Merck Research Laboratories
Synthesis and biological evaluation of novel biotin-iminoalditol conjugates.
Bioorg Med Chem Lett 20: 4077-9 (2010)
Technische Universit£T Graz
Efficient synthesis of Hsp90 inhibitor dimers as potential antitumor agents.
Bioorg Med Chem 18: 5732-7 (2010)
Hokkaido University
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
Bioorg Med Chem Lett 20: 4328-32 (2010)
Merck Research Laboratory
Chemical proteomics identifies Nampt as the target of CB30865, an orphan cytotoxic compound.
Chem Biol 17: 659-64 (2010)
Kyowa Hakko Kogyo
ATPases as drug targets: insights from heat shock proteins 70 and 90.
J Med Chem 53: 7280-6 (2010)
Vernalis R&D
Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.
Antimicrob Agents Chemother 54: 3825-33 (2010)
Oklahoma State University
In vitro potentiation of carbapenems with ME1071, a novel metallo-beta-lactamase inhibitor, against metallo-beta-lactamase- producing Pseudomonas aeruginosa clinical isolates.
Antimicrob Agents Chemother 54: 3625-9 (2010)
Toho University School Of Medicine
Amide conjugates of ketoprofen and indole as inhibitors of Gli1-mediated transcription in the Hedgehog pathway.
Bioorg Med Chem 18: 4801-11 (2011)
St. Jude Children'S Research Hospital
[d4U]-spacer-[HI-236] double-drug inhibitors of HIV-1 reverse-transcriptase.
Bioorg Med Chem 18: 4661-73 (2010)
University Of Cape Town
C(2)-Symmetric azobenzene-amino acid conjugates and their inhibition of Subtilisin Kexin Isozyme-1.
Bioorg Med Chem Lett 20: 3977-81 (2010)
Indian Institute Of Technology
Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity.
Bioorg Med Chem Lett 20: 3906-10 (2010)
Birla Institute Of Technology
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
Eur J Med Chem 45: 3740-51 (2010)
Universit£
Further delineation of hydrophobic binding sites in dopamine D(2)/D(3) receptors for N-4 substituents on the piperazine ring of the hybrid template 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol.
Bioorg Med Chem 18: 5661-74 (2010)
Wayne State University
Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors.
Bioorg Med Chem Lett 20: 4376-81 (2010)
University Of Florida
Synthesis and structure-activity relationships of N-(2-oxo-3-oxetanyl)amides as N-acylethanolamine-hydrolyzing acid amidase inhibitors.
J Med Chem 53: 5770-81 (2010)
University Of California
A type-II kinase inhibitor capable of inhibiting the T315I"gatekeeper" mutant of Bcr-Abl.
J Med Chem 53: 5439-48 (2010)
Harvard Medical School
Evaluation of N-substitution in 6,7-benzomorphan compounds.
Bioorg Med Chem 18: 4975-82 (2010)
University Of Catania
Virtual fragment screening for novel inhibitors of 6-phosphogluconate dehydrogenase.
Bioorg Med Chem 18: 5056-62 (2010)
University Of Dundee
Derivatives of tetrahydroisoquinoline: synthesis and initial evaluation of novel non-peptide antagonists of the alpha(IIb)beta(3)-integrin.
Bioorg Med Chem Lett 20: 4444-6 (2010)
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine
3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.
Bioorg Med Chem Lett 20: 4390-4 (2010)
Vanderbilt University Medical Center
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.
Bioorg Med Chem Lett 20: 4350-4 (2010)
Merck Research Laboratories
Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity.
Bioorg Med Chem Lett 20: 4399-405 (2010)
Merck Research Laboratories
Discovery of novel sphingosine kinase-1 inhibitors. Part 2.
Bioorg Med Chem Lett 20: 4550-4 (2010)
Genzyme
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents.
Eur J Med Chem 45: 4096-103 (2010)
Beijing Institute Of Biotechnology
2-phenyl-1-[4-(2-piperidine-1-yl-ethoxy)benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: synthesis and pharmacological evaluation.
Bioorg Med Chem 18: 4905-16 (2010)
Freie Universit£T Berlin
Syntheses and herbicidal activity of new triazolopyrimidine-2-sulfonamides as acetohydroxyacid synthase inhibitor.
Bioorg Med Chem 18: 4897-904 (2010)
Central China Normal University
Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors.
Bioorg Med Chem 18: 4928-38 (2010)
Universit£
Coumarinyl-substituted sulfonamides strongly inhibit several human carbonic anhydrase isoforms: solution and crystallographic investigations.
Bioorg Med Chem 18: 4873-8 (2010)
University Of Florida
beta-Secretase (BACE-1) inhibitory effect of biflavonoids.
Bioorg Med Chem Lett 20: 4558-60 (2010)
Shujitsu University
Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes.
Bioorg Med Chem Lett 20: 4395-8 (2010)
Bristol-Myers Squibb
Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.
Bioorg Med Chem Lett 20: 4483-6 (2010)
Merck Research Laboratories
Synthesis, fluorine-18 radiolabeling, and biological evaluation of N-((E)-4-fluorobut-2-en-1-yl)-2beta-carbomethoxy-3beta-(4'-halophenyl)nortropanes: candidate radioligands for in vivo imaging of the brain dopamine transporter with positron emission tomography.
J Med Chem 53: 5549-57 (2010)
Emory University
Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol.
J Med Chem 53: 5676-83 (2010)
Institute For Cancer Research
Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors.
J Med Chem 53: 5639-55 (2010)
The Institute Of Cancer Research
Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides.
Bioorg Med Chem 18: 4939-46 (2010)
Cardiff University
Synthesis, molecular modeling, and biological evaluation of cinnamic acid metronidazole ester derivatives as novel anticancer agents.
Bioorg Med Chem 18: 4991-6 (2010)
Nanjing University
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.
Bioorg Med Chem Lett 20: 4715-8 (2010)
Novartis Institutes For Biomedical Research
Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.
Bioorg Med Chem Lett 20: 4607-10 (2010)
Amgen
Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties.
Bioorg Med Chem Lett 20: 4587-92 (2010)
Glaxosmithkline
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.
Bioorg Med Chem Lett 20: 4447-50 (2010)
Merck Research Laboratories
Design, synthesis, and structure-activity relationships of pyrazole derivatives as potential FabH inhibitors.
Bioorg Med Chem Lett 20: 4657-60 (2010)
Nanjing University
Synthesis and pharmacological evaluation of aryl aminosulfonamide derivatives as potent 5-HT(6) receptor antagonists.
Bioorg Med Chem Lett 20: 4440-3 (2010)
Suven Life Sciences
Heteroadamantyl cannabinoids.
J Med Chem 53: 5656-66 (2010)
University Of Hawaii At Manoa
Development of chemical probes: toward the mode of action of a methylene-linked di(aryl acetate) E1.
Bioorg Med Chem 18: 4917-27 (2010)
University College London
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II.
Bioorg Med Chem Lett 20: 4719-23 (2010)
Novartis Institutes For Biomedical Research
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Bioorg Med Chem Lett 20: 4406-11 (2010)
Università
Identification of novel alpha7 nAChR positive allosteric modulators with the use of pharmacophore in silico screening methods.
Bioorg Med Chem Lett 20: 4561-5 (2010)
Glaxosmithkline
Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule.
J Med Chem 53: 5511-22 (2010)
Universita Degli Studi Di Firenze
Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).
J Med Chem 53: 5827-43 (2010)
Glaxosmithkline
Design and synthesis of C-2 substituted thiazolo and dihydrothiazolo ring-fused 2-pyridones: pilicides with increased antivirulence activity.
J Med Chem 53: 5690-5 (2010)
Ume£
Peptide HIV-1 integrase inhibitors from HIV-1 gene products.
J Med Chem 53: 5356-60 (2010)
Tokyo Medical And Dental University
(-)-N-Formylanonaine from Michelia alba as a human tyrosinase inhibitor and antioxidant.
Bioorg Med Chem 18: 5241-7 (2010)
Kaohsiung Medical University
Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
Bioorg Med Chem Lett 20: 4491-5 (2010)
Bristol-Myers Squibb
Rational design of a novel peripherally-restricted, orally active CB(1) cannabinoid antagonist containing a 2,3-diarylpyrrole motif.
Bioorg Med Chem Lett 20: 4573-7 (2010)
Sanofi-Aventis R&D
Cyclic amide bioisosterism: strategic application to the design and synthesis of HCV NS5B polymerase inhibitors.
Bioorg Med Chem Lett 20: 4614-9 (2010)
Roche Palo Alto
Nantenine as an acetylcholinesterase inhibitor: SAR, enzyme kinetics and molecular modeling investigations.
J Enzyme Inhib Med Chem 26: 46-55 (2011)
City University Of New York Hunter College
Synthesis and antiproliferative activities against Hep-G2 of salicylanide derivatives: potent inhibitors of the epidermal growth factor receptor (EGFR) tyrosine kinase.
J Enzyme Inhib Med Chem 26: 37-45 (2011)
Nanjing University
Theoretical studies on the molecular basis of HIV-1RT/NNRTIs interactions.
J Enzyme Inhib Med Chem 26: 29-36 (2011)
Chulalongkorn University
2-acylamino-4,6-diphenylpyridine derivatives as novel GPR54 antagonists with good brain exposure and in vivo efficacy for plasma LH level in male rats.
Bioorg Med Chem 18: 5157-71 (2010)
Takeda Pharmaceutical
Pteridine-sulfonamide conjugates as dual inhibitors of carbonic anhydrases and dihydrofolate reductase with potential antitumor activity.
Bioorg Med Chem 18: 5081-9 (2010)
Instituto Superior T£Cnico
Deoxynojirimycin and its hexosaminyl derivatives bind to natural killer cell receptors rNKR-P1A and hCD69.
Bioorg Med Chem Lett 20: 4645-8 (2010)
Universit£
NF-kappaB inducing kinase (NIK) inhibitors: identification of new scaffolds using virtual screening.
Bioorg Med Chem Lett 20: 4515-20 (2010)
University Of Namur
Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.
Bioorg Med Chem 18: 5071-80 (2010)
University Of Innsbruck And Center For Molecular Biosciences Innsbruck-Cmbi
Piperidinyl-nicotinamides as potent and selective somatostatin receptor subtype 5 antagonists.
Bioorg Med Chem Lett 20: 4521-5 (2010)
F. Hoffmann-La Roche
T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones-optimization, design and synthesis.
Bioorg Med Chem Lett 20: 4602-6 (2010)
Merck Research Laboratory
4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important.
Bioorg Med Chem Lett 20: 4507-10 (2010)
Merck Research Laboratories
Identification of potent virtual leads to design novel indoleamine 2,3-dioxygenase inhibitors: pharmacophore modeling and molecular docking studies.
Eur J Med Chem 45: 4004-12 (2010)
Gyeongsang National University
Synthesis, semipreparative HPLC separation, biological evaluation, and 3D-QSAR of hydrazothiazole derivatives as human monoamine oxidase B inhibitors.
Bioorg Med Chem 18: 5063-70 (2010)
Sapienza University Of Rome
Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.
Bioorg Med Chem Lett 20: 4653-6 (2010)
Glaxosmithkline
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.
Bioorg Med Chem Lett 20: 4639-44 (2010)
Glaxosmithkline
Unusual activity pattern of leucine aminopeptidase inhibitors based on phosphorus containing derivatives of methionine and norleucine.
J Enzyme Inhib Med Chem 26: 155-61 (2011)
Academy Of Sciences Of The Czech Republic
Solution phase synthesis of a combinatorial library of chalcones and flavones as potent cathepsin V inhibitors.
J Comb Chem 12: 687-95 (2010)
Universidade Federal De SaO Carlo
Complexes of bacterial nicotinate mononucleotide adenylyltransferase with inhibitors: implication for structure-based drug design and improvement.
J Med Chem 53: 5229-39 (2010)
University Of Texas Southwestern Medical Center
ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Bioorg Med Chem 18: 4422-32 (2010)
Chinese Academy Of Sciences
Alpneumines A-H, new anti-melanogenic indole alkaloids from Alstonia pneumatophora.
Bioorg Med Chem 18: 4415-21 (2010)
Hoshi University
Design, synthesis, and docking of highly hypolipidemic agents: Schizosaccharomyces pombe as a new model for evaluating alpha-asarone-based HMG-CoA reductase inhibitors.
Bioorg Med Chem 18: 4238-48 (2010)
Instituto Polit£Cnico Nacional (Ipn)
Pharmacophore and structure-activity relationships of integrase inhibition within a dual inhibitor scaffold of HIV reverse transcriptase and integrase.
Bioorg Med Chem 18: 4202-11 (2010)
University Of Minnesota
New aryldithiolethione derivatives as potent histone deacetylase inhibitors.
Bioorg Med Chem 18: 4187-94 (2010)
Sulfidris
Celecoxib prodrugs possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
Bioorg Med Chem Lett 20: 4544-9 (2010)
University Of Alberta
Identification of glycosylated exendin-4 analogue with prolonged blood glucose-lowering activity through glycosylation scanning substitution.
Bioorg Med Chem Lett 20: 4631-4 (2010)
Shionogi And
3-Formylchromones: potential antiinflammatory agents.
Eur J Med Chem 45: 4058-64 (2010)
University Of Karachi
Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives.
J Med Chem 53: 5129-43 (2010)
Universidad Autonoma De Madrid
The pthaladyns: GTP competitive inhibitors of dynamin I and II GTPase derived from virtual screening.
J Med Chem 53: 5267-80 (2010)
The University Of Newcastle
Analysis of the binding of mixed lineage leukemia 1 (MLL1) and histone 3 peptides to WD repeat domain 5 (WDR5) for the design of inhibitors of the MLL1-WDR5 interaction.
J Med Chem 53: 5179-85 (2010)
University Of Michigan
3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors.
Bioorg Med Chem Lett 20: 4709-11 (2010)
Mitsubishi Tanabe Pharma
Aryl sulfonamides containing tetralin allylic amines as potent and selective bradykinin B1 receptor antagonists.
Bioorg Med Chem Lett 20: 4593-7 (2010)
Amgen
A specific and direct comparison of the trifluoromethyl and pentafluoro sulfanyl groups on the selective dopamine D(3) antagonist 3-(3-{[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]thio}propyl)-1-phenyl-3-azabicyclo[3.1.0]hexane template.
Bioorg Med Chem Lett 20: 4566-8 (2010)
Glaxosmithkline
Synthesis and structure-affinity relationships of novel small molecule natural product derivatives capable of discriminating between serotonin 5-HT1A, 5-HT2A, 5-HT2C receptor subtypes.
Bioorg Med Chem 18: 4783-92 (2011)
University Of North Texas Health Science Center
Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists.
Bioorg Med Chem 18: 4821-9 (2011)
Abbott Laboratories
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
Bioorg Med Chem 18: 4601-5 (2010)
Fudan University
Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.
Bioorg Med Chem 18: 4674-86 (2011)
National Taiwan University
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.
Bioorg Med Chem 18: 4615-24 (2011)
Chinese Academy Of Sciences
Crystallographic and docking studies of purine nucleoside phosphorylase from Mycobacterium tuberculosis.
Bioorg Med Chem 18: 4769-74 (2011)
Pontifical Catholic University Of Rio Grande Do Sul
Chemoselective regulation of TREK2 channel: activation by sulfonate chalcones and inhibition by sulfonamide chalcones.
Bioorg Med Chem Lett 20: 4237-9 (2010)
Gyeongsang National University
Discovery of aminopyridines substituted with benzoxazole as orally active c-Met kinase inhibitors.
Bioorg Med Chem Lett 20: 4223-7 (2010)
Korea Research Institute Of Chemical Technology
Interaction of aminoadamantane derivatives with the influenza A virus M2 channel-docking using a pore blocking model.
Bioorg Med Chem Lett 20: 4182-7 (2010)
University Of Athens
Optimization of isochromanone based urotensin II receptor agonists.
Bioorg Med Chem 18: 4844-54 (2011)
University Of Gothenburg
Synthesis and inhibitory activities of novel C-3 substituted azafagomines: a new type of selective inhibitors ofa-L-fucosidases.
Bioorg Med Chem 18: 4648-60 (2011)
University Of Seville
Click chemistry to probe Hsp90: Synthesis and evaluation of a series of triazole-containing novobiocin analogues.
Bioorg Med Chem Lett 20: 3957-60 (2010)
The University Of Kansas
The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38alpha MAP kinase.
Bioorg Med Chem Lett 20: 3936-40 (2010)
Glaxosmithkline
Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors.
Bioorg Med Chem Lett 20: 3925-9 (2010)
Johnson & Johnson Pharmaceutical Research & Development
2-Substituted N-aryl piperazines as novel triple reuptake inhibitors for the treatment of depression.
Bioorg Med Chem Lett 20: 3941-5 (2010)
Roche Palo Alto
5-Nitro-2,6-dioxohexahydro-4-pyrimidinecarboxamides: synthesis, in vitro antimycobacterial activity, cytotoxicity, and isocitrate lyase inhibition studies.
J Enzyme Inhib Med Chem 25: 765-72 (2010)
Birla Institute Of Technology
Novel highly potent and selective nonsteroidal aromatase inhibitors: synthesis, biological evaluation and structure-activity relationships investigation.
J Med Chem 53: 5347-51 (2010)
University Of Bologna
Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity.
J Med Chem 53: 5290-301 (2010)
Research Triangle Institute
(Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators.
J Med Chem 53: 5197-212 (2010)
Wayne State University
Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria.
J Med Chem 53: 5155-64 (2010)
Novartis Institute For Tropical Diseases
Structurally designed trans-2-phenylcyclopropylamine derivatives potently inhibit histone demethylase LSD1/KDM1 .
Biochemistry 49: 6494-503 (2010)
Riken Systems And Structural Biology Center
Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid.
Antimicrob Agents Chemother 54: 3776-82 (2010)
Texas A&M University
5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administration.
Bioorg Med Chem Lett 20: 4598-601 (2010)
Amira Pharmaceuticals
Pyrazolopyridazine alpha-2-delta-1 ligands for the treatment of neuropathic pain.
Bioorg Med Chem Lett 20: 4683-8 (2010)
Glaxosmithkline
Design, synthesis and biological evaluation of CB1 cannabinoid receptor ligands derived from the 1,5-diarylpyrazole scaffold.
J Enzyme Inhib Med Chem 26: 222-30 (2011)
Nanchang University School Of Pharmaceutical Science
Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.
J Med Chem 53: 5213-28 (2010)
The Institute Of Cancer Research
Structural basis for the interaction between tankyrase-2 and a potent Wnt-signaling inhibitor.
J Med Chem 53: 5352-5 (2010)
Karolinska Institutet
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.
J Med Chem 53: 5320-32 (2010)
Merck Research Laboratories
Development of tryptase inhibitors derived from thalidomide.
Bioorg Med Chem 18: 5323-38 (2010)
The University Of Tokyo
Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment.
Bioorg Med Chem Lett 20: 4308-12 (2010)
Sanofi-Aventis
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents.
Bioorg Med Chem Lett 20: 4012-4 (2010)
Chinese Academy Of Sciences
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.
Bioorg Med Chem Lett 20: 4045-9 (2010)
The Institute Of Cancer Research
Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.
Bioorg Med Chem Lett 20: 4210-4 (2010)
Johnson & Johnson Pharmaceutical Research & Development
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.
J Med Chem 52: 5164-75 (2010)
University Of Arizona
(3-Phenylsulfonylcycloalkano[e and d]pyrazolo[1,5-a]pyrimidin-2-yl)amines: potent and selective antagonists of the serotonin 5-HT6 receptor.
J Med Chem 53: 5186-96 (2010)
Chemical Diversity Research Institute
Design, synthesis, and biological evaluation of resveratrol analogues as aromatase and quinone reductase 2 inhibitors for chemoprevention of cancer.
Bioorg Med Chem 18: 5352-66 (2010)
Purdue University
Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents.
Bioorg Med Chem 18: 5261-73 (2010)
Duquesne University
Structure-activity relationships and hepatic safety risks of thiazole agonists of the thrombopoietin receptor.
Bioorg Med Chem Lett 20: 4069-72 (2010)
Pfizer
Synthesis and evaluation of quinazolinone derivatives as inhibitors of NF-kappaB, AP-1 mediated transcription and eIF-4E mediated translational activation: inhibitors of multi-pathways involve in cancer.
Eur J Med Chem 45: 3558-63 (2010)
B.V. Patel Pharmaceutical Education And Research Development Centre
Thiadiazole carbamates: potent inhibitors of lysosomal acid lipase and potential Niemann-Pick type C disease therapeutics.
J Med Chem 53: 5281-9 (2010)
Weill Cornell Medical College
Click chemistry approach to new N-substituted aminocyclitols as potential pharmacological chaperones for Gaucher disease.
J Med Chem 53: 5248-55 (2010)
Universitat De Barcelona
Synthesis and biodistribution of [11C]A-836339, a new potential radioligand for PET imaging of cannabinoid type 2 receptors (CB2).
Bioorg Med Chem 18: 5202-7 (2010)
Johns Hopkins Medical Institutions
A novel and one-pot synthesis of new 1-tosyl pyrrol-2-one derivatives and analysis of carbonic anhydrase inhibitory potencies.
Bioorg Med Chem 18: 4468-74 (2010)
Atat£Rk University
Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII.
Eur J Med Chem 45: 3656-61 (2010)
Medical University Of Gdansk
Synthesis of 5-amino-1,3,4-thiadiazole-2-sulphonamide derivatives and their inhibition effects on human carbonic anhydrase isozymes.
J Enzyme Inhib Med Chem 26: 231-7 (2011)
Dumlupinar University
Discovery of potent ligands for estrogen receptor beta by structure-based virtual screening.
J Med Chem 53: 5361-5 (2010)
East China University Of Science And Technology
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.
J Med Chem 53: 4980-8 (2010)
National Health Research Institutes
Correlating solution binding and ESI-MS stabilities by incorporating solvation effects in a confined cucurbit[8]uril system.
J Phys Chem B 114: 8606-15 (2010)
University Of Cambridge
Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.
J Med Chem 53: 5049-53 (2010)
Saarland University
Stereoselective phosphorylation of cyclopropavir by pUL97 and competitive inhibition by maribavir.
Antimicrob Agents Chemother 54: 3093-8 (2010)
University Of Michigan
Extended-spectrum cephalosporinase in Acinetobacter baumannii.
Antimicrob Agents Chemother 54: 3484-8 (2010)
Paris-Sud University
Structure-activity analysis of vinylogous urea inhibitors of human immunodeficiency virus-encoded ribonuclease H.
Antimicrob Agents Chemother 54: 3913-21 (2010)
National Cancer Institute-Frederick
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.
Bioorg Med Chem Lett 20: 4080-4 (2010)
University Of Arizona
Epsilon substituted lysinol derivatives as HIV-1 protease inhibitors.
Bioorg Med Chem Lett 20: 4065-8 (2010)
Merck Research Laboratories
QSAR studies of bioactivities of 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 receptor ligands using physicochemical descriptors and MLR and ANN-modeling.
Eur J Med Chem 45: 3911-5 (2010)
Islamic Azad University
Synthesis, stability, biochemical and pharmacokinetic properties of a new potent and selective 4-oxo-ß-lactam inhibitor of human leukocyte elastase.
J Enzyme Inhib Med Chem 26: 169-75 (2011)
University Of Lisbon
Novel tacrine-8-hydroxyquinoline hybrids as multifunctional agents for the treatment of Alzheimer's disease, with neuroprotective, cholinergic, antioxidant, and copper-complexing properties.
J Med Chem 53: 4927-37 (2010)
Instituto De Quimica Medica
Site-specific orthogonal labeling of the carboxy terminus of alpha-tubulin.
ACS Chem Biol 5: 777-85 (2010)
Binghamton University
Discovery of potent and orally active tricyclic-based FBPase inhibitors.
Bioorg Med Chem 18: 5346-51 (2010)
Daiichi Sankyo
Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists.
Bioorg Med Chem Lett 20: 4104-7 (2010)
Glaxosmithkline
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.
Bioorg Med Chem 18: 5291-300 (2010)
Washington University
Discovery of orally available spirodiketopiperazine-based CCR5 antagonists.
Bioorg Med Chem 18: 5208-23 (2010)
Minase Research Institute
Synthesis and biological activity of glycosyl-1H-1,2,3-triazoles.
Bioorg Med Chem Lett 20: 4263-5 (2010)
Academy Of Sciences Of The Czech Republic
New 2-arylnaphthalenediols and triol inhibitors of HIV-1 integrase--discovery of a new polyhydroxylated antiviral agent.
Bioorg Med Chem 18: 5194-201 (2010)
Universit£
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.
Bioorg Med Chem Lett 20: 4140-6 (2010)
Roche Research Center
Synthesis and evaluation of vinyl sulfones as caspase-3 inhibitors. A structure-activity study.
Eur J Med Chem 45: 3858-63 (2010)
University Of Lisbon
Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.
Bioorg Med Chem 18: 5441-8 (2010)
Meiji Seika Kaisha
Synthesis and biological study of 3-(phenylsulfonyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines as potent and selective serotonin 5-HT6 receptor antagonists.
Bioorg Med Chem 18: 5282-90 (2010)
Chemical Diversity Research Institute
Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents.
Bioorg Med Chem 18: 5413-24 (2010)
Uppsala University
Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors.
Bioorg Med Chem Lett 20: 4060-4 (2010)
Johnson & Johnson Pharmaceutical Research & Development
Triterpene saponins from Clematis chinensis and their potential anti-inflammatory activity.
J Nat Prod 73: 1234-9 (2010)
Peking University Health Science Center
Complementarity between a docking and a high-throughput screen in discovering new cruzain inhibitors.
J Med Chem 53: 4891-905 (2010)
University Of California San Francisco
1H-1,2,3-triazol-1-yl thiodigalactoside derivatives as high affinity galectin-3 inhibitors.
Bioorg Med Chem 18: 5367-78 (2010)
The Hashemite University
Identification of novel inhibitors for a low molecular weight protein tyrosine phosphatase via virtual screening.
Bioorg Med Chem 18: 5449-56 (2010)
Purdue University
Synthesis and molecular docking studies of novel 2-chloro-pyridine derivatives containing flavone moieties as potential antitumor agents.
Bioorg Med Chem Lett 20: 4163-7 (2010)
Nanjing University
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
Bioorg Med Chem Lett 20: 4215-8 (2010)
Roche Palo Alto
Synthesis, antiproliferative activity and inhibition of tubulin polymerization by 1,5- and 1,8-disubstituted 10H-anthracen-9-ones bearing a 10-benzylidene or 10-(2-oxo-2-phenylethylidene) moiety.
Eur J Med Chem 45: 3420-38 (2010)
Westphalian Wilhelms-University
Bacterial transferase MraY inhibitors: synthesis and biological evaluation.
Bioorg Med Chem 18: 4560-9 (2010)
University Of Paris
Discovery of tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin KSP.
Bioorg Med Chem 18: 4167-77 (2010)
China Pharmaceutical University
Design and synthesis of disubstituted (4-piperidinyl)-piperazine derivatives as potent acetyl-CoA carboxylase inhibitors.
Bioorg Med Chem Lett 20: 3965-8 (2010)
Taisho Pharmaceutical
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.
Eur J Med Chem 45: 3459-71 (2010)
East China University Of Science And Technology
Discovery and optimization of boronic acid based inhibitors of autotaxin.
J Med Chem 53: 4958-67 (2010)
Institute
The action of herbicides on fatty acid biosynthesis and elongation in barley and cucumber.
Pest Manag Sci 66: 794-800 (2010)
Cardiff University
Synthesis and in vivo evaluation of [11C]MPTQ: a potential PET tracer for alpha2A-adrenergic receptors.
Bioorg Med Chem Lett 20: 3654-7 (2010)
Columbia University
MMP-13 selective isonipecotamide alpha-sulfone hydroxamates.
Bioorg Med Chem Lett 20: 3561-4 (2010)
Pfizer
Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates.
Bioorg Med Chem Lett 20: 3557-60 (2010)
Pfizer
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II).
Bioorg Med Chem Lett 20: 3502-6 (2010)
Elan Pharmaceuticals
Antitrypanosomal alkaloids from Polyalthia suaveolens (Annonaceae): their effects on three selected glycolytic enzymes of Trypanosoma brucei.
Bioorg Med Chem Lett 20: 3495-8 (2010)
University Of Yaound£
6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple reuptake inhibitor.
J Med Chem 53: 4989-5001 (2010)
Glaxosmithkline
Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazone.
J Med Chem 53: 5012-24 (2010)
Kyorin Pharmaceutical
Computer-aided identification of Trypanosoma brucei uridine diphosphate galactose 4'-epimerase inhibitors: toward the development of novel therapies for African sleeping sickness.
J Med Chem 53: 5025-32 (2010)
University Of California San Diego
Selective hexapeptide agonists and antagonists for human complement C3a receptor.
J Med Chem 53: 4938-48 (2010)
The University Of Queensland
Novel approaches for targeting thymidylate synthase to overcome the resistance and toxicity of anticancer drugs.
J Med Chem 53: 6539-49 (2010)
Institute Of Theoretical Studies Ggmbh
Selective synthesis and biological evaluation of sulfate-conjugated resveratrol metabolites.
J Med Chem 53: 5033-43 (2010)
Purdue University
Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
J Med Chem 53: 4862-76 (2010)
University Of Li£Ge
Glutathione transferase from Plasmodium falciparum--interaction with malagashanine and selected plant natural products.
J Enzyme Inhib Med Chem 25: 854-62 (2010)
University Of Zimbabwe
Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds.
J Med Chem 53: 5054-8 (2010)
Kyoto University
Synthesis of new 8(S)-HETE analogs and their biological evaluation as activators of the PPAR nuclear receptors.
J Enzyme Inhib Med Chem 25: 653-72 (2010)
Universit?? De Rennes 1
One-pot synthesis of 4,6-diaryl-2-oxo(imino)-1,2-dihydropyridine-3-carbonitrile; a New Scaffold for p38alpha MAP kinase inhibition.
J Comb Chem 12: 559-65 (2010)
German University In Cairo
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
Antimicrob Agents Chemother 54: 3478-80 (2010)
Achillion Pharmaceuticals
PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication.
Antimicrob Agents Chemother 54: 3187-96 (2010)
Pharmasset
Identification and characterization of novel classes of macrophage migration inhibitory factor (MIF) inhibitors with distinct mechanisms of action.
J Biol Chem 285: 26581-98 (2010)
Ecole Polytechnique FÉDÉRale De Lausanne
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.
J Med Chem 53: 4701-19 (2010)
Ariad Pharmaceuticals
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
Bioorg Med Chem 18: 4255-68 (2010)
Chinese Academy Of Sciences
A statistical analysis of in vitro human microsomal metabolic stability of small phenyl group substituents, leading to improved design sets for parallel SAR exploration of a chemical series.
Bioorg Med Chem 18: 4405-14 (2010)
Astrazeneca
Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists.
Bioorg Med Chem Lett 20: 4700-3 (2010)
Merck Research Laboratories
Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
J Med Chem 53: 4731-48 (2010)
Barrow Neurological Institute
Molecular switch controlling the binding of anionic bile acid conjugates to human apical sodium-dependent bile acid transporter.
J Med Chem 53: 4749-60 (2010)
University Of Maryland
Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity.
J Med Chem 53: 4691-700 (2010)
Zafes/Liff/Goethe University Frankfurt
Xestosaprols from the Indonesian marine sponge Xestospongia sp.
J Nat Prod 73: 1188-91 (2010)
University Of Hawaii At Manoa
Factor Xa inhibitors: next-generation antithrombotic agents.
J Med Chem 53: 6243-74 (2010)
Bristol-Myers Squibb
Identification of a chemoreceptor for tricarboxylic acid cycle intermediates: differential chemotactic response towards receptor ligands.
J Biol Chem 285: 23126-36 (2010)
Csic
Identification of novel quinazolin-4(3H)-ones as inhibitors of thermolysin, the prototype of the M4 family of proteinases.
Bioorg Med Chem 18: 4317-27 (2010)
University Of Troms£
Peptide fragmentation as an approach in modeling of an active peptide and designing a competitive inhibitory peptide for HMG-CoA reductase.
Bioorg Med Chem 18: 4300-9 (2010)
Institute Of The Chemistry Of Plant Substances
Quinlobelane: a water-soluble lobelane analogue and inhibitor of VMAT2.
Bioorg Med Chem Lett 20: 3584-7 (2010)
University Of Kentucky
Synthesis and characterization of N,N-dialkyl and N-alkyl-N-aralkyl fenpropimorph-derived compounds as high affinity ligands for sigma receptors.
Bioorg Med Chem 18: 4397-404 (2010)
University Of Wisconsin School Of Medicine And Public Health
Selective angiotensin II AT(2) receptor agonists with reduced CYP 450 inhibition.
Bioorg Med Chem 18: 4570-90 (2010)
Uppsala University
Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders.
Bioorg Med Chem Lett 20: 3708-12 (2010)
Merck Sharp & Dohme
Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists.
Bioorg Med Chem Lett 20: 3618-22 (2010)
Amgen
Prenylcoumarin with Rev-export inhibitory activity from Cnidii Monnieris Fructus.
Bioorg Med Chem Lett 20: 3717-20 (2010)
Osaka University
In silico characterization of cytisinoids docked into an acetylcholine binding protein.
Bioorg Med Chem Lett 20: 3683-7 (2010)
Instituto De Investigaciones Biol£Gicas Clemente Estable
Discovery of a series of indan carboxylic acid glycogen phosphorylase inhibitors.
Bioorg Med Chem Lett 20: 3511-4 (2010)
Astrazeneca
Synthesis and biological activity of oxadiazole and triazolothiadiazole derivatives as tyrosinase inhibitors.
Bioorg Med Chem Lett 20: 3755-9 (2010)
University Putra Malaysia
New estrogenic compounds isolated from Broussonetia kazinoki.
Bioorg Med Chem Lett 20: 3764-7 (2010)
Sookmyung Women'S University
Validated QSAR analysis of some diaryl substituted pyrazoles as CCR2 inhibitors by various linear and nonlinear multivariate chemometrics methods.
Eur J Med Chem 45: 3394-406 (2010)
Tehran University Of Medical Sciences
Triazole-linked inhibitors of inosine monophosphate dehydrogenase from human and Mycobacterium tuberculosis.
J Med Chem 53: 4768-78 (2010)
University Of Minnesota
Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia.
J Med Chem 53: 4603-14 (2010)
F. Hoffmann-La Roche
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
J Med Chem 53: 4654-67 (2010)
Universidade De Vigo
Synthesis and cytotoxicity of novel indirubin-5-carboxamides.
Bioorg Med Chem 18: 4509-15 (2010)
University Of Kaiserslautern
IKKbeta inhibitors identification part II: ligand and structure-based virtual screening.
Bioorg Med Chem 18: 3951-60 (2010)
Institute Of Science And Technology
Synthesis and biological evaluation of bicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
Bioorg Med Chem Lett 20: 3521-5 (2010)
Shanghai Hengrui Pharmaceuticals
Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
Bioorg Med Chem Lett 20: 3565-8 (2010)
Shanghai Hengrui Pharmaceuticals
CoMFA and CoMSIA 3D-QSAR studies on quionolone caroxylic acid derivatives inhibitors of HIV-1 integrase.
Eur J Med Chem 45: 3413-9 (2010)
Lanzhou University
Carbonic anhydrase inhibitors: Inhibition of human erythrocyte isozymes I and II with a series of phenolic acids.
Chem Biol Drug Des 75: 515-20 (2010)
Ataturk University
The use of biochemical and biophysical tools for triage of high-throughput screening hits - A case study with Escherichia coli phosphopantetheine adenylyltransferase.
Chem Biol Drug Des 75: 444-54 (2010)
Pfizer
Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.
Bioorg Med Chem 18: 4351-62 (2010)
Cephalon
5-arylamino-1,2,4-triazin-6(1H)-one CRF1 receptor antagonists.
Bioorg Med Chem Lett 20: 3579-83 (2010)
Bristol-Myers Squibb Research And Development
Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs.
Bioorg Med Chem Lett 20: 3737-41 (2010)
Gedeon Richter
2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR.
Bioorg Med Chem Lett 20: 3540-4 (2010)
Glaxosmithkline
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.
Bioorg Med Chem Lett 20: 3628-31 (2010)
Novartis Institute Of Biomedical Research
Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.
Bioorg Med Chem Lett 20: 3750-4 (2010)
Merck Research Laboratories
Discovery of a novel series of CXCR3 antagonists.
Bioorg Med Chem Lett 20: 3614-7 (2010)
Merck Serono
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
Bioorg Med Chem Lett 20: 3596-600 (2010)
National Health Research Institutes
5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer.
Bioorg Med Chem Lett 20: 3526-9 (2010)
Wyeth Research
Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.
Bioorg Med Chem Lett 20: 3726-9 (2010)
Kitasato University
2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.
Bioorg Med Chem Lett 20: 3545-9 (2010)
Glaxosmithkline
Unexpected reaction of 2-alkylsulfanylimidazoles to imidazol-2-ones: pyridinylimidazol-2-ones as novel potent p38alpha mitogen-activated protein kinase inhibitors.
J Med Chem 53: 4798-802 (2010)
Eberhard Karls University Of Tubingen
Design of selective, ATP-competitive inhibitors of Akt.
J Med Chem 53: 4615-22 (2010)
Pfizer
Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.
J Med Chem 53: 4803-7 (2010)
Universita Di Siena
Rearranged diterpenoids from the biotransformation of ent-trachyloban-18-oic acid by Rhizopus arrhizus.
J Nat Prod 73: 1121-5 (2010)
Centre De Recherche De Gif
Identification and functional characterization of a stable, centrally active derivative of the neurotensin (8-13) fragment as a potential first-in-class analgesic.
J Med Chem 53: 4623-32 (2010)
Medical University Of South Carolina Campus
Structure-activity relationships in human toll-like receptor 7-active imidazoquinoline analogues.
J Med Chem 53: 4450-65 (2010)
University Of Kansas
Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules.
J Med Chem 53: 4793-7 (2010)
Sanford-Burnham Medical Research Institute
Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis.
J Med Chem 53: 4545-9 (2010)
National Tsing Hua University
Identification of the three-dimensional pharmacophore of kappa-opioid receptor agonists.
Bioorg Med Chem 18: 4446-52 (2010)
Kitasato University
Novel tricyclic Delta(2)-isoxazoline and 3-oxo-2-methyl-isoxazolidine derivatives: synthesis and binding affinity at neuronal nicotinic acetylcholine receptor subtypes.
Bioorg Med Chem 18: 4498-508 (2010)
Universit£
New hydroxypyrimidinone-containing sulfonamides as carbonic anhydrase inhibitors also acting as MMP inhibitors.
Bioorg Med Chem Lett 20: 3623-7 (2010)
Lneg
Tyrosinase inhibitory effect of benzoic acid derivatives and their structure-activity relationships.
J Enzyme Inhib Med Chem 25: 812-7 (2010)
Yonsei University
Sialic acid-mimic peptides as hemagglutinin inhibitors for anti-influenza therapy.
J Med Chem 53: 4441-9 (2010)
Keio University
Synthesis and evaluation of new endomorphin-2 analogues containing (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) residues.
J Med Chem 53: 4550-4 (2010)
Universit£
Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators.
Bioorg Med Chem 18: 3875-84 (2010)
Chinese Academy Of Sciences
Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK).
Bioorg Med Chem 18: 4547-59 (2010)
Nycomed Pharma
Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.
Bioorg Med Chem 18: 4459-67 (2010)
Ewha Womans University
On the inhibition of histone deacetylase 8.
Bioorg Med Chem 18: 4103-10 (2010)
University Of Notre Dame
Design and synthesis of new potent anticancer pyrazoles with high FLT3 kinase inhibitory selectivity.
Bioorg Med Chem 18: 3961-73 (2010)
Institute Of Science And Technology
Dammaranes from Gynostemma pentaphyllum and synthesis of their derivatives as inhibitors of protein tyrosine phosphatase 1B.
Bioorg Med Chem 18: 3934-9 (2010)
Chinese Academy Of Sciences
The scope of thallium nitrate oxidative cyclization of chalcones; synthesis and evaluation of isoflavone and aurone analogs for their inhibitory activity against interleukin-5.
Bioorg Med Chem 18: 4441-5 (2010)
Chungnam National University
New aminopropandiol derivatives as orally available and short-acting calcium-sensing receptor antagonists.
Bioorg Med Chem Lett 20: 3809-13 (2010)
Central Pharmaceutical Research Institute
Rapid synthesis of an array of trisubstituted urea-based soluble epoxide hydrolase inhibitors facilitated by a novel solid-phase method.
Bioorg Med Chem Lett 20: 3703-7 (2010)
Boehringer Ingelheim Pharmaceuticals
Design, synthesis and evaluation of 2,4-disubstituted pyrimidines as cholinesterase inhibitors.
Bioorg Med Chem Lett 20: 3606-9 (2010)
University Of Waterloo
Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligands.
Bioorg Med Chem Lett 20: 3636-9 (2010)
Abbott Laboratories
Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV.
Bioorg Med Chem Lett 20: 3601-5 (2010)
Istituto Di Biostrutture E Bioimmagini-Cnr
Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors.
Bioorg Med Chem Lett 20: 3649-53 (2010)
Newcastle University
Novel 8-arylated purines as inhibitors of glycogen synthase kinase.
Eur J Med Chem 45: 3389-93 (2010)
Institut Curie
Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase.
Bioorg Med Chem 18: 4475-84 (2010)
Sun Yat-Sen University
Synthesis and anti-inflammatory activity of new arylidene-thiazolidine-2,4-diones as PPARgamma ligands.
Bioorg Med Chem 18: 3805-11 (2010)
Universidade Federal De Pernambuco
Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents.
Bioorg Med Chem 18: 4138-48 (2010)
Central Drug Research Institute
Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists.
Bioorg Med Chem Lett 20: 3669-74 (2010)
Bristol-Myers Squibb Pharmaceutical Research Institute
The discovery and SAR of indoline-3-carboxamides--a new series of 5-HT6 antagonists.
Bioorg Med Chem Lett 20: 3713-6 (2010)
Schering-Plough Research Institute
Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain.
Bioorg Med Chem Lett 20: 3760-3 (2010)
Merck Frosst Canada
A structure-activity relationship study elucidating the mechanism of sequence-specific collagen recognition by the chaperone HSP47.
Bioorg Med Chem 18: 3767-75 (2010)
Waseda University
Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.
Bioorg Med Chem Lett 20: 3788-92 (2010)
Pfizer
Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists.
Bioorg Med Chem Lett 20: 3742-5 (2010)
Pfizer
Synthesis and biological evaluation of tricyclic anilinopyrimidines as IKKbeta inhibitors.
Bioorg Med Chem Lett 20: 3821-5 (2010)
Pfizer
Biochemical and biophysical characterization of unique switch pocket inhibitors of p38a.
Bioorg Med Chem Lett 20: 5787-92 (2010)
Abbott Laboratories
Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.
Bioorg Med Chem Lett 20: 3746-9 (2010)
Boehringer Ingelheim Pharmaceuticals
Discovery of highly selective inhibitors of human fatty acid binding protein 4 (FABP4) by virtual screening.
Bioorg Med Chem Lett 20: 3675-9 (2010)
Chinese Academy Of Sciences
An isoaurone and other constituents from Trichosanthes kirilowii seeds inhibit hypoxia-inducible factor-1 and nuclear factor-kappaB.
J Nat Prod 73: 1167-9 (2010)
Korean Research Institute Of Biosciences And Biotechnology
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.
J Med Chem 53: 4531-44 (2010)
Glaxosmithkline
Design and synthesis of novel Gefitinib analogues with improved anti-tumor activity.
Bioorg Med Chem 18: 3812-22 (2010)
Southeast University
Synthesis and in vitro toxicity of 4-MTA, its characteristic clandestine synthesis byproducts and related sulfur substituted alpha-alkylthioamphetamines.
Bioorg Med Chem 18: 4009-31 (2010)
Trinity College
Regiospecific and conformationally restrained analogs of melphalan and DL-2-NAM-7 and their affinities for the large neutral amino acid transporter (system LAT1) of the blood-brain barrier.
Bioorg Med Chem Lett 20: 3688-91 (2010)
University Of Kentucky
1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives: a novel type II Raf kinase inhibitors.
Bioorg Med Chem Lett 20: 3805-8 (2010)
Institute Of Science And Technology
Quinolines and structurally related heterocycles as antimalarials.
Eur J Med Chem 45: 3245-64 (2010)
National Institute Of Pharmaceutical Education And Research
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).
J Med Chem 53: 4379-89 (2010)
Siena Biotech
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
J Med Chem 53: 4481-7 (2010)
Amgen
Human cytochrome P450 2E1 structures with fatty acid analogs reveal a previously unobserved binding mode.
J Biol Chem 285: 22282-90 (2010)
The University Of Kansas
Inhibition of Mycobacterium tuberculosis tyrosine phosphatase PtpA by synthetic chalcones: kinetics, molecular modeling, toxicity and effect on growth.
Bioorg Med Chem 18: 3783-9 (2010)
Universidade Federal De Santa Catarina
Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.
Bioorg Med Chem Lett 20: 3235-9 (2010)
Boehringer Ingelheim Pharmaceuticals
Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity.
Bioorg Med Chem Lett 20: 3211-5 (2010)
Pukyong National University
Cryptosphaerolide, a cytotoxic Mcl-1 inhibitor from a marine-derived ascomycete related to the genus Cryptosphaeria.
J Nat Prod 73: 998-1001 (2010)
University Of California San Diego
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.
J Med Chem 53: 4367-78 (2010)
Cyclacel
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
J Med Chem 53: 4522-30 (2010)
Glaxosmithkline
Rational design of a topical androgen receptor antagonist for the suppression of sebum production with properties suitable for follicular delivery.
J Med Chem 53: 4422-7 (2010)
Pfizer
Biochemical and structural analysis of the binding determinants of a vascular endothelial growth factor receptor peptidic antagonist.
J Med Chem 53: 4428-40 (2010)
University Of Paris
Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231).
J Med Chem 53: 4511-21 (2010)
Pfizer
Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index.
J Med Chem 53: 4502-10 (2010)
Amgen
Lipophilic bisphosphonates are potent inhibitors of Plasmodium liver-stage growth.
Antimicrob Agents Chemother 54: 2987-93 (2010)
National Institute Of Immunology
2,5-Dideoxy-2,5-imino-d-altritol as a new class of pharmacological chaperone for Fabry disease.
Bioorg Med Chem 18: 3790-4 (2010)
University Of Toyama
Synthesis and structure-activity relationships of 2-acylamino-4,6-diphenylpyridine derivatives as novel antagonists of GPR54.
Bioorg Med Chem 18: 3841-59 (2010)
Takeda Pharmaceutical
In vitro studies on a class of quinoline containing histamine H3 antagonists.
Bioorg Med Chem Lett 20: 3295-300 (2010)
Abbott Laboratories
Discovery of a new potent bisamide FMS kinase inhibitor.
Bioorg Med Chem Lett 20: 3216-8 (2010)
Institute Of Science And Technology
3-Indolyl sultams as selective CRTh2 antagonists.
Bioorg Med Chem Lett 20: 3287-90 (2010)
Athersys
Discovery of TRPV1 antagonist ABT-116.
Bioorg Med Chem Lett 20: 3291-4 (2010)
Abbott Laboratories
Synthesis, SAR and evaluation of [1,4']-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists.
Bioorg Med Chem Lett 20: 3219-22 (2010)
Roche Palo Alto
Structure-activity relationships of carbocyclic 6-benzylthioinosine analogues as subversive substrates of Toxoplasma gondii adenosine kinase.
Bioorg Med Chem 18: 3403-12 (2010)
University Of Georgia
Serotonin derivatives as a new class of non-ATP-competitive receptor tyrosine kinase inhibitors.
Bioorg Med Chem 18: 3387-402 (2010)
Universit£T Leipzig
Site-activated chelators targeting acetylcholinesterase and monoamine oxidase for Alzheimer's therapy.
ACS Chem Biol 5: 603-10 (2010)
The Weizmann Institute Of Science
Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis.
J Med Chem 53: 4412-21 (2010)
Arena Pharmaceuticals
Synthesis and characterization of potent inhibitors of Trypanosoma cruzi dihydrofolate reductase.
Bioorg Med Chem 18: 4056-66 (2010)
University Of Alabama
Synthesis of 4-[(diethylamino)methyl]-phenol derivatives as novel cholinesterase inhibitors with selectivity towards butyrylcholinesterase.
Bioorg Med Chem Lett 20: 3254-8 (2010)
Sun Yat-Sen University
Synthesis of neurotensin(8-13)-phosphopeptide heterodimers via click chemistry.
Bioorg Med Chem Lett 20: 3306-9 (2010)
Institute Of Radiopharmacy
Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles.
Bioorg Med Chem Lett 20: 3265-71 (2010)
University Of Edinburgh
Studies on two types of PTP1B inhibitors for the treatment of type 2 diabetes: Hologram QSAR for OBA and BBB analogues.
Bioorg Med Chem Lett 20: 3329-37 (2010)
Tsinghua University
Identification of new non-carboxylic acid containing inhibitors of aldose reductase.
Bioorg Med Chem 18: 4049-55 (2010)
University Of Messina
Analogs of zanamivir with modified C4-substituents as the inhibitors against the group-1 neuraminidases of influenza viruses.
Bioorg Med Chem 18: 4074-84 (2010)
National Taiwan University
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
Bioorg Med Chem 18: 3925-33 (2010)
Kansai University
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
Bioorg Med Chem 18: 4119-37 (2010)
Mcgill University
New potent inhibitors of tyrosinase: novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site.
Bioorg Med Chem 18: 4042-8 (2010)
King Saud University
Structural determinants for the inhibitory ligands of orotidine-5'-monophosphate decarboxylase.
Bioorg Med Chem 18: 4032-41 (2010)
University Health Network
Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.
Bioorg Med Chem Lett 20: 3367-71 (2010)
Johnson & Johnson Pharmaceutical Research & Development
Glycine amides as PPARalpha agonists.
Bioorg Med Chem Lett 20: 3376-9 (2010)
Bayer-Schering Pharma
Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.
Bioorg Med Chem Lett 20: 3372-5 (2010)
Merck Research Laboratories
Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines.
Bioorg Med Chem 18: 3910-24 (2010)
Universit£
Synthesis and NMDA receptor affinity of fluorinated dioxadrol analogues.
Bioorg Med Chem 18: 4095-102 (2010)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhems-Universit£T M£Nster
Dual Src and Abl inhibitors target wild type Abl and the AblT315I Imatinib-resistant mutant with different mechanisms.
Bioorg Med Chem 18: 3999-4008 (2010)
Institute Of Molecular Genetics Igm-Cnr
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
Bioorg Med Chem Lett 20: 3314-21 (2010)
S*Bio
Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.
J Med Chem 53: 4399-411 (2010)
Biotie Therapies
Pyrimidine ribonucleotides with enhanced selectivity as P2Y(6) receptor agonists: novel 4-alkyloxyimino, (S)-methanocarba, and 5'-triphosphate gamma-ester modifications.
J Med Chem 53: 4488-501 (2010)
National Institute Of Diabetes And Digestive And Kidney Diseases
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
J Med Chem 53: 4198-211 (2010)
Actelion Pharmaceuticals
Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT(1) melatoninergic ligands.
Bioorg Med Chem 18: 3426-36 (2010)
University Of Lille
Flexible ligand recognition of peroxisome proliferator-activated receptor-gamma (PPARgamma).
Bioorg Med Chem Lett 20: 3344-7 (2010)
Rikkyo University
Anthranilic acid replacements in a niacin receptor agonist.
Bioorg Med Chem Lett 20: 3426-30 (2010)
Merck
Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility.
BMC Chem Biol 10: 5 (2010)
University Of Pittsburgh
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
J Med Chem 53: 4066-84 (2010)
Pfizer
BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
J Med Chem 53: 4166-76 (2010)
Sanford-Burnham Medical Research Institute
1-(2-Ethoxyethyl)-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors.
Bioorg Med Chem Lett 20: 3120-4 (2010)
Pfizer
3D-QSAR study of benzene sulfonamide analogs as carbonic anhydrase II inhibitors.
Bioorg Med Chem Lett 20: 3089-93 (2010)
Gitam University
Cyclopeptide Smac mimetics as antagonists of IAP proteins.
Bioorg Med Chem Lett 20: 3043-6 (2010)
University Of Michigan
Synthesis and SAR of novel isoquinoline CXCR4 antagonists with potent anti-HIV activity.
Bioorg Med Chem Lett 20: 3026-30 (2010)
Glaxosmithkline
Vaccinia virus virulence factor N1L is a novel promising target for antiviral therapeutic intervention.
J Med Chem 53: 3899-906 (2010)
Institute For Medical Research
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
J Med Chem 53: 4212-22 (2010)
Wilhelms-Universit£T M£Nster
2-aminoimidazole amino acids as inhibitors of the binuclear manganese metalloenzyme human arginase I.
J Med Chem 53: 4266-76 (2010)
University Of Pennsylvania
Novel irreversible fluorescent probes targeting the 18 kDa translocator protein: synthesis and biological characterization.
J Med Chem 53: 4085-93 (2010)
Universit£
Mechanism-based inhibitors of the aspartyl protease plasmepsin II as potential antimalarial agents.
J Med Chem 53: 4234-47 (2010)
Wayne State University
N-Hydroxybenzimidazole inhibitors of ExsA MAR transcription factor in Pseudomonas aeruginosa: In vitro anti-virulence activity and metabolic stability.
Bioorg Med Chem Lett 20: 3380-3 (2010)
Paratek Pharmaceuticals
Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism.
Bioorg Med Chem Lett 20: 3436-40 (2010)
Roche Palo Alto
Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: Pyridazinylmethylphenyl glucoside congeners.
Bioorg Med Chem Lett 20: 3420-5 (2010)
Green Cross
Synthesis of novel peptidomimetics as inhibitors of protozoan cysteine proteases falcipain-2 and rhodesain.
Eur J Med Chem 45: 3228-33 (2010)
University Of Messina
Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.
Bioorg Med Chem Lett 20: 3361-6 (2010)
Kalypsys
A vHTS approach for the identification of beta-adrenoceptor ligands.
Bioorg Med Chem Lett 20: 3399-404 (2010)
4Sc
NO-releasing esters show carbonic anhydrase inhibitory action against human isoforms I and II.
Bioorg Med Chem 18: 3559-63 (2010)
Atat£Rk University
1-(3-Deoxy-3-fluoro-beta-d-glucopyranosyl) pyrimidine derivatives as inhibitors of glycogen phosphorylase b: Kinetic, crystallographic and modelling studies.
Bioorg Med Chem 18: 3413-25 (2010)
National Hellenic Research Foundation
Virtual screening, selection and development of a benzindolone structural scaffold for inhibition of lumazine synthase.
Bioorg Med Chem 18: 3518-34 (2010)
Purdue University
8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors.
Bioorg Med Chem Lett 20: 3356-60 (2010)
Cephalon
Optimisation of a pyrazole series of progesterone antagonists; Part 1.
Bioorg Med Chem Lett 20: 3384-6 (2010)
Pfizer
Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands.
Bioorg Med Chem Lett 20: 3405-8 (2010)
F. Hoffmann-La Roche
Carbocyclic potential DNA minor groove binders and their biological evaluation.
J Enzyme Inhib Med Chem 25: 629-34 (2010)
Medical University
Second generation analogues of the cancer drug clinical candidate tipifarnib for anti-Chagas disease drug discovery.
J Med Chem 53: 3887-98 (2010)
University Of Washington
A collection of caged compounds for probing roles of local translation in neurobiology.
Bioorg Med Chem 18: 7746-52 (2010)
University Of Toronto
5-Functionalized indazoles as glucocorticoid receptor agonists.
Bioorg Med Chem Lett 20: 3017-20 (2010)
Amri
5D-QSAR for spirocyclic sigma1 receptor ligands by Quasar receptor surface modeling.
Eur J Med Chem 45: 3116-24 (2010)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Colloid formation by drugs in simulated intestinal fluid.
J Med Chem 53: 4259-65 (2010)
University Of California San Francisco
Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.
J Nat Prod 73: 988-91 (2010)
Griffith University
Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237.
ACS Chem Biol 5: 563-76 (2010)
University Of Sheffield
Creating an antibacterial with in vivo efficacy: synthesis and characterization of potent inhibitors of the bacterial cell division protein FtsZ with improved pharmaceutical properties.
J Med Chem 53: 3927-36 (2010)
Biota Europe
Iminochromene inhibitors of dynamins I and II GTPase activity and endocytosis.
J Med Chem 53: 4094-102 (2010)
The University Of Newcastle
Inhibition of the Fe(4)S(4)-cluster-containing protein IspH (LytB): electron paramagnetic resonance, metallacycles, and mechanisms.
J Am Chem Soc 132: 6719-27 (2010)
University Of Illinois At Urbana-Champaign
The alternative medicine pawpaw and its acetogenin constituents suppress tumor angiogenesis via the HIF-1/VEGF pathway.
J Nat Prod 73: 956-61 (2010)
University Of Mississippi
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
J Med Chem 53: 4028-37 (2010)
Merck Research Laboratories
Substrate selectivity and a novel role in inhibitor discrimination by residue 237 in the KPC-2 beta-lactamase.
Antimicrob Agents Chemother 54: 2867-77 (2010)
Case Western Reserve University
Polyamines in drug discovery: from the universal template approach to the multitarget-directed ligand design strategy.
J Med Chem 53: 5906-14 (2010)
University Of Bologna
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.
J Med Chem 53: 3973-4001 (2010)
Glaxosmithkline
Synthesis and evaluation of benzoxazinone derivatives on activity of human neutrophil elastase and on hemorrhagic shock-induced lung injury in rats.
Eur J Med Chem 45: 3111-5 (2010)
Chang Gung University
Design of new potent and selective secretory phospholipase A(2) inhibitors. 6-Synthesis, structure-activity relationships and molecular modelling of 1-substituted-4-[4,5-dihydro-1,2,4-(4H)-oxadiazol-5-one-3-yl(methyl)]-functionalized aryl piperazin/one/dione derivatives.
Bioorg Med Chem 18: 3588-600 (2010)
Universit£
Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists.
Bioorg Med Chem Lett 20: 3116-9 (2010)
Roche Palo Alto
Utilization of an in vivo reporter for high throughput identification of branched small molecule regulators of hypoxic adaptation.
Chem Biol 17: 380-91 (2010)
Weill Medical College Of Cornell University
Novel estrone mimetics with high 17beta-HSD1 inhibitory activity.
Bioorg Med Chem 18: 3494-505 (2010)
Saarland University And Helmholtz Institute For Pharmaceutical Research Saarland (Hips)
Functionalized pyrazoles and pyrazolo[3,4-d]pyridazinones: Synthesis and evaluation of their phosphodiesterase 4 inhibitory activity.
Bioorg Med Chem 18: 3506-17 (2010)
Universit£
Synthesis and opioid activity of novel 6-substituted-6-demethoxy-ethenomorphinans.
Bioorg Med Chem 18: 3535-42 (2010)
University Of Debrecen
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Bioorg Med Chem Lett 20: 3050-64 (2010)
Johns Hopkins University
Synthesis of DOTA-conjugated multimeric [Tyr3]octreotide peptides via a combination of Cu(I)-catalyzed"click" cycloaddition and thio acid/sulfonyl azide"sulfo-click" amidation and their in vivo evaluation.
J Med Chem 53: 3944-53 (2010)
Utrecht University
Structure-activity relationships of fluorinated (E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-enone-O-methyloxime (ABP688) derivatives and the discovery of a high affinity analogue as a potential candidate for imaging metabotropic glutamate recepors subtype 5 (mGluR5) with positron emission tomog
J Med Chem 53: 4009-17 (2010)
Eth Zurich
Discovery of GS-9131: Design, synthesis and optimization of amidate prodrugs of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148.
Bioorg Med Chem 18: 3606-17 (2010)
Gilead Sciences
Synthesis and binding analysis of unique AG2 pentasaccharide to human Siglec-2 using NMR techniques.
Bioorg Med Chem 18: 3720-5 (2010)
Institute
3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.
Bioorg Med Chem Lett 20: 3129-33 (2010)
Merck Research Laboratories
Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.
Bioorg Med Chem Lett 20: 3173-6 (2010)
University Of Regensburg
Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold.
Eur J Med Chem 45: 2919-27 (2010)
Technische Universit£T Braunschweig
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines.
J Med Chem 53: 4300-4 (2010)
Pfizer
Lessons learned from herbal medicinal products: the example of St. John's Wort (perpendicular).
J Nat Prod 73: 1015-21 (2010)
Westfalische Wilhelms-Universitat
Structure-activity relationships of 6-methyl-benzo[b]thiophene-2-carboxylic acid (1-[(S)-1-benzyl-4-[4-(tetrahydropyran-4-ylmethyl)piperazin-1-yl]butylcarbamoyl]cyclopentyl)amide, potent antagonist of the neurokinin-2 receptor.
J Med Chem 53: 4148-65 (2010)
Menarini Ricerche
Synthesis and evaluation of 17alpha-arylestradiols as ligands for estrogen receptor alpha and beta.
J Med Chem 53: 4290-4 (2010)
Academy Of Sciences Of The Czech Republic
Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation.
J Med Chem 53: 3954-63 (2010)
Universit£
4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.
J Med Chem 53: 4110-8 (2010)
Universit£
Function-oriented synthesis of simplified caprazamycins: discovery of oxazolidine-containing uridine derivatives as antibacterial agents against drug-resistant bacteria.
J Med Chem 53: 3793-813 (2010)
Hokkaido University
Structure-based discovery of A2A adenosine receptor ligands.
J Med Chem 53: 3748-55 (2010)
University Of California
Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.
J Nat Prod 73: 980-4 (2010)
University Of Basel
Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).
J Med Chem 53: 3814-30 (2010)
Bristol-Myers Squibb Research And Development
Design, synthesis, and interaction study of quinazoline-2(1H)-thione derivatives as novel potential Bcl-xL inhibitors.
J Med Chem 53: 3465-79 (2010)
Chinese Academy Of Sciences
Comparison of in vitro activities of fluoroquinolone-like 2,4- and 1,3-diones.
Antimicrob Agents Chemother 54: 3011-4 (2010)
University Of Minnesota Medical School
Specificity of induction of the vanA and vanB operons in vancomycin-resistant enterococci by telavancin.
Antimicrob Agents Chemother 54: 2814-8 (2010)
Theravance
Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.
Bioorg Med Chem 18: 3575-87 (2010)
Duquesne University
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility.
Bioorg Med Chem Lett 20: 3039-42 (2010)
Pfizer
The contribution of a 2-amino group on receptor tyrosine kinase inhibition and antiangiogenic activity in 4-anilinosubstituted pyrrolo[2,3-d]pyrimidines.
Bioorg Med Chem Lett 20: 3177-81 (2010)
Duquesne University
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
J Med Chem 53: 3675-84 (2010)
Novartis Institutes For Biomedical Research
1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors.
Bioorg Med Chem Lett 20: 3125-8 (2010)
Pfizer
Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads.
Bioorg Med Chem Lett 20: 3158-60 (2010)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.
Bioorg Med Chem Lett 20: 3161-4 (2010)
Glaxosmithkline
Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one.
Bioorg Med Chem Lett 20: 3182-5 (2010)
Bristol-Myers Squibb
Investigation of the bioactive conformation of histamine H3 receptor antagonists by the cyclopropylic strain-based conformational restriction strategy.
J Med Chem 53: 3585-93 (2010)
Hokkaido University
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.
J Med Chem 53: 3532-51 (2010)
Nerviano Medical Sciences
Synthesis, characterization and vasculoprotective effects of nitric oxide-donating derivatives of chrysin.
Bioorg Med Chem 18: 3020-5 (2010)
Central South University
Anti-microtubule 'plinabulin' chemical probe KPU-244-B3 labeled both alpha- and beta-tubulin.
Bioorg Med Chem 18: 3169-74 (2010)
Tokyo University Of Pharmacy And Life Sciences
Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase.
Bioorg Med Chem Lett 20: 3146-9 (2010)
Pfizer
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
J Med Chem 53: 3454-64 (2010)
University Of Southern California
Merging the structural motifs of functionalized amino acids and alpha-aminoamides: compounds with significant anticonvulsant activities.
J Med Chem 53: 3756-71 (2010)
University Of North Carolina
Frontal affinity chromatography-mass spectrometry useful for characterization of new ligands for GPR17 receptor.
J Med Chem 53: 3489-501 (2010)
University Of Pavia
Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist.
Bioorg Med Chem Lett 20: 3107-11 (2010)
Pfizer
Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides.
Bioorg Med Chem Lett 20: 3142-5 (2010)
Takeda California
Benzimidazole and imidazole inhibitors of histone deacetylases: Synthesis and biological activity.
Bioorg Med Chem Lett 20: 3138-41 (2010)
Takeda California
Mono-, di-, and triaryl substituted tetrahydropyrans as cyclooxygenase-2 and tumor growth inhibitors. Synthesis and biological evaluation.
J Med Chem 53: 3707-17 (2010)
Guru Nanak Dev University
A nonazole CYP51 inhibitor cures Chagas' disease in a mouse model of acute infection.
Antimicrob Agents Chemother 54: 2480-8 (2010)
University Of California
Discovery of PDK1 kinase inhibitors with a novel mechanism of action by ultrahigh throughput screening.
J Biol Chem 285: 18838-46 (2010)
Merck Research Laboratories
3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. Part 3: Synthesis, metabolic stability, and biological evaluation of optically active analogs.
Bioorg Med Chem 18: 3212-23 (2010)
Minase Research Institute
Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists.
Bioorg Med Chem 18: 3078-87 (2010)
Monash University
Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.
J Med Chem 53: 3840-4 (2010)
Meiji Seika Kaisha
Glutarimide alkaloids and a terpenoid benzoquinone from Cordia globifera.
J Nat Prod 73: 992-4 (2010)
Chulabhorn Research Institute
Cytotoxic and NF-kappaB inhibitory constituents of Artocarpus rigida.
J Nat Prod 73: 949-55 (2010)
The Ohio State University
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.
Nat Chem Biol 6: 359-68 (2010)
Dana-Farber Cancer Institute
Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.
Bioorg Med Chem 18: 3026-35 (2010)
National Institute On Drug Abuse-Intramural Research Program
In silico directed chemical probing of the adenosine receptor family.
Bioorg Med Chem 18: 3043-52 (2010)
Universidade Do Minho
Antagonism of 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates toward voltage-dependent L-type Ca2+ channels Ca V 1.3 and Ca V 1.2.
Bioorg Med Chem 18: 3147-58 (2010)
Northwestern University
Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers.
Bioorg Med Chem Lett 20: 2705-8 (2010)
Institute Of Science And Technology
Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.
Bioorg Med Chem Lett 20: 2998-3002 (2010)
Bristol-Myers Squibb Research And Development
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
Bioorg Med Chem Lett 20: 2903-7 (2010)
Wyeth Pharmaceuticals
Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.
Bioorg Med Chem Lett 20: 2755-60 (2010)
Johnson & Johnson Pharmaceutical Research & Development
Chromone-2- and -3-carboxylic acids inhibit differently monoamine oxidases A and B.
Bioorg Med Chem Lett 20: 2709-12 (2010)
Universit£
In vitro TRPV1 activity of piperine derived amides.
Bioorg Med Chem 18: 3299-306 (2010)
Universidad De Antioquia
Design of pentapeptidic BACE1 inhibitors with carboxylic acid bioisosteres at P1' and P4 positions.
Bioorg Med Chem 18: 3175-86 (2010)
Kyoto Pharmaceutical University
Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.
Bioorg Med Chem 18: 3159-68 (2010)
Chugai Pharmaceutical
Synthesis and biological activity of cyclotetrapeptide analogues of the natural HDAC inhibitor FR235222.
Bioorg Med Chem 18: 3252-60 (2010)
Universit£
KDR Kinase Inhibitor Isolated from the Mushroom Boletopsis leucomelas.
J Nat Prod 73: 1002-4 (2010)
Meiji Pharmaceutical University
Discovery of novel and potent leukotriene B4 receptor antagonists. Part 1.
J Med Chem 53: 3502-16 (2010)
Roche Research Center
Elaborate ligand-based pharmacophore exploration and QSAR analysis guide the synthesis of novel pyridinium-based potent beta-secretase inhibitory leads.
Bioorg Med Chem 18: 3088-115 (2010)
Applied Science University
3'-(1,2,3-Triazol-1-yl)-3'-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations.
Bioorg Med Chem 18: 3261-9 (2010)
Swedish University Agricultural Sciences
Water-soluble PDE4 inhibitors for the treatment of dry eye.
Bioorg Med Chem Lett 20: 2928-32 (2010)
Kalypsys
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.
Bioorg Med Chem Lett 20: 2809-12 (2010)
Wyeth Research
Synthesis and biological activity of 2H-quinolizin-2-one based p38alpha MAP kinase inhibitors.
Bioorg Med Chem Lett 20: 2765-9 (2010)
Merck Research Laboratories
(-)-Menthylamine derivatives as potent and selective antagonists of transient receptor potential melastatin type-8 (TRPM8) channels.
Bioorg Med Chem Lett 20: 2729-32 (2010)
Sapienza University Of Rome
Pyrazolylthiazole as DeltaF508-cystic fibrosis transmembrane conductance regulator correctors with improved hydrophilicity compared to bithiazoles.
J Med Chem 53: 3772-81 (2010)
University Of California Davis
The identification of a novel natural activator of p300 histone acetyltranferase provides new insights into the modulation mechanism of this enzyme.
Chembiochem 11: 818-27 (2010)
Universitá
Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
Bioorg Med Chem 18: 3231-7 (2010)
Peking University
Cytotoxicity and inhibition of DNA topoisomerase I of polyhydroxylated triterpenoids and triterpenoid glycosides.
Bioorg Med Chem Lett 20: 2790-6 (2010)
Stephen F. Austin State University
Discovery of novel leukotriene A4 hydrolase inhibitors based on piperidine and piperazine scaffolds.
Bioorg Med Chem Lett 20: 2851-4 (2010)
Decode Chemistry
Synthesis of 7-benzyl-5-(piperidin-1-yl)-6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c][2,7]naphthyridin-1-ylamine and its analogs as bombesin receptor subtype-3 agonists.
Bioorg Med Chem Lett 20: 2785-9 (2010)
Amri
Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines as A2B receptor antagonists.
Eur J Med Chem 45: 2884-92 (2010)
Universidade De A Coru£A
Bradykinin B1 receptor antagonists as potential therapeutic agents for pain.
J Med Chem 53: 5383-99 (2010)
Johnson & Johnson Pharmaceutical Research And Development
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.
J Med Chem 53: 4561-84 (2010)
Johns Hopkins University Brain Science Institute
Sugar-based peptidomimetics as potential inhibitors of the vascular endothelium growth factor binding to neuropilin-1.
Bioorg Med Chem 18: 3285-98 (2010)
Nancy Universit£-Cnrs
Prenylated pterocarpans as bacterial neuraminidase inhibitors.
Bioorg Med Chem 18: 3335-44 (2010)
Chosun University
Identification of serotonin 5-HT1A receptor partial agonists in ginger.
Bioorg Med Chem 18: 3345-51 (2010)
Department Of Chemistry And Applied Biosciences
Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation.
Bioorg Med Chem 18: 3307-19 (2010)
Pfizer
Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B.
Bioorg Med Chem Lett 20: 2876-9 (2010)
Chinese Academy Of Sciences
Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.
Bioorg Med Chem Lett 20: 2801-5 (2010)
Universit£
Identification of a novel series of potent RON receptor tyrosine kinase inhibitors.
Bioorg Med Chem Lett 20: 2745-9 (2010)
Methylgene
Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
Bioorg Med Chem Lett 20: 2797-800 (2010)
Arena Pharmaceuticals
Synthesis of a biologically active isomer of kotalanol, a naturally occurring glucosidase inhibitor.
Bioorg Med Chem 18: 2829-35 (2010)
Simon Fraser University
Exploration of secondary and tertiary pharmacophores in unsymmetrical N,N'-diaryl urea inhibitors of soluble epoxide hydrolase.
Bioorg Med Chem Lett 20: 2740-4 (2010)
Ar£Te Therapeutics
Probing the cannabinoid CB1/CB2 receptor subtype selectivity limits of 1,2-diarylimidazole-4-carboxamides by fine-tuning their 5-substitution pattern.
Bioorg Med Chem Lett 20: 2770-5 (2010)
Solvay Pharma
Design of new dopamine D2 receptor ligands: biosynthesis and pharmacological evaluation of the hydroxylated metabolite of LASSBio-581.
Bioorg Med Chem Lett 20: 2888-91 (2010)
Universidade Federal De Goi£S
Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.
Bioorg Med Chem Lett 20: 2924-7 (2010)
Wyeth Research
The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.
Bioorg Med Chem Lett 20: 2897-902 (2010)
Pfizer
Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents.
J Med Chem 53: 3611-7 (2010)
Friedrich-Schiller-Universitat Jena
5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity.
J Med Chem 53: 3696-706 (2010)
Institute Of Science And Technology
A prodrug approach towards the development of tricyclic-based FBPase inhibitors.
Bioorg Med Chem Lett 20: 2938-41 (2010)
Daiichi Sankyo
Targeting multiple chorismate-utilizing enzymes with a single inhibitor: validation of a three-stage design.
J Med Chem 53: 3718-29 (2010)
University Of California
Synthesis and anti-tumor activities of methyl 2-O-aryl-6-O-aryl'-D-glucopyranosides.
Bioorg Med Chem Lett 20: 2855-8 (2010)
Ocean University Of China
Imidazoacridin-6-ones as novel inhibitors of the quinone oxidoreductase NQO2.
Bioorg Med Chem Lett 20: 2832-6 (2010)
The University Of Manchester And Manchester Cancer Research Center
Synthesis and structure-activity relationships of 2-aryl-4-oxazolylmethoxy benzylglycines and 2-aryl-4-thiazolylmethoxy benzylglycines as novel, potent PPARalpha selective activators- PPARalpha and PPARgamma selectivity modulation.
Bioorg Med Chem Lett 20: 2933-7 (2010)
Bristol-Myers Squibb R & D
Novel benzimidazole-pyrimidine conjugates as potent antitumor agents.
Eur J Med Chem 45: 2336-44 (2010)
National Research Centre
Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.
J Med Chem 53: 5085-107 (2010)
Ferrara University
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
J Med Chem 53: 5367-82 (2010)
Novartis Pharma
A novel class of antihyperlipidemic agents with low density lipoprotein receptor up-regulation via the adaptor protein autosomal recessive hypercholesterolemia.
J Med Chem 53: 3284-95 (2010)
Dainippon Sumitomo Pharma
Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor.
J Med Chem 53: 3517-31 (2010)
Takeda Pharmaceutical
Imaging progesterone receptor in breast tumors: synthesis and receptor binding affinity of fluoroalkyl-substituted analogues of tanaproget.
J Med Chem 53: 3349-60 (2010)
University Of Illinois
Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships.
J Med Chem 53: 3417-21 (2010)
University Of Copenhagen
Design, synthesis and anticholinesterase activity of some new a-aminobisphosphonates.
J Enzyme Inhib Med Chem 25: 827-35 (2010)
Tarbiat Modares University
A series of alpha-heterocyclic carboxaldehyde thiosemicarbazones inhibit topoisomerase IIalpha catalytic activity.
J Med Chem 53: 3048-64 (2010)
Chinese Academy Of Sciences
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
Antimicrob Agents Chemother 54: 2603-10 (2010)
Kenya Medical Research Institute/Wellcome Trust Collaborative Research Program
Non-classical antifolates. Part 2: synthesis, biological evaluation, and molecular modeling study of some new 2,6-substituted-quinazolin-4-ones.
Bioorg Med Chem 18: 2849-63 (2010)
King Saud University
Bivalent 5,8,9,13b-tetrahydro-6H-isoquino[1,2-a]isoquinolines and -isoquinolinium salts: novel heterocyclic templates for butyrylcholinesterase inhibitors.
Bioorg Med Chem Lett 20: 2946-9 (2010)
Friedrich-Schiller-Universit£T Jena
Molecular modelling, synthesis and acetylcholinesterase inhibition of ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate.
Bioorg Med Chem Lett 20: 2950-3 (2010)
Laboratorio De Radicales Libres Y QuÍMica Computacional (Iqog, Csic)
Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta.
Bioorg Med Chem Lett 20: 2958-63 (2010)
Technische Universit£T Darmstadt
A rapid oxime linker-based library approach to identification of bivalent inhibitors of the Yersinia pestis protein-tyrosine phosphatase, YopH.
Bioorg Med Chem Lett 20: 2813-6 (2010)
National Cancer Institute-Frederick
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
J Med Chem 53: 3296-304 (2010)
Wyeth Pharmaceuticals
Pharmacophore development and application toward the identification of novel, small-molecule autotaxin inhibitors.
J Med Chem 53: 3095-105 (2010)
The University Of Memphis
Solution phase parallel synthesis of substituted 3-phenylsulfonyl-[1,2,3]triazolo[1,5-a]quinazolines: selective serotonin 5-HT(6) receptor antagonists.
J Comb Chem 12: 445-52 (2010)
Chemical Diversity Research Institute
Truxillic acid derivatives act as peroxisome proliferator-activated receptor gamma activators.
Bioorg Med Chem Lett 20: 2920-3 (2010)
Goethe-University Frankfurt
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.
Bioorg Med Chem Lett 20: 2837-42 (2010)
Merck Research Laboratories
New aromatic monoesters of alpha-aminoaralkylphosphonic acids as inhibitors of aminopeptidase N/CD13.
Bioorg Med Chem 18: 2930-6 (2010)
Wroclaw University Of Technology
Synthesis and structure-activity relationship studies of peptidomimetic PKB/Akt inhibitors: the significance of backbone interactions.
Bioorg Med Chem 18: 2976-85 (2010)
The Hebrew University Of Jerusalem
Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.
Bioorg Med Chem Lett 20: 2864-7 (2010)
Johnson & Johnson Pharmaceutical Research And Development
Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction.
Bioorg Med Chem Lett 20: 2987-90 (2010)
Lehigh University
New 5-HT(1A) receptor ligands containing a N'-cyanoisonicotinamidine nucleus: synthesis and in vitro pharmacological evaluation.
Bioorg Med Chem Lett 20: 2978-82 (2010)
Universit£
Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia.
Bioorg Med Chem Lett 20: 2983-6 (2010)
Wyeth Research
The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.
Bioorg Med Chem Lett 20: 2916-9 (2010)
Neurocrine Biosciences
Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.
Bioorg Med Chem Lett 20: 2912-5 (2010)
Amri
Synthesis and biological evaluation of novel 2-arylalkylthio-4-amino-6-benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
Bioorg Med Chem Lett 20: 3003-5 (2010)
Capital Medical University
Efficient synthesis and identification of novel propane-1,3-diamino bridged CCR5 antagonists with variation on the basic center carrier.
Eur J Med Chem 45: 2827-40 (2010)
Institute Of Materia Medica
Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae.
Bioorg Med Chem 18: 2912-9 (2010)
The University Of Queensland
A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.
Bioorg Med Chem Lett 20: 2474-7 (2010)
Merck Research Laboratories
gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.
Bioorg Med Chem Lett 20: 2425-30 (2010)
Bristol-Myers Squibb
Discovery of novel N-acylsulfonamide analogs as potent and selective EP3 receptor antagonists.
Bioorg Med Chem Lett 20: 2639-43 (2010)
Minase Research Institute
The development and validation of a novel virtual screening cascade protocol to identify potential serotonin 5-HT(7)R antagonists.
Bioorg Med Chem Lett 20: 2465-8 (2010)
Polish Academy Of Sciences
Amide-based inhibitors of p38alpha MAP kinase. Part 2: design, synthesis and SAR of potent N-pyrimidyl amides.
Bioorg Med Chem Lett 20: 2560-3 (2010)
Scios
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Bioorg Med Chem Lett 20: 2408-11 (2010)
Genentech
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
Bioorg Med Chem Lett 20: 2452-5 (2010)
Abbott Laboratories
Curcumin derivatives inhibit testicular 17beta-hydroxysteroid dehydrogenase 3.
Bioorg Med Chem Lett 20: 2549-51 (2010)
School Of Pharmacy
Amide-based inhibitors of p38alpha MAP kinase. Part 1: discovery of novel N-pyridyl amide lead molecules.
Bioorg Med Chem Lett 20: 2556-9 (2010)
Scios
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
J Med Chem 53: 3412-6 (2010)
Glaxosmithkline
Hybrid ortho/allosteric ligands for the adenosine A(1) receptor.
J Med Chem 53: 3028-37 (2010)
Leiden University
Optimization of arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.
Bioorg Med Chem Lett 20: 2868-71 (2010)
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors.
Bioorg Med Chem Lett 20: 2443-7 (2010)
S*Bio
The effect of the pyridyl nitrogen position in pyridylpiperazine sigma ligands.
Bioorg Med Chem Lett 20: 2564-5 (2010)
University Of Maryland
A structure-guided approach to creating covalent FGFR inhibitors.
Chem Biol 17: 285-95 (2010)
Harvard Medical School
2-MeS-beta,gamma-CCl2-ATP is a potent agent for reducing intraocular pressure.
J Med Chem 53: 3305-19 (2010)
Bar-Ilan University
Removal of sphingosine 1-phosphate receptor-3 (S1P(3)) agonism is essential, but inadequate to obtain immunomodulating 2-aminopropane-1,3-diol S1P(1) agonists with reduced effect on heart rate.
J Med Chem 53: 3154-68 (2010)
Mitsubishi Tanabe Pharma
Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.
J Med Chem 53: 3142-53 (2010)
Abbott Laboratories
Design, synthesis and evaluation of novel 2-thiophen-5-yl-3H-quinazolin-4-one analogues as inhibitors of transcription factors NF-kappaB and AP-1 mediated transcriptional activation: Their possible utilization as anti-inflammatory and anti-cancer agents.
Bioorg Med Chem 18: 2796-808 (2010)
B.V. Patel Pharmaceutical Education And Research Development Centre
Discovery of a new series of Aurora inhibitors through truncation of GSK1070916.
Bioorg Med Chem Lett 20: 2552-5 (2010)
Glaxosmithkline
Virtual screening for the identification of novel nonsteroidal glucocorticoid modulators.
J Med Chem 53: 3065-74 (2010)
Trinity College
Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors.
J Med Chem 53: 3169-82 (2010)
Wyeth Research
Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
J Med Chem 53: 3183-97 (2010)
Pfizer
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
Antimicrob Agents Chemother 54: 2401-8 (2010)
Institute-Jewish General Hospital
In vitro properties of BAL30072, a novel siderophore sulfactam with activity against multiresistant gram-negative bacilli.
Antimicrob Agents Chemother 54: 2291-302 (2010)
Basilea Pharmaceutica International
Biochemical characterization of the cellular glycosylphosphatidylinositol-linked membrane type-6 matrix metalloproteinase.
J Biol Chem 285: 16076-86 (2010)
Sanford-Burnham Medical Research Institute
Rational design of a pirinixic acid derivative that acts as subtype-selective PPARgamma modulator.
Bioorg Med Chem Lett 20: 2469-73 (2010)
Goethe-University Frankfurt
B-Raf kinase inhibitors: hit enrichment through scaffold hopping.
Bioorg Med Chem Lett 20: 2431-4 (2010)
Wyeth Research
The significance of 2-furyl ring substitution with a 2-(para-substituted) aryl group in a new series of pyrazolo-triazolo-pyrimidines as potent and highly selective hA(3) adenosine receptors antagonists: new insights into structure-affinity relationship and receptor-antagonist recognition.
J Med Chem 53: 3361-75 (2010)
National University Of Singapore
Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.
J Med Chem 53: 3330-48 (2010)
Neurogen
Conjugates of plumbagin and phenyl-2-amino-1-thioglucoside inhibit MshB, a deacetylase involved in the biosynthesis of mycothiol.
Bioorg Med Chem 18: 2501-14 (2010)
University Of Cape Town
Synthesis, molecular modeling and biological evaluation of PSB as targeted antibiotics.
Bioorg Med Chem 18: 2447-55 (2010)
Nanjing University
Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10.
Bioorg Med Chem 18: 2485-90 (2010)
Gifu Pharmaceutical University
Synthesis and pharmacological characterization of a new series of 5,7-disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazine derivatives as adenosine receptor antagonists: A preliminary inspection of ligand-receptor recognition process.
Bioorg Med Chem 18: 2524-36 (2010)
National University Of Singapore
Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel.
Bioorg Med Chem Lett 20: 2493-6 (2010)
Merck Research Laboratories
Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.
Bioorg Med Chem Lett 20: 2520-4 (2010)
Praecis Pharmaceuticals
Synthesis and antiproliferative activity of indolizine derivatives incorporating a cyclopropylcarbonyl group against Hep-G2 cancer cell line.
Eur J Med Chem 45: 3184-90 (2010)
Nanjing University
Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists.
Bioorg Med Chem 18: 2491-500 (2010)
University Of Delhi
Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi.
Bioorg Med Chem 18: 2566-74 (2010)
University Of California Santa Cruz
1,7-Disubstituted oxyindoles are potent and selective EP(3) receptor antagonists.
Bioorg Med Chem Lett 20: 2658-64 (2010)
Decode Chemistry
Conformationally-restricted amino acid analogues bearing a distal sulfonic acid show selective inhibition of system x(c)(-) over the vesicular glutamate transporter.
Bioorg Med Chem Lett 20: 2680-3 (2010)
The University Of Montana
Design and synthesis of 1,4-dihydropyridine derivatives as BACE-1 inhibitors.
Eur J Med Chem 45: 2578-90 (2010)
Institute Of Science And Technology
Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies.
Bioorg Med Chem Lett 20: 2586-90 (2010)
Wyeth Research
(1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment.
J Med Chem 53: 3247-61 (2010)
Taisho Pharmaceutical
Structure-activity relationships in toll-like receptor-2 agonistic diacylthioglycerol lipopeptides.
J Med Chem 53: 3198-213 (2010)
University Of Kansas
Synthesis and preliminary pharmacological characterisation of a new class of nitrogen-containing bisphosphonates (N-BPs).
Bioorg Med Chem 18: 2428-38 (2010)
Universit£
4,7-Dichloro benzothien-2-yl sulfonylaminomethyl boronic acid: first boronic acid-derived beta-lactamase inhibitor with class A, C, and D activity.
Bioorg Med Chem Lett 20: 2622-4 (2010)
Merck
Carbonic anhydrase inhibitors. The beta-carbonic anhydrases from the fungal pathogens Cryptococcus neoformans and Candida albicans are strongly inhibited by substituted-phenyl-1H-indole-5-sulfonamides.
Bioorg Med Chem Lett 20: 2508-11 (2010)
Istanbul University
Identification of potent, highly constrained CGRP receptor antagonists.
Bioorg Med Chem Lett 20: 2572-6 (2010)
Merck
Benzyl prolinate derivatives as novel selective KCC2 blockers.
Bioorg Med Chem Lett 20: 2542-5 (2010)
Ucb Pharma
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.
Bioorg Med Chem Lett 20: 2516-9 (2010)
Argenta Discovery
(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
Bioorg Med Chem Lett 20: 2605-8 (2010)
Institute Of Pharmacology And Toxicology
Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
J Med Chem 53: 3376-88 (2010)
Genzyme
Derivatives of schisandrin with increased inhibitory potential on prostaglandin E(2) and leukotriene B(4) formation in vitro.
Bioorg Med Chem 18: 2809-15 (2010)
University Of Graz
Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.
Bioorg Med Chem Lett 20: 2591-6 (2010)
Merck Research Laboratories
Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor.
Bioorg Med Chem Lett 20: 2512-5 (2010)
Wyeth Research
A computational study of the binding of 3-(arylidene) anabaseines to two major brain nicotinic acetylcholine receptors and to the acetylcholine binding protein.
Eur J Med Chem 45: 2433-46 (2010)
University Of Florida
Effects of some drugs on human erythrocyte 6-phosphogluconate dehydrogenase: an in vitro study.
J Enzyme Inhib Med Chem 25: 476-9 (2010)
Ataturk University
Design, synthesis, and urease inhibition studies of some 1,3,4-oxadiazoles and 1,2,4-triazoles derived from mandelic acid.
J Enzyme Inhib Med Chem 25: 572-6 (2010)
Quaid-I-Azam University
Nostotrebin 6, a bis(cyclopentenedione) with cholinesterase inhibitory activity isolated from Nostoc sp. str. Lukesová 27/97.
J Enzyme Inhib Med Chem 25: 414-20 (2010)
Brno University Of Technology
Synthesis and biological evaluation of 8-oxoadenine derivatives as toll-like receptor 7 agonists introducing the antedrug concept.
J Med Chem 53: 2964-72 (2010)
Dainippon Sumitomo Pharma
Synthesis of new beta-1-C-alkylated imino-L-iditols: A comparative study of their activity as beta-glucocerebrosidase inhibitors.
Bioorg Med Chem 18: 2645-50 (2010)
Universit£
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.
Bioorg Med Chem Lett 20: 2609-13 (2010)
Novartis Institutes For Biomedical Research
Design, synthesis and in vitro/in vivo evaluation of orally bioavailable prodrugs of a catechol-O-methyltransferase inhibitor.
Bioorg Med Chem Lett 20: 2614-6 (2010)
University Of Eastern Finland
Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors.
Bioorg Med Chem Lett 20: 2644-7 (2010)
Wyeth Research
Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.
Bioorg Med Chem Lett 20: 2629-33 (2010)
Neurocrine Biosciences
Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT(2)-selective melatonin ligands.
Bioorg Med Chem Lett 20: 2582-5 (2010)
Hong Kong University Of Science And Technology
2,5-Disubstituted pyridines as potent GPR119 agonists.
Bioorg Med Chem Lett 20: 2577-81 (2010)
Glaxosmithkline
Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase.
Bioorg Med Chem Lett 20: 2634-8 (2010)
Pfizer
Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay.
Bioorg Med Chem Lett 20: 2111-4 (2010)
Meijo University
Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kalpha.
Bioorg Med Chem Lett 20: 2654-7 (2010)
Wyeth Research
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.
Bioorg Med Chem Lett 20: 2648-53 (2010)
Wyeth Research
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.
Bioorg Med Chem Lett 20: 2099-102 (2010)
Yangji Chemicals
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.
Bioorg Med Chem Lett 20: 2068-73 (2010)
Wyeth
Inside HDAC with HDAC inhibitors.
Eur J Med Chem 45: 2095-116 (2010)
Universit£
Urease inhibitors from Hypericum oblongifolium WALL.
J Enzyme Inhib Med Chem 25: 296-9 (2010)
University Of Peshawar
Semisynthesis of alpha-methyl-gamma-lactones and in vitro evaluation of their activity on protein farnesyltransferase.
J Enzyme Inhib Med Chem 25: 172-9 (2010)
Ufr Des Sciences Pharmaceutiques Et Ingenierie De La Sante
Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer.
J Enzyme Inhib Med Chem 25: 158-71 (2010)
Universit?? Lille Nord De France
Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor.
J Med Chem 53: 2892-901 (2010)
Chemical Genomics Centre Of The Max Planck Society
Complexity in influenza virus targeted drug design: interaction with human sialidases.
J Med Chem 53: 2998-3002 (2010)
Pf-Imss-Kek-Sbrc, Ibaraki 305-0801, Japan.
Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.
Bioorg Med Chem Lett 20: 2074-7 (2010)
Merck Research Laboratories
Discovery of a novel selective PPARgamma modulator from (-)-Cercosporamide derivatives.
Bioorg Med Chem Lett 20: 2095-8 (2010)
Daiichi Sankyo
Toward the development of potent and selective bisubstrate inhibitors of protein arginine methyltransferases.
Bioorg Med Chem Lett 20: 2103-5 (2010)
University Park
Discovery of small molecule isozyme non-specific inhibitors of mammalian acetyl-CoA carboxylase 1 and 2.
Bioorg Med Chem Lett 20: 2383-8 (2010)
Pfizer
Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship.
Eur J Med Chem 45: 2453-66 (2010)
Zentrum F£R Pharmaforschung
"Carba"-analogues of fentanyl are opioid receptor agonists.
J Med Chem 53: 2875-81 (2010)
Clinical Research Institute Of Montreal
Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.
J Med Chem 53: 2825-35 (2010)
University Of Minnesota
Emerging targets in osteoporosis disease modification.
J Med Chem 53: 4332-53 (2010)
Amgen
3'-[4-Aryl-(1,2,3-triazol-1-yl)]-3'-deoxythymidine analogues as potent and selective inhibitors of human mitochondrial thymidine kinase.
J Med Chem 53: 2902-12 (2010)
Ghent University
Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).
J Med Chem 53: 2854-64 (2010)
Bristol-Myers Squibb
A virtual screening hit reveals new possibilities for developing group III metabotropic glutamate receptor agonists.
J Med Chem 53: 2797-813 (2010)
Universite Paris Descartes
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.
J Med Chem 53: 2973-85 (2010)
Amgen
Inhibition studies of a beta-carbonic anhydrase from Brucella suis with a series of water soluble glycosyl sulfanilamides.
Bioorg Med Chem Lett 20: 2178-82 (2010)
Universit£
Structural investigation of the binding of 5-substituted swainsonine analogues to Golgi alpha-mannosidase II.
Chembiochem 11: 673-80 (2010)
University Of Toronto
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.
Bioorg Med Chem Lett 20: 2106-10 (2010)
Merck Research Laboratories
Synthesis of cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines and their evaluation as 5-HT6 receptor antagonists.
Bioorg Med Chem Lett 20: 2133-6 (2010)
Chemical Diversity Research Institute
Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents.
Bioorg Med Chem Lett 20: 2125-8 (2010)
Glaxosmithkline
Novel acyl coenzyme A (CoA): diacylglycerol acyltransferase-1 inhibitors: synthesis and biological activities of diacylethylenediamine derivatives.
Bioorg Med Chem 18: 2785-95 (2010)
Takeda Pharmaceutical
Purine derivatives as potent gamma-secretase modulators.
Bioorg Med Chem Lett 20: 2279-82 (2010)
Merck Research Laboratories
Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9).
Bioorg Med Chem Lett 20: 2254-8 (2010)
The Scripps Research Institute
Discovery of novel (S)-alpha-phenyl-gamma-amino butanamide containing CCR5 antagonists via functionality inversion approach.
Bioorg Med Chem Lett 20: 2219-23 (2010)
Institute Of Materia Medica
Structure-based design of novel human Pin1 inhibitors (II).
Bioorg Med Chem Lett 20: 2210-4 (2010)
Pfizer
Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.
Bioorg Med Chem Lett 20: 2311-5 (2010)
Merck Research Laboratories
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors.
Bioorg Med Chem Lett 20: 2195-9 (2010)
Elan Pharmaceuticals
Structure-activity relationship of novel DAPK inhibitors identified by structure-based virtual screening.
Bioorg Med Chem 18: 2728-34 (2010)
Pharmadesign
Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension.
Bioorg Med Chem Lett 20: 2204-9 (2010)
Merck Frosst Centre For Therapeutic Research
Synthesis, molecular modeling and biological evaluation of novel tadalafil analogues as phosphodiesterase 5 and colon tumor cell growth inhibitors, new stereochemical perspective.
Eur J Med Chem 45: 1278-86 (2010)
German University In Cairo
Conformational refinement of hydroxamate-based histone deacetylase inhibitors and exploration of 3-piperidin-3-ylindole analogues of dacinostat (LAQ824).
J Med Chem 53: 2952-63 (2010)
Novartis Institutes For Biomedical Research
Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors.
Bioorg Med Chem 18: 2081-8 (2010)
Universidad De M£Laga
Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity.
Bioorg Med Chem Lett 20: 2365-9 (2010)
Pfizer
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.
Bioorg Med Chem Lett 20: 2326-9 (2010)
Wyeth Research
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.
Bioorg Med Chem Lett 20: 2174-7 (2010)
Vanderbilt University Medical Center
Synthesis and biological evaluation of N-difluoromethyl-1,2-dihydropyrid-2-one acetic acid regioisomers: dual inhibitors of cyclooxygenases and 5-lipoxygenase.
Bioorg Med Chem Lett 20: 2168-73 (2010)
University Of Alberta
Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors.
Bioorg Med Chem Lett 20: 2163-7 (2010)
Pfizer
The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist.
Bioorg Med Chem Lett 20: 2340-3 (2010)
Medicines Research Centre
Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides.
Eur J Med Chem 45: 2396-404 (2010)
Medical University Of Gdansk
Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases.
J Med Chem 53: 2913-26 (2010)
Griffith University
Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.
J Med Chem 53: 2741-56 (2010)
The Institute Of Cancer Research
Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5).
J Med Chem 53: 2656-60 (2010)
Pfizer
Affinity of ceftaroline and other beta-lactams for penicillin-binding proteins from Staphylococcus aureus and Streptococcus pneumoniae.
Antimicrob Agents Chemother 54: 1670-7 (2010)
Hershey Medical Center
Structure-activity relationship of (N)-Methanocarba phosphonate analogues of 5'-AMP as cardioprotective agents acting through a cardiac P2X receptor.
J Med Chem 53: 2562-76 (2010)
National Institutes Of Diabetes And Digestive And Kidney Diseases
Gneyulins A and B, stilbene trimers, and noidesols A and B, dihydroflavonol-C-glucosides, from the bark of Gnetum gnemonoides.
J Nat Prod 73: 763-7 (2010)
Hoshi University
Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists.
J Med Chem 53: 2390-400 (2010)
Griffin Discoveries
Fragment-based deconstruction of Bcl-xL inhibitors.
J Med Chem 53: 2577-88 (2010)
Universite De Lyon
Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case of bioisosterism between a carboxylic acid moiety and that of a tetrazole.
Bioorg Med Chem 18: 2107-14 (2010)
Aristotle University Of Thessaloniki
Synthesis and in vitro biological evaluation of carbon-11-labeled quinoline derivatives as new candidate PET radioligands for cannabinoid CB2 receptor imaging.
Bioorg Med Chem 18: 2099-106 (2010)
Indiana University School Of Medicine
Design of potent and selective GSK3beta inhibitors with acceptable safety profile and pharmacokinetics.
Bioorg Med Chem Lett 20: 2344-9 (2010)
Sanofi-Aventis
Synthesis of some 5-phenylisoxazole-3-carboxylic acid derivatives as potent xanthine oxidase inhibitors.
Eur J Med Chem 45: 2663-70 (2010)
Shenyang Pharmaceutical University
Alstiphyllanines E-H, picraline and ajmaline-type alkaloids from Alstonia macrophylla inhibiting sodium glucose cotransporter.
Bioorg Med Chem 18: 2152-8 (2010)
Hoshi University
Structural-based design and synthesis of novel 9-deazaguanine derivatives having a phosphate mimic as multi-substrate analogue inhibitors for mammalian PNPs.
Bioorg Med Chem 18: 2275-84 (2010)
Tokyo University Of Pharmacy And Life Sciences
Synthesis and kinetic analysis of some phosphonate analogs of cyclophostin as inhibitors of human acetylcholinesterase.
Bioorg Med Chem 18: 2265-74 (2010)
University Of Missouri St. Louis
Melanogenesis inhibitors from the desert plant Anastatica hierochuntica in B16 melanoma cells.
Bioorg Med Chem 18: 2337-45 (2010)
Kyoto Pharmaceutical University
Identification of amide bioisosteres of triazole oxytocin antagonists.
Bioorg Med Chem Lett 20: 2224-8 (2010)
Pfizer
Potent and selective inhibition of human cytochrome P450 3A4 by seco-pancratistatin structural analogs.
Bioorg Med Chem Lett 20: 2335-9 (2010)
Mcmaster University
Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Bioorg Med Chem Lett 20: 2250-3 (2010)
Jeil Pharmaceutical
Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.
Bioorg Med Chem Lett 20: 2229-33 (2010)
Genentech
Inhibition of eEF2-K by thieno[2,3-b]pyridine analogues.
Bioorg Med Chem Lett 20: 2283-6 (2010)
Kyowa Hakko Kogyo
Affinity reagents that target a specific inactive form of protein kinases.
Chem Biol 17: 195-206 (2010)
University Of Washington
Discovery of dual inhibitors of the immune cell PI3Ks p110delta and p110gamma: a prototype for new anti-inflammatory drugs.
Chem Biol 17: 123-34 (2010)
University Of California San Francisco
Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase.
Bioorg Med Chem 18: 2317-26 (2010)
Temple University School Of Medicine
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
Bioorg Med Chem 18: 2204-18 (2010)
King'S College London
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
Bioorg Med Chem 18: 2195-203 (2010)
University Of Bonn
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Bioorg Med Chem Lett 20: 2264-9 (2010)
Biogen Idec
Tetrahydroindolizinone NK1 antagonists.
Bioorg Med Chem Lett 20: 2354-8 (2010)
Merck Research Laboratories
Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
Bioorg Med Chem Lett 20: 2321-5 (2010)
Wyeth Research
4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
Bioorg Med Chem Lett 20: 2259-63 (2010)
Wyeth Research
Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists.
Bioorg Med Chem Lett 20: 2359-64 (2010)
Merck Research Laboratories
Novel benzothiophene H1-antihistamines for the treatment of insomnia.
Bioorg Med Chem Lett 20: 2316-20 (2010)
Neurocrine Biosciences
Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors.
Bioorg Med Chem Lett 20: 2379-82 (2010)
Johnson & Johnson Pharmaceutical Research & Development
Development of GlcNAc-inspired iminocyclitiols as potent and selective N-acetyl-beta-hexosaminidase inhibitors.
ACS Chem Biol 5: 489-97 (2010)
Academia Sinica
Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids.
Bioorg Med Chem 18: 2159-64 (2010)
Universit£
Exploration of inhibitors for diaminopimelate aminotransferase.
Bioorg Med Chem 18: 2141-2151 (2010)
University Of Alberta
Design, synthesis and evaluation of constrained tetrahydroimidazopyrimidine derivatives as antagonists of corticotropin-releasing factor type 1 receptor (CRF1R).
Bioorg Med Chem Lett 20: 1905-9 (2010)
Bristol-Myers Squibb Research & Development
Discovery of a new series of 5-HT1A receptor agonists.
Bioorg Med Chem Lett 20: 2017-20 (2010)
Universit£
Benzimidazole Thumb Pocket I finger-loop inhibitors of HCV NS5B polymerase: improved drug-like properties through C-2 SAR in three sub-series.
Bioorg Med Chem Lett 20: 1825-9 (2010)
Boehringer Ingelheim (Canada)
Fragment screening of inhibitors for MIF tautomerase reveals a cryptic surface binding site.
Bioorg Med Chem Lett 20: 1821-4 (2010)
Sanofi-Aventis
Discovery of novel and potent benzhydryl-tropane trypanocides highly selective for Trypanosoma cruzi.
Bioorg Med Chem Lett 20: 1816-8 (2010)
Institute Of Medical Research
Phenolic constituents of the aerial parts of Cimicifuga simplex and Cimicifuga japonica.
J Nat Prod 73: 609-12 (2010)
University Of Shizuoka
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
J Med Chem 53: 2666-70 (2010)
Merck Research Laboratories
Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: 1,3,4-Thiadiazolylmethylphenyl glucoside congeners.
Bioorg Med Chem 18: 2178-94 (2010)
Green Cross
Differential binding of phenothiazine urea derivatives to wild-type human cholinesterases and butyrylcholinesterase mutants.
Bioorg Med Chem 18: 2232-44 (2010)
Dalhousie University
Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.
Bioorg Med Chem Lett 20: 1895-9 (2010)
Merck Research Laboratories
Dopamine receptor ligands. Part 18: (1) modification of the structural skeleton of indolobenzazecine-type dopamine receptor antagonists.
J Med Chem 53: 2646-50 (2010)
Friedrich-Schiller-Universit£T Jena
JBIR-22, an inhibitor for protein-protein interaction of the homodimer of proteasome assembly factor 3.
J Nat Prod 73: 628-31 (2010)
Biomedicinal Information Research Center (Birc)
Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models.
J Med Chem 53: 2622-35 (2010)
Universit£
Membrane permeable cyclic peptidyl inhibitors against human Peptidylprolyl Isomerase Pin1.
J Med Chem 53: 2494-501 (2010)
The Ohio State University
Discovery of dipeptides with high affinity to the specific binding site for substance P1-7.
J Med Chem 53: 2383-9 (2010)
Uppsala University
Discovery and SAR of thiazolidine-2,4-dione analogues as insulin-like growth factor-1 receptor (IGF-1R) inhibitors via hierarchical virtual screening.
J Med Chem 53: 2661-5 (2010)
Chinese Academy Of Sciences
Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus.
Bioorg Med Chem 18: 2173-7 (2010)
Institute Of Plant Biochemistry
3D-QSAR and docking studies on transforming growth factor (TGF)-beta receptor 1 antagonists.
Bioorg Med Chem Lett 20: 1918-23 (2010)
Northeastern Ohio Universities Colleges Of Medicine And Pharmacy
SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.
Bioorg Med Chem Lett 20: 1885-9 (2010)
Merck Research Laboratories
Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists.
Bioorg Med Chem Lett 20: 1830-3 (2010)
Roche Palo Alto
Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Bioorg Med Chem Lett 20: 1890-4 (2010)
Bristol-Myers Squibb
A novel insulin secretagogue based on a dinucleoside polyphosphate scaffold.
J Med Chem 53: 2472-81 (2010)
Bar-Ilan University
A concise synthesis of 1,4-dihydro-[1,4]diazepine-5,7-dione, a novel 7-TM receptor ligand core structure with melanocortin receptor agonist activity.
Bioorg Med Chem 18: 1822-33 (2010)
Glaxosmithkline
Discovery and SAR of hydantoin TACE inhibitors.
Bioorg Med Chem Lett 20: 1877-80 (2010)
Merck Research Laboratories
Identification of a urea bioisostere of a triazole oxytocin antagonist.
Bioorg Med Chem Lett 20: 1851-3 (2010)
Pfizer
Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing.
Bioorg Med Chem Lett 20: 1858-60 (2010)
Novartis Institutes For Biomedical Research
Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors.
Bioorg Med Chem Lett 20: 1924-7 (2010)
Universit£
Ultrasmall particle of iron oxide--RGD peptidomimetic conjugate: synthesis and characterisation.
Bioorg Med Chem Lett 20: 1861-5 (2010)
Universit£
Design, synthesis and preliminary activity assay of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as novel Histone deacetylases (HDACs) inhibitors.
Bioorg Med Chem 18: 1761-72 (2010)
Shandong University
Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238.
Bioorg Med Chem 18: 1749-60 (2010)
University Of Bologna
Synthesis of fluorinated C-mannopeptides as sialyl Lewisx mimics for E- and P-selectin inhibition.
Bioorg Med Chem Lett 20: 1957-60 (2010)
Universit£
Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.
Bioorg Med Chem Lett 20: 1900-4 (2010)
Abbott Laboratories
Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors. Part 2: Modification of P3, P4, and P5 regions.
Bioorg Med Chem Lett 20: 2375-8 (2010)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis, biological activity, and molecular modeling studies of 1H-1,2,3-triazole derivatives of carbohydrates as alpha-glucosidases inhibitors.
J Med Chem 53: 2364-75 (2010)
Universidade Federal Do Rio De Janeiro
1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors.
J Med Chem 53: 2534-51 (2010)
Glaxosmithkline
Noncovalent tripeptidyl benzyl- and cyclohexyl-amine inhibitors of the cysteine protease caspase-1.
J Med Chem 53: 2651-5 (2010)
The University Of Queensland
Identification of 2-anilino-9-methoxy-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepin-6-ones as dual PLK1/VEGF-R2 kinase inhibitor chemotypes by structure-based lead generation.
J Med Chem 53: 2433-42 (2010)
Technische Universitat Braunschweig
5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists.
J Med Chem 53: 2521-7 (2010)
Wyeth Research
Salicylic acid based small molecule inhibitor for the oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2).
J Med Chem 53: 2482-93 (2010)
Indiana University School Of Medicine
The design and development of 2-aryl-2-hydroxy ethylamine substituted 1H,7H-pyrido[1,2,3-de]quinoxaline-6-carboxamides as inhibitors of human cytomegalovirus polymerase.
Bioorg Med Chem Lett 20: 1994-2000 (2010)
Pfizer
Design and evaluation of Trypanosoma brucei metacaspase inhibitors.
Bioorg Med Chem Lett 20: 2001-6 (2010)
University Of Antwerp
The synthesis and angiotensin converting enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives.
Bioorg Med Chem Lett 20: 1990-3 (2010)
University Of Calabria
Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.
Bioorg Med Chem Lett 20: 1913-7 (2010)
Merck Research Laboratories
SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii.
Bioorg Med Chem Lett 20: 1873-6 (2010)
Korea Research Institute Of Bioscience And Biotechnology
Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.
Bioorg Med Chem Lett 20: 1985-9 (2010)
Sanofi-Aventis
SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors.
Bioorg Med Chem Lett 20: 2044-7 (2010)
Pennsylvania State Hershey College Of Medicine
Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.
J Med Chem 53: 2636-45 (2010)
Wyeth Research
Selectively nonselective kinase inhibition: striking the right balance.
J Med Chem 53: 1413-37 (2010)
Schering-Plough
Synthesis of new pyrrolo[2,3-d]pyrimidine derivatives and evaluation of their activities against human colon cancer cell lines.
Eur J Med Chem 45: 1453-8 (2010)
University College Of Pharmaceutical Sciences
The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.
J Med Chem 53: 2227-38 (2010)
Merck Frosst Centre For Therapeutic Research
Gymnochromes E and F, cytotoxic phenanthroperylenequinones from a deep-water crinoid, Holopus rangii.
J Nat Prod 73: 712-5 (2010)
Florida Atlantic University
Hybrid molecules from xanomeline and tacrine: enhanced tacrine actions on cholinesterases and muscarinic M1 receptors.
J Med Chem 53: 2094-103 (2010)
China Pharmaceutical University
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation.
J Med Chem 53: 2204-14 (2010)
Research Triangle Institute
Structural insights into the design of small molecule inhibitors that selectively antagonize Mcl-1.
J Med Chem 53: 2314-8 (2010)
Institute Of Chemical And Engineering Sciences
Structural basis for platelet antiaggregation by angiotensin II type 1 receptor antagonist losartan (DuP-753) via glycoprotein VI.
J Med Chem 53: 2087-93 (2010)
Japan Biological Informatics Consortium (Jbic)
1-Alkyl-4-phenyl-6-alkoxy-1H-quinazolin-2-ones: a novel series of potent calcium-sensing receptor antagonists.
J Med Chem 53: 2250-63 (2010)
Novartis Institutes For Biomedical Research
Colony stimulating factor-1 receptor as a target for small molecule inhibitors.
Bioorg Med Chem 18: 1789-97 (2010)
University Of Newcastle
Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.
Bioorg Med Chem Lett 20: 1972-5 (2010)
Vanderbilt University Medical Center
Synthesis and biological evaluation of botulinum neurotoxin a protease inhibitors.
J Med Chem 53: 2264-76 (2010)
Microbiotix
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
J Med Chem 53: 2510-20 (2010)
Neurosearch Sweden
Turning enzymes ON with small molecules.
Nat Chem Biol 6: 179-188 (2010)
University Of California
Substituted fused bicyclic pyrrolizinones as potent, orally bioavailable hNK1 antagonists.
Bioorg Med Chem Lett 20: 2007-12 (2010)
Merck Research Laboratories
Synthesis and evaluation of 2-pyridylbenzothiazole, 2-pyridylbenzoxazole and 2-pyridylbenzofuran derivatives as 11C-PET imaging agents for beta-amyloid plaques.
Bioorg Med Chem Lett 20: 1976-80 (2010)
Astrazeneca
Selective benzimidazole inhibitors of the antigen receptor-mediated NF-kappaB activation pathway.
Bioorg Med Chem 18: 1918-24 (2010)
Human Biomolecular Research Institute
Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors.
Bioorg Med Chem 18: 1925-35 (2010)
Universidade Federal Do Rio Grande Do Sul
Novel thiophene derivatives as PTP1B inhibitors with selectivity and cellular activity.
Bioorg Med Chem 18: 1773-82 (2010)
Chinese Academy Of Sciences
Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1.
Bioorg Med Chem Lett 20: 2370-4 (2010)
Johnson & Johnson Pharmaceutical Research & Development
The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure.
Bioorg Med Chem Lett 20: 2013-6 (2010)
Glaxosmithkline
Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells.
Bioorg Med Chem Lett 20: 2033-7 (2010)
Institute Of Science And Technology
Discovery of novel inhibitors for DHODH via virtual screening and X-ray crystallographic structures.
Bioorg Med Chem Lett 20: 1981-4 (2010)
Sanofi-Aventis
Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.
Bioorg Med Chem Lett 20: 1965-8 (2010)
Wyeth Research
Synthesis and preliminary evaluation of peptidomimetic inhibitors of human beta-secretase.
Eur J Med Chem 45: 2089-94 (2010)
Peking University
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.
Bioorg Med Chem 18: 1844-53 (2010)
Nerviano Medical Sciences
Synthesis and characterization of novel 1,2,4-triazine derivatives with antiproliferative activity.
Bioorg Med Chem 18: 1816-21 (2010)
Martin-Luther-Universit£T Halle-Wittenberg
Effect of 3'-end capping of aptamer with various 2',4'-bridged nucleotides: Enzymatic post-modification toward a practical use of polyclonal aptamers.
Bioorg Med Chem Lett 20: 1626-9 (2010)
Gunma University
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Bioorg Med Chem Lett 20: 1744-8 (2010)
Bristol-Myers Squibb
Structure-activity relationships of norepinephrine reuptake inhibitors with benzothiadiazine dioxide or dihydrosulfostyril cores.
Bioorg Med Chem Lett 20: 1555-8 (2010)
Pfizer
Dioxo-triazines as a novel series of cathepsin K inhibitors.
Bioorg Med Chem Lett 20: 1488-90 (2010)
Schering-Plough
S1P receptor mediated activity of FTY720 phosphate mimics.
Bioorg Med Chem Lett 20: 1485-7 (2010)
Novartis Institutes For Biomedical Research
3D-QSAR studies on quinazoline antifolate thymidylate synthase inhibitors by CoMFA and CoMSIA models.
Eur J Med Chem 45: 1560-71 (2010)
Meerut Institute Of Engineering And Technology
Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt).
J Med Chem 53: 2239-49 (2010)
The Institute Of Cancer Research
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
J Med Chem 53: 2215-26 (2010)
Domainex
Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion.
J Med Chem 53: 2038-50 (2010)
Universit£
Synthesis and uptake of fluorescence-labeled Combi-molecules by P-glycoprotein-proficient and -deficient uterine sarcoma cells MES-SA and MES-SA/DX5.
J Med Chem 53: 2104-13 (2010)
Mcgill University Health Center/Royal Victoria Hospital
Interaction of (benzylidene-hydrazono)-1,4-dihydropyridines with beta-amyloid, acetylcholine, and butyrylcholine esterases.
Bioorg Med Chem 18: 2049-59 (2010)
Ege University
Synthesis, in vitro progesterone receptors affinity of gadolinium containing mifepristone conjugates and estimation of binding sites in human breast cancer cells.
Bioorg Med Chem 18: 1891-8 (2010)
University Of Quebec At Trois-Rivieres
Development of selective and reversible pyrazoline based MAO-A inhibitors: Synthesis, biological evaluation and docking studies.
Bioorg Med Chem 18: 1875-81 (2010)
Institute Of Technology
Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines.
Bioorg Med Chem Lett 20: 1573-7 (2010)
Korea Institute Of Science And Technology
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.
Bioorg Med Chem Lett 20: 1524-7 (2010)
Schering-Plough
Derivatives of aryl amines containing the cytotoxic 1,4-dioxo-2-butenyl pharmacophore.
Bioorg Med Chem Lett 20: 1510-5 (2010)
Acadia University
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
Bioorg Med Chem Lett 20: 1491-5 (2010)
Merck Serono
C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization.
Bioorg Med Chem Lett 20: 1569-72 (2010)
Pfizer
Discovery of a novel series of potent S1P1 agonists.
Bioorg Med Chem Lett 20: 1516-9 (2010)
Merck Serono
Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors.
Bioorg Med Chem Lett 20: 1551-4 (2010)
Merck Research Laboratories
Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.
Bioorg Med Chem Lett 20: 1705-11 (2010)
Green Cross
Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone.
Eur J Med Chem 45: 2010-7 (2010)
Department Of Functional Crop
Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
J Med Chem 53: 2155-70 (2010)
University Of Bath
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.
J Med Chem 53: 1964-78 (2010)
The Institute Of Cancer Research
Enhancement of hydrophobic interactions and hydrogen bond strength by cooperativity: synthesis, modeling, and molecular dynamics simulations of a congeneric series of thrombin inhibitors.
J Med Chem 53: 2126-35 (2010)
The State University Of New York
Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold.
J Med Chem 53: 2076-86 (2010)
University Of Bonn
Discovery of 4-(4-(2-((5-Hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)(propyl)amino)ethyl)piperazin-1-yl)quinolin-8-ol and its analogues as highly potent dopamine D2/D3 agonists and as iron chelator: in vivo activity indicates potential application in symptomatic and neuroprotective therapy for Parkin
J Med Chem 53: 2114-25 (2010)
Wayne State University
Toward biophysical probes for the 5-HT3 receptor: structure-activity relationship study of granisetron derivatives.
J Med Chem 53: 2324-8 (2010)
University Of Warwick
The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
J Med Chem 53: 2063-75 (2010)
Universite De Sherbrooke
Small molecule JNK (c-Jun N-terminal kinase) inhibitors.
J Med Chem 53: 3005-12 (2010)
Merck Research Laboratories
Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5-dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors.
J Med Chem 53: 2136-45 (2010)
University Of St. Andrews
PER-6, an extended-spectrum beta-lactamase from Aeromonas allosaccharophila.
Antimicrob Agents Chemother 54: 1619-22 (2010)
Bicetre Hospital
Antiproliferative activity of novel benzo[b][1,6]naphthyridines in human solid tumor cell lines.
Bioorg Med Chem Lett 20: 1504-6 (2010)
Vilnius University
Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
Bioorg Med Chem Lett 20: 1507-9 (2010)
Harvard Medical School
Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template.
Bioorg Med Chem Lett 20: 1604-9 (2010)
Pfizer
Synthesis of physostigmine analogues and evaluation of their anticholinesterase activities.
Bioorg Med Chem Lett 20: 1532-4 (2010)
Zhejiang University
Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists.
Bioorg Med Chem Lett 20: 1539-42 (2010)
Actelion Pharmaceuticals
Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs.
Bioorg Med Chem Lett 20: 1601-3 (2010)
Kyorin Pharmaceutical
Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors.
Bioorg Med Chem Lett 20: 1669-73 (2010)
Astrazeneca R&D Boston
LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators.
Bioorg Med Chem Lett 20: 1712-7 (2010)
The University Of Tokyo
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
J Med Chem 53: 1937-50 (2010)
Umr Cnrs 6026-Universit£
Discovery of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (nelotanserin) and related 5-hydroxytryptamine2A inverse agonists for the treatment of insomnia.
J Med Chem 53: 1923-36 (2010)
Arena Pharmaceuticals
Synthesis and evaluation of paracetamol esters as novel fatty acid amide hydrolase inhibitors.
J Med Chem 53: 2286-98 (2010)
University Of Cagliari
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
J Med Chem 53: 2000-9 (2010)
Curis
Piperazinyl glutamate pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation.
J Med Chem 53: 2010-37 (2010)
Pfizer
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.
J Med Chem 53: 2171-87 (2010)
Nerviano Medical Sciences
Chemical phylogenetics of histone deacetylases.
Nat Chem Biol 6: 238-243 (2010)
Dana-Farber Cancer Institute
SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling.
Bioorg Med Chem 18: 1958-67 (2010)
Universit£
Design, asymmetric synthesis, and evaluation of pseudosymmetric sulfoximine inhibitors against HIV-1 protease.
Bioorg Med Chem 18: 2037-48 (2010)
University Of Minnesota
3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators.
Bioorg Med Chem Lett 20: 1657-60 (2010)
Wyeth Pharmaceuticals
Acidic elements in histamine H(3) receptor antagonists.
Bioorg Med Chem Lett 20: 1581-4 (2010)
Johann Wolfgang Goethe University
Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Bioorg Med Chem Lett 20: 1680-4 (2010)
Amgen
The role of phosphate in the action of thymidine phosphorylase inhibitors: Implications for the catalytic mechanism.
Bioorg Med Chem Lett 20: 1648-51 (2010)
University At Buffalo
Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage-initial study for Myasthenia gravis implications.
Bioorg Med Chem Lett 20: 1763-6 (2010)
Military Health Sciences
Discovery of potent and selective bicyclic A(2B) adenosine receptor antagonists via bioisosteric amide replacement.
Bioorg Med Chem Lett 20: 1634-7 (2010)
RhôNe-Poulenc Rorer
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.
Bioorg Med Chem Lett 20: 1661-4 (2010)
Vertex Pharmaceuticals
Discovery of potent and bioavailable GSK-3beta inhibitors.
Bioorg Med Chem Lett 20: 1693-6 (2010)
Roche Palo Alto
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.
Bioorg Med Chem Lett 20: 1724-7 (2010)
Novartis Institutes For Biomedical Research
Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists.
Bioorg Med Chem 18: 2001-9 (2010)
Universidade De Porto
Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols.
Bioorg Med Chem 18: 2029-36 (2010)
National Institute Of Pharmaceutical Education And Research
Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists.
Bioorg Med Chem Lett 20: 1697-700 (2010)
RhôNe-Poulenc Rorer
Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst(3) receptor antagonists.
Bioorg Med Chem Lett 20: 1728-34 (2010)
Novartis Institutes For Biomedical Research
Azole-based inhibitors of AKT/PKB for the treatment of cancer.
Bioorg Med Chem Lett 20: 1559-64 (2010)
Amgen
Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists.
Bioorg Med Chem Lett 20: 1638-41 (2010)
7Tm Pharma
Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors.
Bioorg Med Chem Lett 20: 1721-3 (2010)
Kyoto University
2-Anilino-4-aryl-1,3-thiazole inhibitors of valosin-containing protein (VCP or p97).
Bioorg Med Chem Lett 20: 1677-9 (2010)
Kyowa Hakko Kogyo
Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds.
Bioorg Med Chem Lett 20: 1610-3 (2010)
Vrije Universiteit Brussel
Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc.
Bioorg Med Chem Lett 20: 1674-6 (2010)
Roche Palo Alto
Radiosynthesis of novel carbon-11-labeled triaryl ligands for cannabinoid-type 2 receptor.
Bioorg Med Chem Lett 20: 1565-8 (2010)
National Institute Of Radiological Sciences
Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists.
Bioorg Med Chem Lett 20: 1752-7 (2010)
Solvay Pharma
Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors.
Bioorg Med Chem Lett 20: 1718-20 (2010)
Kyoto University
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.
Bioorg Med Chem Lett 20: 1758-62 (2010)
Amgen
2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics.
Bioorg Med Chem Lett 20: 1652-6 (2010)
Amgen
Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode.
Bioorg Med Chem Lett 20: 1543-7 (2010)
Pfizer
Novel tetrahydrochinoline derived CETP inhibitors.
Bioorg Med Chem Lett 20: 1740-3 (2010)
Bayer Healthcare
SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors.
Bioorg Med Chem Lett 20: 1593-7 (2010)
Merck Frosst Centre For Therapeutic Research
Pharmacophore-based 3D QSAR studies on a series of high affinity 5-HT1A receptor ligands.
Eur J Med Chem 45: 1508-14 (2010)
Universidade Federal Da Para£Ba
Incorporation of fluorinated phenylalanine generates highly specific inhibitor of proteasome's chymotrypsin-like sites.
J Med Chem 53: 2319-23 (2010)
Gorlaeus Laboratories
1-(Indolin-1-yl)-1-phenyl-3-propan-2-olamines as potent and selective norepinephrine reuptake inhibitors.
J Med Chem 53: 2051-62 (2010)
Wyeth Research
Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids.
J Med Chem 53: 1951-63 (2010)
University Of W£Rzburg
Structural basis for selective inhibition of purine nucleoside phosphorylase from Schistosoma mansoni: kinetic and structural studies.
Bioorg Med Chem 18: 1421-7 (2010)
Universidade Federal Da Bahia
3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. part 2: optimization of the side chains to improve in vitro and in vivo potencies.
Bioorg Med Chem 18: 1641-58 (2010)
Minase Research Institute
Podophyllotoxin analogues active versus Trypanosoma brucei.
Bioorg Med Chem Lett 20: 1787-91 (2010)
Vanderbilt University School Of Medicine
Novel cyclic-imide peptidomimetics as aminopeptidase N inhibitors. Structure-based design, chemistry and activity evaluation. II.
Eur J Med Chem 45: 1618-26 (2010)
Shandong University
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J Med Chem 53: 1867-70 (2010)
University Of Michigan
Synthesis and biological evaluation of polysulfated oligosaccharide glycosides as inhibitors of angiogenesis and tumor growth.
J Med Chem 53: 1686-99 (2010)
Progen Pharmaceuticals
Design and synthesis of potent and selective BACE-1 inhibitors.
J Med Chem 53: 1458-64 (2010)
Stockholm University
Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist.
J Med Chem 53: 1857-61 (2010)
Glaxosmithkline
2-Arylthiomorpholine derivatives as potent and selective monoamine oxidase B inhibitors.
Bioorg Med Chem 18: 1388-95 (2010)
University Of Chile
Discovery of potent BACE-1 inhibitors containing a new hydroxyethylene (HE) scaffold: exploration of P1' alkoxy residues and an aminoethylene (AE) central core.
Bioorg Med Chem 18: 1711-23 (2010)
Stockholm University
Synthesis and SAR of thiazolidinedione derivatives as 15-PGDH inhibitors.
Bioorg Med Chem 18: 1428-33 (2010)
Chosun University
Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis.
J Med Chem 53: 1465-72 (2010)
Trigen
Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors.
J Med Chem 53: 1473-82 (2010)
Trigen
Discovery of novel fibroblast growth factor receptor 1 kinase inhibitors by structure-based virtual screening.
J Med Chem 53: 1662-72 (2010)
Yale University
Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.
J Med Chem 53: 1871-5 (2010)
University Of Utah
Insight into binding of phosphodiesterase-9A selective inhibitors by crystal structures and mutagenesis.
J Med Chem 53: 1726-31 (2010)
University Of North Carolina
Synthesis, biological evaluation, and molecular modeling of 1-benzyl-1H-imidazoles as selective inhibitors of aldosterone synthase (CYP11B2).
J Med Chem 53: 1712-25 (2010)
Eindhoven University Of Technology
Design of novel nicotinamides as potent and selective monoamine oxidase a inhibitors.
Bioorg Med Chem 18: 1659-64 (2010)
Nanjing University
CoMFA analysis of tgDHFR and rlDHFR based on antifolates with 6-5 fused ring system using the all-orientation search (AOS) routine and a modified cross-validated r(2)-guided region selection (q(2)-GRS) routine and its initial application.
Bioorg Med Chem 18: 1684-701 (2010)
Duquesne University
Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.
Bioorg Med Chem 18: 1482-96 (2010)
University Of Milano-Bicocca
Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.
Bioorg Med Chem Lett 20: 1378-83 (2010)
Neuromed Pharmaceuticals
Synthesis and theoretical studies on energetics of novel N- and O- perfluoroalkyl triazole tagged thienopyrimidines--their potential as adenosine receptor ligands.
Eur J Med Chem 45: 1739-45 (2010)
Institute Of Chemical Technology
Designing inhibitors against fructose 1,6-bisphosphatase: exploring natural products for novel inhibitor scaffolds.
Eur J Med Chem 45: 1478-84 (2010)
Boston College
Discovery of new cholesteryl ester transfer protein inhibitors via ligand-based pharmacophore modeling and QSAR analysis followed by synthetic exploration.
Eur J Med Chem 45: 1598-617 (2010)
Al-Zaytoonah Private University Of Jordan
QSAR study of flavonoids and biflavonoids as influenza H1N1 virus neuraminidase inhibitors.
Eur J Med Chem 45: 1724-30 (2010)
Universidad De Buenos Aires
Synthesis of new thienyl ring containing HIV-1 protease inhibitors: promising preliminary pharmacological evaluation against recombinant HIV-1 proteases.
J Med Chem 53: 1451-7 (2010)
Universit£
Novel inhibitors of dengue virus methyltransferase: discovery by in vitro-driven virtual screening on a desktop computer grid.
J Med Chem 53: 1483-95 (2010)
University Of Basel
Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
J Med Chem 53: 1546-62 (2010)
University Of Strasburg
Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent.
J Med Chem 53: 1616-26 (2010)
China Medical University
Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.
J Med Chem 53: 1843-56 (2010)
Johnson & Johnson Pharmaceutical Research And Development
11beta-Hydroxysteroid dehydrogenase 1 inhibiting constituents from Eriobotrya japonica revealed by bioactivity-guided isolation and computational approaches.
Bioorg Med Chem 18: 1507-15 (2010)
University Of Innsbruck
Binding of curcumin and its long chain derivatives to the activator binding domain of novel protein kinase C.
Bioorg Med Chem 18: 1591-8 (2010)
University Of Houston
Phenyltriazolinones as potent factor Xa inhibitors.
Bioorg Med Chem Lett 20: 1373-7 (2010)
Bristol-Myers Squibb
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
J Med Chem 53: 1830-42 (2010)
The Scripps Research Institute
Discovery and optimization of novel 3-piperazinylcoumarin antagonist of chemokine-like factor 1 with oral antiasthma activity in mice.
J Med Chem 53: 1741-54 (2010)
Chinese Academy Of Medical Sciences And Peking Union Medical College
Potent inhibitor scaffold against Trypanosoma cruzi trans-sialidase.
Bioorg Med Chem 18: 1633-40 (2010)
Hokkaido University
Synthesis and structure-activity relationship of botryllamides that block the ABCG2 multidrug transporter.
Bioorg Med Chem Lett 20: 1330-3 (2010)
Ritsumeikan University
Part II: piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation.
Bioorg Med Chem Lett 20: 1388-94 (2010)
Pfizer
Evaluation of 3,4-dihydroquinazoline-2(1H)-thiones as inhibitors of alpha-MSH-induced melanin production in melanoma B16 cells.
Bioorg Med Chem 18: 1555-62 (2010)
Chungnam National University
Novel matrix metalloproteinase inhibitors derived from quinoxalinone scaffold (Part I).
Bioorg Med Chem 18: 1516-25 (2010)
Shandong University
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Bioorg Med Chem 18: 1702-10 (2010)
Universit£
New potential antitumor compounds from the plant Aristolochia manshuriensis as inhibitors of the CDK2 enzyme.
Bioorg Med Chem Lett 20: 1344-6 (2010)
Schering-Plough Research Institute
Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists.
Bioorg Med Chem Lett 20: 1363-7 (2010)
Glaxosmithkline
Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.
Bioorg Med Chem Lett 20: 1324-9 (2010)
University Of Alberta
Potent oxadiazole CGRP receptor antagonists for the potential treatment of migraine.
Bioorg Med Chem Lett 20: 1368-72 (2010)
Glaxosmithkline
Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective KV1.5 blockers.
Bioorg Med Chem Lett 20: 1436-9 (2010)
Bristol-Myers Squibb Pharmaceutical Research And Development
Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.
Bioorg Med Chem Lett 20: 1384-7 (2010)
Schering-Plough Research Institute
Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT(2A) receptor antagonists.
Bioorg Med Chem 18: 1665-75 (2010)
Ewha Womans University
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
Bioorg Med Chem 18: 1381-7 (2010)
University Of California
Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.
Bioorg Med Chem Lett 20: 1448-52 (2010)
Merck Research Laboratories
Discovery of olodaterol, a novel inhaled beta2-adrenoceptor agonist with a 24 h bronchodilatory efficacy.
Bioorg Med Chem Lett 20: 1410-4 (2010)
Boehringer Ingelheim Pharma
Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists.
J Med Chem 53: 1799-809 (2010)
The Scripps Research Institute
Improvement of physiochemical properties of the tetrahydroazepinoindole series of farnesoid X receptor (FXR) agonists: beneficial modulation of lipids in primates.
J Med Chem 53: 1774-87 (2010)
Wyeth Research
Low molecular weight antagonists of the myelin-associated glycoprotein: synthesis, docking, and biological evaluation.
J Med Chem 53: 1597-615 (2010)
University Of Basel
5-OMe-UDP is a potent and selective P2Y(6)-receptor agonist.
J Med Chem 53: 1673-85 (2010)
Bar-Ilan University
Inhibition of monoamine oxidase by 8-benzyloxycaffeine analogues.
Bioorg Med Chem 18: 1018-28 (2010)
North-West University
Isosorbide-based cholinesterase inhibitors; replacement of 5-ester groups leading to increased stability.
Bioorg Med Chem 18: 1045-53 (2010)
Trinity College
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.
Bioorg Med Chem Lett 20: 1405-9 (2010)
Chugai Pharmaceutical
Synthesis and structure-activity relationships of dimeric peptide antagonists of the human immunoglobulin G-human neonatal Fc receptor (IgG-FcRn) interaction.
J Med Chem 53: 1587-96 (2010)
Syntonix Pharmaceuticals
Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.
J Med Chem 53: 1563-78 (2010)
Duquesne University
Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.
Bioorg Med Chem Lett 20: 1415-9 (2010)
Baylor University
Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent.
Bioorg Med Chem Lett 20: 1440-4 (2010)
Wyeth Research
Synthesis and discovery of 2,3-dihydro-3,8-diphenylbenzo[1,4]oxazines as a novel class of potent cholesteryl ester transfer protein inhibitors.
Bioorg Med Chem Lett 20: 1432-5 (2010)
Johnson & Johnson Pharmaceutical Research And Development
Nonpeptidic tetrafluorophenoxymethyl ketone cruzain inhibitors as promising new leads for Chagas disease chemotherapy.
J Med Chem 53: 1763-73 (2010)
University Of California
De novo design of a picomolar nonbasic 5-HT(1B) receptor antagonist.
J Med Chem 53: 1876-80 (2010)
Astrazeneca Pharmaceuticals
Selective inhibitors of the JMJD2 histone demethylases: combined nondenaturing mass spectrometric screening and crystallographic approaches.
J Med Chem 53: 1810-8 (2010)
University Of Oxford
One step radiosynthesis of 6-[(18)F]fluoronicotinic acid 2,3,5,6-tetrafluorophenyl ester ([(18)F]F-Py-TFP): a new prosthetic group for efficient labeling of biomolecules with fluorine-18.
J Med Chem 53: 1732-40 (2010)
University Of Troms£
Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier for cellular entry.
J Med Chem 53: 1306-18 (2010)
Duquesne University
Boron-containing phenoxyacetanilide derivatives as hypoxia-inducible factor (HIF)-1alpha inhibitors.
Bioorg Med Chem Lett 20: 1453-6 (2010)
Gakushuin University
Rapid behavior-based identification of neuroactive small molecules in the zebrafish.
Nat Chem Biol 6: 231-237 (2010)
Harvard Medical School
Mechanistic insights into a Ca2+-dependent family of alpha-mannosidases in a human gut symbiont.
Nat Chem Biol 6: 125-32 (2010)
Newcastle University
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.
Nat Chem Biol 6: 117-24 (2010)
Medical Research Council-Laboratory Of Molecular Biology
Chemoselective small molecules that covalently modify one lysine in a non-enzyme protein in plasma.
Nat Chem Biol 6: 133-9 (2010)
The Scripps Research Institute
Synthesis of 1-(D-glucopyranosyl)-1,2,3-triazoles and their evaluation as glycogen phosphorylase inhibitors.
Bioorg Med Chem 18: 1171-80 (2010)
University Of Debrecen
Synthesis and structure-activity relationship of substitutions at the C-1 position of Delta9-tetrahydrocannabinol.
Bioorg Med Chem Lett 20: 1424-6 (2010)
Amri
Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.
Bioorg Med Chem Lett 20: 1399-404 (2010)
Glaxosmithkline
Synthesis and evaluation of novel rutaecarpine derivatives and related alkaloids derivatives as selective acetylcholinesterase inhibitors.
Eur J Med Chem 45: 1415-23 (2010)
Sun Yat-Sen University
Triazaspirodimethoxybenzoyls as selective inhibitors of mycobacterial lipoamide dehydrogenase .
Biochemistry 49: 1616-27 (2010)
Weill Cornell Medical College
Pyridinylquinoxalines and pyridinylpyridopyrazines as lead compounds for novel p38 alpha mitogen-activated protein kinase inhibitors.
J Med Chem 53: 1128-37 (2010)
Eberhard-Karls-University Of T£Bingen
Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation.
J Med Chem 53: 1357-69 (2010)
Universidad Complutense De Madrid
The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).
Eur J Med Chem 45: 1379-86 (2010)
Wyeth Research
Design, synthesis, and docking studies of novel benzimidazoles for the treatment of metabolic syndrome.
J Med Chem 53: 1076-85 (2010)
The University Of Mississippi
Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups.
Bioorg Med Chem Lett 20: 848-52 (2010)
Methylgene
Design and synthesis of piperazine-indole p38alpha MAP kinase inhibitors with improved pharmacokinetic profiles.
Bioorg Med Chem Lett 20: 828-31 (2010)
Scios
Evaluation of aldose reductase inhibition and docking studies of 6'-nitro and 6',6''-dinitrorosmarinic acids.
Eur J Med Chem 45: 1663-6 (2010)
National Hellenic Research Foundation
Assessment of species specificity of moulting accelerating compounds in Lepidoptera: comparison of activity between Bombyx mori and Spodoptera littoralis by in vitro reporter and in vivo toxicity assays.
Pest Manag Sci 66: 526-35 (2010)
Ghent University
Design and synthesis of novel quinone inhibitors targeted to the redox function of apurinic/apyrimidinic endonuclease 1/redox enhancing factor-1 (Ape1/ref-1).
J Med Chem 53: 1200-10 (2010)
Purdue University
Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor.
J Med Chem 53: 1190-9 (2010)
Trinity College
Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.
J Med Chem 53: 1261-9 (2010)
Universit£
GES-13, a beta-lactamase variant possessing Lys-104 and Asn-170 in Pseudomonas aeruginosa.
Antimicrob Agents Chemother 54: 1331-3 (2010)
Hellenic Pasteur Institute
Synthesis and biological activity of the calcium modulator (R) and (S)-3-methyl 5-pentyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.
Bioorg Med Chem Lett 20: 805-8 (2010)
Fourth Military Medical University
Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity.
Bioorg Med Chem Lett 20: 824-7 (2010)
Wyeth Research
Structure-based design of a thiazolidinedione which targets the mitochondrial protein mitoNEET.
Bioorg Med Chem Lett 20: 819-23 (2010)
Northeastern Ohio Universities
Remote functionalization of SCH 39166: discovery of potent and selective benzazepine dopamine D1 receptor antagonists.
Bioorg Med Chem Lett 20: 832-5 (2010)
Merck Research Laboratories
Spirocyclic ureas: orally bioavailable 11beta-HSD1 inhibitors identified by computer-aided drug design.
Bioorg Med Chem Lett 20: 881-6 (2010)
Vitae Pharmaceuticals
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.
Bioorg Med Chem Lett 20: 1298-301 (2010)
Merck Research Laboratories
Characterisation of hydrazides and hydrazine derivatives as novel aspartic protease inhibitors.
J Enzyme Inhib Med Chem 25: 673-8 (2010)
University Of Karachi
Characterization of a novel class of polyphenolic inhibitors of plasminogen activator inhibitor-1.
J Biol Chem 285: 7892-902 (2010)
University Of Michigan
Design, synthesis and biological evaluation of new 2,3-diarylquinoline derivatives as selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem 18: 1029-33 (2010)
Shahid Beheshti University Mc
4-Aryl-4-oxo-N-phenyl-2-aminylbutyramides as acetyl- and butyrylcholinesterase inhibitors. Preparation, anticholinesterase activity, docking study, and 3D structure-activity relationship based on molecular interaction fields.
Bioorg Med Chem 18: 1181-93 (2010)
Institute
Discovery of new SCH 39166 analogs as potent and selective dopamine D1 receptor antagonists.
Bioorg Med Chem Lett 20: 836-40 (2010)
Merck Research Laboratories
The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.
Bioorg Med Chem Lett 20: 887-92 (2010)
Merck Frosst Centre For Therapeutic Research
Synthesis, structure and affinity of novel 3-alkoxy-1,2-dihydro-3H-1,4-benzodiazepin-2-ones for CNS central and peripheral benzodiazepine receptors.
Eur J Med Chem 45: 1346-51 (2010)
Institute Of The National Academy Of Sciences Of Ukraine
Synthesis and pharmacological evaluation of new 5-(cyclo)alkyl-5-phenyl- and 5-spiroimidazolidine-2,4-dione derivatives. Novel 5-HT1A receptor agonist with potential antidepressant and anxiolytic activity.
Eur J Med Chem 45: 1295-303 (2010)
Jagiellonian University Medical College
Design, synthesis and evaluation of analogs of initiation factor 4E (eIF4E) cap-binding antagonist Bn7-GMP.
Eur J Med Chem 45: 1304-13 (2010)
University Of Minnesota
beta-Naphthoflavone analogs as potent and soluble aryl hydrocarbon receptor agonists: improvement of solubility by disruption of molecular planarity.
Bioorg Med Chem 18: 1194-203 (2010)
The University Of Tokyo
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.
Bioorg Med Chem Lett 20: 1293-7 (2010)
Novartis Institutes For Biomedical Research
Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors.
J Med Chem 53: 3423-38 (2010)
Mcgill University
Discovery of 3-(4-bromophenyl)-6-nitrobenzo[1.3.2]dithiazolium ylide 1,1-dioxide as a novel dual cyclooxygenase/5-lipoxygenase inhibitor that also inhibits tumor necrosis factor-alpha production.
Bioorg Med Chem 18: 597-604 (2010)
National Taiwan University
Synthesis, in vitro structure-activity relationship, and in vivo studies of 2-arylthiazolidine-4-carboxylic acid amides as anticancer agents.
Bioorg Med Chem 18: 477-95 (2010)
University Of Tennessee Health Science Center
2,4-Diamino-5-methyl-6-substituted arylthio-furo[2,3-d]pyrimidines as novel classical and nonclassical antifolates as potential dual thymidylate synthase and dihydrofolate reductase inhibitors.
Bioorg Med Chem 18: 953-61 (2010)
Duquesne University
The effect of backbone cyclization on PK/PD properties of bioactive peptide-peptoid hybrids: the melanocortin agonist paradigm.
Bioorg Med Chem 18: 580-9 (2010)
The Hebrew University Of Jerusalem
Anti-invasive and anti-angiogenic activities of naturally occurring dibenzodiazepine BU-4664L and its derivatives.
Bioorg Med Chem Lett 20: 963-5 (2010)
Toyama Prefectural University
Piperidine-derived gamma-secretase modulators.
Bioorg Med Chem Lett 20: 1306-11 (2010)
Glaxosmithkline
Novel bis-arylsulfonamides and aryl sulfonimides as inactivators of plasminogen activator inhibitor-1 (PAI-1).
Bioorg Med Chem Lett 20: 966-70 (2010)
Eastern Michigan University
Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.
Bioorg Med Chem Lett 20: 1055-8 (2010)
Kitasato University
Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors.
Bioorg Med Chem 18: 1244-51 (2010)
Sun Yat-Sen University
Design, synthesis and biological evaluation of chrysin long-chain derivatives as potential anticancer agents.
Bioorg Med Chem 18: 1117-23 (2010)
Nanjing University
Discorhabdins from the Korean marine sponge Sceptrella sp.
J Nat Prod 73: 258-62 (2010)
Seoul National University
Rational design of indoleamine 2,3-dioxygenase inhibitors.
J Med Chem 53: 1172-89 (2010)
Institute For Cancer Research
Fructose-1,6-bisphosphatase Inhibitors. 2. Design, synthesis, and structure-activity relationship of a series of phosphonic acid containing benzimidazoles that function as 5'-adenosinemonophosphate (AMP) mimics.
J Med Chem 53: 441-51 (2010)
Metabasis Therapeutics
Antiangiogenic effect of dual/selective alpha(5)beta(1)/alpha(v)beta(3) integrin antagonists designed on partially modified retro-inverso cyclotetrapeptide mimetics.
J Med Chem 53: 106-18 (2010)
Universita Degli Studi Di Bologna
Heat shock protein 90: inhibitors in clinical trials.
J Med Chem 53: 3-17 (2010)
Biogen Idec
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
J Med Chem 53: 1347-56 (2010)
University Of Illinois At Chicago
Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines.
J Med Chem 53: 1392-6 (2010)
National Taiwan University
Novel oxadiazole analogues derived from ethacrynic acid: design, synthesis, and structure-activity relationships in inhibiting the activity of glutathione S-transferase P1-1 and cancer cell proliferation.
J Med Chem 53: 1015-22 (2010)
Shandong University
Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models.
Mol Cancer Ther 9: 134-44 (2010)
Hoffmann-La Roche
Identification of potential and selective collagenase, gelatinase inhibitors from Crataegus pinnatifida.
Bioorg Med Chem Lett 20: 991-3 (2010)
Wonkwang University Sanbon Medical Center
Potent transglutaminase inhibitors, aryl beta-aminoethyl ketones.
Bioorg Med Chem Lett 20: 1141-4 (2010)
Institute Of Physical And Chemical Research (Riken)
Design, synthesis, and evaluation of 2-aryl-7-(3',4'-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines as novel PDE-4 inhibitors.
Bioorg Med Chem Lett 20: 922-6 (2010)
Korea Research Institute Of Chemical Technology
Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase.
Bioorg Med Chem Lett 20: 862-5 (2010)
Academy Of Sciences Of The Czech Republic
Prediction of acetylcholinesterase inhibitors and characterization of correlative molecular descriptors by machine learning methods.
Eur J Med Chem 45: 1167-72 (2010)
Sichuan University
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.
J Med Chem 53: 1086-97 (2010)
Genentech
Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach.
Eur J Med Chem 45: 1133-9 (2010)
Chinese Academy Of Sciences
Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism.
J Med Chem 53: 1338-46 (2010)
Solvay Pharma
Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators.
J Med Chem 53: 1270-80 (2010)
Bristol-Myers Squibb
2,4,6-trisubstituted triazines as protein a mimetics for the treatment of autoimmune diseases.
J Med Chem 53: 1138-45 (2010)
Prometic Biosciences
A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors.
Bioorg Med Chem 18: 1273-9 (2010)
Sapienza University Of Rome
Synthesis and structural and pharmacological properties of cyclopropane-based conformationally restricted analogs of 4-methylhistamine as histamine H3/H4 receptor ligands.
Bioorg Med Chem 18: 1076-82 (2010)
Hokkaido University
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.
Bioorg Med Chem 18: 630-9 (2010)
Wyeth Research
Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.
Bioorg Med Chem 18: 590-6 (2010)
Institute For Medical Research
New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein.
Bioorg Med Chem Lett 20: 954-7 (2010)
University Of Glasgow
Discovery and optimization of RO-85, a novel drug-like, potent, and selective P2X3 receptor antagonist.
Bioorg Med Chem Lett 20: 1031-6 (2010)
Roche Palo Alto
Polar 3-alkylidene-5-pivaloyloxymethyl-5'-hydroxymethyl-gamma-lactones as protein kinase C ligands and antitumor agents.
Bioorg Med Chem Lett 20: 1008-12 (2010)
Seoul National University
9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites.
Bioorg Med Chem Lett 20: 935-8 (2010)
Virginia Commonwealth University
Synthesis, antimalarial and antitubercular activity of acetylenic chalcones.
Bioorg Med Chem Lett 20: 942-4 (2010)
University Of Cape Town
Structure-based drug design of tricyclic 8H-indeno[1,2-d][1,3]thiazoles as potent FBPase inhibitors.
Bioorg Med Chem Lett 20: 1004-7 (2010)
Daiichi Sankyo
Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).
Bioorg Med Chem 18: 1204-12 (2010)
University Of Pavia
Synthesis and structure-activity relationship of 1,2,4-triazole-containing diarylpyrazolyl carboxamide as CB1 cannabinoid receptor-ligand.
Bioorg Med Chem 18: 1149-62 (2010)
Green Cross
An octahydro-cyclopenta[c]pyrrole series of inhibitors of the type 1 glycine transporter.
Bioorg Med Chem Lett 20: 907-11 (2010)
Pfizer
Phenylacetic acid regioisomers possessing a N-difluoromethyl-1,2-dihydropyrid-2-one pharmacophore: evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.
Bioorg Med Chem Lett 20: 896-902 (2010)
University Of Alberta
Discovery of cyclicsulfonamide derivatives as 11beta-hydroxysteroid dehydrogenase 1 inhibitors.
Bioorg Med Chem Lett 20: 1065-9 (2010)
Korea University
Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length.
Bioorg Med Chem Lett 20: 997-9 (2010)
Graduate School Of Life Science And Systems Engineering
Discovery and SAR of substituted 3-oxoisoindoline-4-carboxamides as potent inhibitors of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Bioorg Med Chem Lett 20: 1023-6 (2010)
Abbott Laboratories
Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors.
Eur J Med Chem 45: 1158-66 (2010)
National Organization For Drug Control & Research
Inhibition of IKK-beta: a new development in the mechanism of the anti-obesity effects of PTP1B inhibitors SA18 and SA32.
Bioorg Med Chem Lett 20: 1075-7 (2010)
Inha University
Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem.
Bioorg Med Chem Lett 20: 918-21 (2010)
Merck Research Labs
Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors.
J Med Chem 53: 942-50 (2010)
Schering-Plough Research Institute
Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.
J Med Chem 53: 951-65 (2010)
Schering-Plough Research Institute
Urotensin-II receptor modulators as potential drugs.
J Med Chem 53: 2695-708 (2010)
Johnson & Johnson Pharmaceutical Research & Development
Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.
J Med Chem 53: 1222-37 (2010)
Pfizer
[Lys(DOTA)4]BVD15, a novel and potent neuropeptide Y analog designed for Y1 receptor-targeted breast tumor imaging.
Bioorg Med Chem Lett 20: 950-3 (2010)
Universit£
Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.
Bioorg Med Chem Lett 20: 1237-40 (2010)
Wyeth Research
Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specific sirtinol analogues.
J Med Chem 53: 1407-11 (2010)
Institute Of Psychiatry And Neuroscience Of Paris
Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist.
J Med Chem 53: 1319-28 (2010)
Chinese Academy Of Sciences
Optimization of a pipemidic acid autotaxin inhibitor.
J Med Chem 53: 1056-66 (2010)
The University Of Memphis
Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.
J Med Chem 53: 1004-14 (2010)
New Mexico State University
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-(substituted phenyl)epibatidine analogues. Nicotinic partial agonists.
J Nat Prod 73: 306-12 (2010)
Research Triangle Institute
Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.
J Med Chem 53: 1238-49 (2010)
Wyeth Research
Development of (S)-N6-(2-(4-(isoquinolin-1-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]-thiazole-2,6-diamine and its analogue as a D3 receptor preferring agonist: potent in vivo activity in Parkinson's disease animal models.
J Med Chem 53: 1023-37 (2010)
Wayne State University
Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.
J Med Chem 53: 1067-75 (2010)
Philipps University Marburg
Antifolate and antiproliferative activity of 6,8,10-triazaspiro[4.5]deca-6,8-dienes and 1,3,5-triazaspiro[5.5]undeca-1,3-dienes.
Bioorg Med Chem 18: 737-43 (2010)
National University Of Singapore
Towards the synthesis of bisubstrate inhibitors of protein farnesyltransferase: Synthesis and biological evaluation of new farnesylpyrophosphate analogues.
Bioorg Med Chem 18: 543-56 (2010)
Centre De Recherche De Gif-Sur-Yvette
2-Dialkynyl derivatives of (N)-methanocarba nucleosides: 'Clickable' A(3) adenosine receptor-selective agonists.
Bioorg Med Chem 18: 508-17 (2010)
Niddk
Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective beta(2)-adrenergic receptor agonists.
Bioorg Med Chem 18: 728-36 (2010)
Medical University Of Lublin
Fluoroalkene modification of mercaptoacetamide-based histone deacetylase inhibitors.
Bioorg Med Chem 18: 605-11 (2010)
Saga University
Triazoloacridin-6-ones as novel inhibitors of the quinone oxidoreductases NQO1 and NQO2.
Bioorg Med Chem 18: 696-706 (2010)
University Of Manchester And Manchester Cancer Research Center
Novel anilinophthalimide derivatives as potential probes for beta-amyloid plaque in the brain.
Bioorg Med Chem 18: 1337-43 (2010)
Beijing Normal University
Oxime carbamate--discovery of a series of novel FAAH inhibitors.
Bioorg Med Chem Lett 20: 1272-7 (2010)
Bristol-Myers Squibb Research & Development
Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core.
Eur J Med Chem 45: 870-82 (2010)
Link£Ping University
Synthesis and investigation of inhibition effect of fluorinated sulfonamide derivatives on carbonic anhydrase.
Eur J Med Chem 45: 1225-9 (2010)
University Of Montpellier
Structure of aldehyde reductase in ternary complex with a 5-arylidene-2,4-thiazolidinedione aldose reductase inhibitor.
Eur J Med Chem 45: 1140-5 (2010)
Monash University (Parkville Campus)
Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters.
Bioorg Med Chem 18: 640-9 (2010)
University Of Kentucky
2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety.
Bioorg Med Chem Lett 20: 1019-22 (2010)
Merck Research Laboratories
Novel small molecule bradykinin B1 receptor antagonists. Part 3: hydroxyurea derivatives.
Bioorg Med Chem Lett 20: 1233-6 (2010)
Jerini
Asymmetric syntheses of daedalin A and quercinol and their tyrosinase inhibitory activity.
Bioorg Med Chem Lett 20: 1063-4 (2010)
Shinshu University
Synthesis and hSERT activity of homotryptamine analogs. Part 6: [3+2] dipolar cycloaddition of 3-vinylindoles.
Bioorg Med Chem Lett 20: 1027-30 (2010)
Bristol-Myers Squibb
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
Bioorg Med Chem Lett 20: 1241-6 (2010)
Purdue University
Design and synthesis of selective inhibitors of placental alkaline phosphatase.
Bioorg Med Chem 18: 573-9 (2010)
Human Biomolecular Research Institute
Click synthesis of estradiol-cyclodextrin conjugates as cell compartment selective estrogens.
Bioorg Med Chem 18: 809-21 (2010)
University Of Illinois At Chicago
Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers.
Bioorg Med Chem 18: 612-20 (2010)
Hadassah Hebrew University Hospital
Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies.
Bioorg Med Chem Lett 20: 1084-9 (2010)
Solvay Pharma
Piperidine-based heterocyclic oxalyl amides as potent p38alpha MAP kinase inhibitors.
Bioorg Med Chem Lett 20: 1059-62 (2010)
Scios
Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists.
Bioorg Med Chem Lett 20: 1114-7 (2010)
Pfizer
Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 20: 1106-8 (2010)
F. Hoffmann-La Roche
Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.
Bioorg Med Chem Lett 20: 1219-24 (2010)
Novartis Institutes For Biomedical Research
Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Bioorg Med Chem Lett 20: 1109-13 (2010)
F. Hoffmann-La Roche
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.
Bioorg Med Chem Lett 20: 1177-80 (2010)
7Tm Pharma
Molecular design of small organic molecules based on structural information for a conformationally constrained peptide that binds to G-CSF receptor.
Bioorg Med Chem Lett 20: 1169-72 (2010)
Osaka Prefecture University
Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).
Bioorg Med Chem Lett 20: 1094-9 (2010)
Irbm/Merck Research Laboratories
Synthesis and activity of amides of tripeptides as potential urokinase inhibitors.
J Enzyme Inhib Med Chem 25: 139-42 (2010)
Medical University Of Bialystok
New antihyperglycemic, alpha-glucosidase inhibitory, and cytotoxic derivatives of benzimidazoles.
J Enzyme Inhib Med Chem 25: 80-6 (2010)
Indian Institute Of Chemical Technology
Stereoselective inhibition of butyrylcholinesterase by enantiomers of exo- and endo-2-norbornyl-N-n-butylcarbamates.
J Enzyme Inhib Med Chem 25: 13-20 (2010)
Chung Shan Medical University Hospital
Fluorobenzoyl dipeptidyl derivatives as inhibitors of the Fasciola hepatica cysteine protease cathepsin L1.
J Enzyme Inhib Med Chem 25: 1-12 (2010)
Dublin City University
Benzo[e]isoindole-1,3-diones as potential inhibitors of glycogen synthase kinase-3 (GSK-3). Synthesis, kinase inhibitory activity, zebrafish phenotype, and modeling of binding mode.
J Med Chem 53: 994-1003 (2010)
Peking University
Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins).
J Med Chem 53: 1383-6 (2010)
Ludwig-Maximilians-Universit£T M£Nchen
Inhibition of AcpA phosphatase activity with ascorbate attenuates Francisella tularensis intramacrophage survival.
J Biol Chem 285: 5171-7 (2010)
University Of Florida
Mechanism of hepatitis C virus RNA polymerase inhibition with dihydroxypyrimidines.
Antimicrob Agents Chemother 54: 977-83 (2010)
Mcgill University
High throughput receptor-based virtual screening under ZINC database, synthesis, and biological evaluation of ketol-acid reductoisomerase inhibitors.
Chem Biol Drug Des 75: 228-32 (2010)
Nankai University
The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors.
J Med Chem 53: 850-4 (2010)
Universit£
Micropeptins from an Israeli fishpond water bloom of the cyanobacterium Microcystis sp.
J Nat Prod 73: 352-8 (2010)
Tel-Aviv University
Using NMR solvent water relaxation to investigate metalloenzyme-ligand binding interactions.
J Med Chem 53: 867-75 (2010)
University Of Oxford
Probing Torpedo californica acetylcholinesterase catalytic gorge with two novel bis-functional galanthamine derivatives.
J Med Chem 53: 745-51 (2010)
Istituto Di Cristallografia
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.
Bioorg Med Chem Lett 20: 1128-33 (2010)
Bristol-Myers Squibb
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2.
Bioorg Med Chem Lett 20: 1181-5 (2010)
7Tm Pharma
Molecular modeling study of 4-phenylpiperazine and 4-phenyl-1,2,3,6-tetrahydropyridine derivatives: a new step towards the design of high-affinity 5-HT1A ligands.
Bioorg Med Chem Lett 20: 1118-23 (2010)
University Of Li£Ge
Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.
Bioorg Med Chem Lett 20: 1100-5 (2010)
Merck Research Laboratories
Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2.
Bioorg Med Chem 18: 707-18 (2010)
The Institute Of Cancer Research
Synthesis and biological evaluation of new potential inhibitors of N-acylethanolamine hydrolyzing acid amidase.
Bioorg Med Chem Lett 20: 1210-3 (2010)
University Of Salerno
Synthesis and antidepressant activity of optical isomers of 2-(4-benzylpiperazin-1-yl)-1-(5-chloro-6-methoxynaphthalen-2-yl) propan-1-ol (SIPI5056).
Bioorg Med Chem Lett 20: 1256-9 (2010)
Institute Of Pharmaceutical Industry
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.
Bioorg Med Chem Lett 20: 1189-93 (2010)
Schering-Plough Research Institute
5'-O-Dephosphorylated 2',5'-oligoadenylate (2-5A) with 8-methyladenosine at the 2'-terminus activates human RNase L.
Bioorg Med Chem Lett 20: 1186-8 (2010)
Gifu University
Natural ortho-dihydroxyisoflavone derivatives from aged Korean fermented soybean paste as potent tyrosinase and melanin formation inhibitors.
Bioorg Med Chem Lett 20: 1162-4 (2010)
Amorepacific
2,3-Diaminopyrazines as rho kinase inhibitors.
Bioorg Med Chem Lett 20: 1137-40 (2010)
Amri
Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists.
Bioorg Med Chem Lett 20: 1173-6 (2010)
Merck Research Laboratories
Design and synthesis of novel bis-oximinoalkanoic acids as potent PPARalpha agonists.
Bioorg Med Chem Lett 20: 1156-61 (2010)
Zydus Research Centre
Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators.
Bioorg Med Chem Lett 20: 1269-71 (2010)
Merck Research Laboratories
In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.
ACS Chem Biol 5: 245-53 (2010)
Vanderbilt University
Molassamide, a depsipeptide serine protease inhibitor from the marine cyanobacterium Dichothrix utahensis.
J Nat Prod 73: 459-62 (2010)
Smithsonian Marine Station At Ft. Pierce
Novel KCNQ2/Q3 agonists as potential therapeutics for epilepsy and neuropathic pain.
J Med Chem 53: 887-96 (2010)
Icagen
Diaryl piperidines as CB1 receptor antagonists.
Bioorg Med Chem Lett 20: 1278-83 (2010)
Merck Research Laboratories
Development of near-infrared fluorophore (NIRF)-labeled activity-based probes for in vivo imaging of legumain.
ACS Chem Biol 5: 233-43 (2010)
Stanford University
Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
J Med Chem 53: 822-39 (2010)
Congenia
Novel small molecule bradykinin B1 receptor antagonists. Part 2: 5-membered diaminoheterocycles.
Bioorg Med Chem Lett 20: 1229-32 (2010)
Jerini
Biaryl piperidines as potent and selective delta opioid receptor ligands.
Bioorg Med Chem Lett 20: 503-7 (2010)
Pfizer
Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Bioorg Med Chem Lett 20: 448-52 (2010)
Irbm-Merck Research Laboratories Rome
Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood-brain-barrier.
Bioorg Med Chem Lett 20: 453-7 (2010)
7Tm Pharma
Inhibition of Yersinia protein tyrosine phosphatase by phosphonate derivatives of calixarenes.
Bioorg Med Chem Lett 20: 483-7 (2010)
National Academy Of Sciences Of Ukraine
Novel small molecule bradykinin B1 receptor antagonists. Part 1: benzamides and semicarbazides.
Bioorg Med Chem Lett 20: 1225-8 (2010)
Jerini
Inhibition studies of soybean (Glycine max) urease with heavy metals, sodium salts of mineral acids, boric acid, and boronic acids.
J Enzyme Inhib Med Chem 25: 646-52 (2010)
Banaras Hindu University
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.
J Med Chem 52: 7958-61 (2009)
Universita Di Perugia
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.
J Med Chem 52: 7938-41 (2009)
Vertex Pharmaceuticals
N-sulfonylanthranilic acid derivatives as allosteric inhibitors of dengue viral RNA-dependent RNA polymerase.
J Med Chem 52: 7934-7 (2009)
Novartis Institute For Tropical Diseases
Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai.
J Med Chem 53: 778-86 (2010)
University Of Innsbruck
Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors.
Bioorg Med Chem Lett 20: 488-92 (2010)
Irbm-Merck Research Laboratories Rome
Synthesis, characterization and antiglaucoma activity of a novel proton transfer compound and a mixed-ligand Zn(II) complex.
Bioorg Med Chem 18: 930-8 (2010)
Dumlupinar University
A diazirine-based photoaffinity etoposide probe for labeling topoisomerase II.
Bioorg Med Chem 18: 830-8 (2010)
University Of Manitoba
Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation.
Bioorg Med Chem 18: 822-9 (2010)
Deutsches Krebsforschungszentrum
Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.
Bioorg Med Chem Lett 20: 684-8 (2010)
Glaxosmithkline
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.
Bioorg Med Chem Lett 20: 618-22 (2010)
Glaxosmithkline
Novel spiropiperidine-based stearoyl-CoA desaturase-1 inhibitors: Identification of 1'-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-5-(trifluoromethyl)-3,4-dihydrospiro[chromene-2,4'-piperidine].
Bioorg Med Chem Lett 20: 746-54 (2010)
Daiichi Sankyo
2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.
Bioorg Med Chem Lett 20: 673-8 (2010)
Glaxosmithkline
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
Bioorg Med Chem Lett 20: 526-30 (2010)
Wyeth Pharmaceuticals
Development of carbohydrate-derived inhibitors of acid sphingomyelinase.
Bioorg Med Chem 18: 939-44 (2010)
Humboldt Universit£T Zu Berlin
1-Indol-1-yl-propan-2-ones and related heterocyclic compounds as dual inhibitors of cytosolic phospholipase A(2)alpha and fatty acid amide hydrolase.
Bioorg Med Chem 18: 945-52 (2010)
University Of M£Nster
Characterization of non-lipid autotaxin inhibitors.
Bioorg Med Chem 18: 769-76 (2010)
The University Of Memphis
Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles.
Bioorg Med Chem Lett 20: 763-6 (2010)
Minase Research Institute
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
Bioorg Med Chem Lett 20: 521-5 (2010)
Wyeth Pharmaceuticals
Non-aromatic A-ring replacement in the triaryl bis-sulfone CB2 receptor inhibitors.
Bioorg Med Chem Lett 20: 608-11 (2010)
Merck Research Laboratories
Novel thioamide derivatives as neutral CB1 receptor antagonists.
Bioorg Med Chem Lett 20: 479-82 (2010)
Astrazeneca R & D M£Lndal
Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB(2) agonists for the treatment of inflammatory pain.
Bioorg Med Chem Lett 20: 465-8 (2010)
Glaxosmithkline
Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitors.
Bioorg Med Chem 18: 855-62 (2010)
Islamic Azad University
Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumor agents.
Bioorg Med Chem 18: 880-6 (2010)
Nanjing University
Probes for narcotic receptor mediated phenomena. 40. N-substituted cis-4a-ethyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-8-ols.
Bioorg Med Chem 18: 91-9 (2010)
Nida
The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators.
Bioorg Med Chem Lett 20: 493-8 (2010)
Amgen
Synthesis and in vivo evaluation of bicyclic gababutins.
Bioorg Med Chem Lett 20: 461-4 (2010)
Pfizer
2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.
Bioorg Med Chem Lett 20: 679-83 (2010)
Glaxosmithkline
Isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists.
Bioorg Med Chem Lett 20: 726-9 (2010)
Banyu Tsukuba Research Institute
Fluorinated piperidine acetic acids as gamma-secretase modulators.
Bioorg Med Chem Lett 20: 755-8 (2010)
Merck Research Laboratories
Discovery of (pyridin-4-yl)-2H-tetrazole as a novel scaffold to identify highly selective matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis.
Bioorg Med Chem Lett 20: 576-80 (2010)
Pfizer
The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.
Bioorg Med Chem Lett 20: 759-62 (2010)
Glaxosmithkline
3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. Part 1: discovery and exploration of the carboxyamide side chain.
Bioorg Med Chem 18: 80-90 (2010)
Minase Research Institute
Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.
Bioorg Med Chem Lett 20: 558-62 (2010)
Vanderbilt University Medical Center
Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa.
Bioorg Med Chem Lett 20: 513-5 (2010)
Korea Research Institute Of Bioscience And Biotechnology
Synthesis and PGE(2) production inhibition of 1H-furan-2,5-dione and 1H-pyrrole-2,5-dione derivatives.
Bioorg Med Chem Lett 20: 734-7 (2010)
Kyung Hee University
Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles.
Bioorg Med Chem Lett 20: 704-8 (2010)
Roche Palo Alto
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
Bioorg Med Chem Lett 20: 499-502 (2010)
Merck Frosst Centre For Therapeutic Research
Identification of a new class of small molecule C5a receptor antagonists.
Bioorg Med Chem Lett 20: 662-4 (2010)
Wyeth Research
Through the"gatekeeper door": exploiting the active kinase conformation.
J Med Chem 53: 2681-94 (2010)
Nerviano Medical Sciences
Dual-action lipophilic iminosugar improves glycemic control in obese rodents by reduction of visceral glycosphingolipids and buffering of carbohydrate assimilation.
J Med Chem 53: 689-98 (2010)
Leiden University
Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.
J Med Chem 53: 759-77 (2010)
Boehringer Ingelheim Pharmaceuticals
Recent advances in the discovery of competitive protein tyrosine phosphatase 1B inhibitors for the treatment of diabetes, obesity, and cancer.
J Med Chem 53: 2333-44 (2010)
Incyte
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