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Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.
J Med Chem 48: 4596-607 (2005)
Serono Pharmaceutical Research Institute
Identification of novel extracellular signal-regulated kinase docking domain inhibitors.
J Med Chem 48: 4586-95 (2005)
University Of Maryland
Adamantyl cannabinoids: a novel class of cannabinergic ligands.
J Med Chem 48: 4576-85 (2005)
Northeastern University
Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase.
J Med Chem 48: 4547-57 (2005)
Irbm (Merck Research Laboratories Rome)
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.
J Med Chem 48: 4535-46 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and biological evaluation of geminal disulfones as HIV-1 integrase inhibitors.
J Med Chem 48: 4526-34 (2005)
University Of California
Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography.
J Med Chem 48: 4511-25 (2005)
Aventis Pharma
Design and synthesis of new nonsteroidal glucocorticoid modulators through application of an"agreement docking" method.
J Med Chem 48: 4507-10 (2005)
Glaxosmithkline
Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex.
Neuropsychopharmacology 31: 265-77 (2006)
Case Western Reserve University
Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases.
Biochemistry 44: 9430-40 (2005)
Merck Research Laboratories
Inhibition of the severe acute respiratory syndrome 3CL protease by peptidomimetic alpha,beta-unsaturated esters.
Bioorg Med Chem 13: 5240-52 (2005)
National Taiwan University
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.
Bioorg Med Chem Lett 15: 3834-7 (2005)
Zhejiang University
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.
Bioorg Med Chem Lett 15: 3665-9 (2005)
Merck Sharp And Dohme Research Laboratories
Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series.
Bioorg Med Chem Lett 15: 3925-9 (2005)
Merck
In vitro antiproliferative activity against human colon cancer cell lines of representative 4-thiazolidinones. Part I.
Bioorg Med Chem Lett 15: 3930-3 (2005)
Università
A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series.
Bioorg Med Chem Lett 15: 3816-20 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues.
Bioorg Med Chem Lett 15: 3744-7 (2005)
Harvard Medical School
Ketoheterocycle-based inhibitors of cathepsin K: a novel entry into the synthesis of peptidic ketoheterocycles.
Bioorg Med Chem Lett 15: 3891-5 (2005)
Glaxosmithkline
Synthesis of benzoyl phenyl benzoates as effective inhibitors for phospholipase A2 and hyaluronidase enzymes.
Bioorg Med Chem Lett 15: 4100-4 (2005)
University Of Mysore
Hydrophobicity in the design of P2/P2' tetrahydropyrimidinone HIV protease inhibitors.
Bioorg Med Chem Lett 15: 3767-70 (2005)
Clarkson University
Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.
Bioorg Med Chem Lett 15: 3758-62 (2005)
University Of Nottingham
2-Aminoquinazoline inhibitors of cyclin-dependent kinases.
Bioorg Med Chem Lett 15: 3881-5 (2005)
Naeja Pharmaceutical
QSAR of adenosine A3 receptor antagonist 1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives using chemometric tools.
Bioorg Med Chem Lett 15: 3737-43 (2005)
Jadavpur University
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.
Bioorg Med Chem Lett 15: 3912-6 (2005)
Merck Research Laboratories
Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.
Bioorg Med Chem Lett 15: 4143-50 (2005)
Seoul National University
Discovery and in vitro evaluation of potent kinase inhibitors: Pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines.
Bioorg Med Chem Lett 15: 3778-81 (2005)
Glaxosmithkline
L-arginine analogs as alternate substrates for nitric oxide synthase.
Bioorg Med Chem Lett 15: 3934-41 (2005)
University Of California
Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives.
Bioorg Med Chem Lett 15: 3732-6 (2005)
Graduate School Of The Chinese Academy Of Sciences
Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.
Bioorg Med Chem Lett 15: 3900-7 (2005)
Bayer Healthcare
BCUT descriptors to predicting affinity toward A3 adenosine receptors.
Bioorg Med Chem Lett 15: 3491-5 (2005)
Experimental Sugar Cane Station&Quot;Villa Clara-Cienfuegos&Quot
The molecular basis for coxib inhibition of p38alpha MAP kinase.
Bioorg Med Chem Lett 15: 3506-9 (2005)
Universidade Federal Do Rio De Janeiro (Ufrj)
Interaction of chiral MS-245 analogs at h5-HT6 receptors.
Bioorg Med Chem Lett 15: 3510-3 (2005)
Virginia Commonwealth University
Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase.
Bioorg Med Chem Lett 15: 3519-23 (2005)
Glaxosmithkline
Synthesis, structure-activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists.
Bioorg Med Chem Lett 15: 3870-3 (2005)
Pharmaceutical Research Institute
Synthesis of an N-acyl sulfamate analog of luciferyl-AMP: a stable and potent inhibitor of firefly luciferase.
Bioorg Med Chem Lett 15: 3860-4 (2005)
Connecticut College
Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives.
J Biol Chem 280: 31220-9 (2005)
Chinese Academy Of Sciences
Structure-activity relationships of novel endomorphin-2 analogues with N-O turns induced by alpha-aminoxy acids.
Bioorg Med Chem Lett 15: 2986-2989 (2005)
TBA
Efficient synthetic inhibitors of anthrax lethal factor.
Proc Natl Acad Sci U S A 102: 9499-504 (2005)
Burnham Institute For Medical Research
Synthesis and structure-activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists.
Bioorg Med Chem Lett 15: 4029-32 (2005)
Pharmaceutical Research Institute
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.
Bioorg Med Chem Lett 15: 3540-6 (2005)
Glaxosmithkline
3-Thio-1,2,4-triazoles, novel somatostatin sst2/sst5 agonists.
Bioorg Med Chem Lett 15: 3555-9 (2005)
Institut Henri Beaufour
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
Bioorg Med Chem Lett 15: 3568-72 (2005)
University Of Virginia
Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1.
Bioorg Med Chem Lett 15: 3514-8 (2005)
Wyeth Research
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.
Bioorg Med Chem Lett 15: 3501-5 (2005)
Merck Research Laboratories
Investigation of glycine alpha-ketoamide HCV NS3 protease inhibitors: effect of carboxylic acid isosteres.
Bioorg Med Chem Lett 15: 3487-90 (2005)
Pharmaceutical Research Institute
Discovery and SAR of biaryl piperidine MCH1 receptor antagonists through solid-phase encoded combinatorial synthesis.
Bioorg Med Chem Lett 15: 3696-700 (2005)
Pharmacopeia Drug Discovery
SAR studies of 6-aryl-1,3-dihydrobenzimidazol-2-ones as progesterone receptor antagonists.
Bioorg Med Chem Lett 15: 3600-3 (2005)
Wyeth Research
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: highly potent, orally active, adenosine A2A antagonists. Part 1.
Bioorg Med Chem Lett 15: 3670-4 (2005)
Schering-Plough Research Institute
Dibenzodioxocinones--a new class of CETP inhibitors.
Bioorg Med Chem Lett 15: 3611-4 (2005)
Bayer Healthcare Pharma Research
Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors.
Bioorg Med Chem Lett 15: 3560-4 (2005)
Glaxosmithkline
Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.
Bioorg Med Chem Lett 15: 3604-8 (2005)
Vernalis Research
Features of selective kinase inhibitors.
Chem Biol 12: 621-37 (2005)
University Of California San Francisco
Terpenoid tetrahydroisoquinoline alkaloids emetine, klugine, and isocephaeline inhibit the activation of hypoxia-inducible factor-1 in breast tumor cells.
J Nat Prod 68: 947-50 (2005)
University Of Mississippi
Constituents of the leaves of Macaranga tanarius.
J Nat Prod 68: 927-30 (2005)
Ramkhamhaeng University
Indole alkaloids and other constituents of Rauwolfia serpentina.
J Nat Prod 68: 848-52 (2005)
Kobe Pharmaceutical University
Discovery of potent anilide inhibitors against the severe acute respiratory syndrome 3CL protease.
J Med Chem 48: 4469-73 (2005)
National Taiwan University
Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.
J Med Chem 48: 4457-68 (2005)
Merck Research Laboratories
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.
J Med Chem 48: 4444-56 (2005)
University Of Bologna
Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain.
J Med Chem 48: 4420-31 (2005)
Harvard Medical School
Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1.
J Med Chem 48: 4410-9 (2005)
Martin-Luther-University Halle-Wittenberg
Design and synthesis of potent inhibitors of plasmepsin I and II: X-ray crystal structure of inhibitor in complex with plasmepsin II.
J Med Chem 48: 4400-9 (2005)
LinköPing University
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
J Med Chem 48: 4378-88 (2005)
Sapienza University Of Rome
Quinic acid derivatives as sialyl Lewis(x)-mimicking selectin inhibitors: design, synthesis, and crystal structure in complex with E-selectin.
J Med Chem 48: 4346-57 (2005)
Wyeth
Structure-based design of novel Chk1 inhibitors: insights into hydrogen bonding and protein-ligand affinity.
J Med Chem 48: 4332-45 (2005)
Vernalis (R&D)
2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.
J Med Chem 48: 4312-31 (2005)
Domp£
Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands.
J Med Chem 48: 4254-65 (2005)
Emory University
Functionalized pyrrolidines inhibit alpha-mannosidase activity and growth of human glioblastoma and melanoma cells.
J Med Chem 48: 4237-46 (2005)
Institute Of Chemical Sciences And Engineering
Peptoid-peptide hybrids as potent novel melanocortin receptor ligands.
J Med Chem 48: 4224-30 (2005)
Utrecht University
Design, synthesis, and biological activities of pyrrolylethanoneamine derivatives, a novel class of monoamine oxidases inhibitors.
J Med Chem 48: 4220-3 (2005)
Sapienza University Of Rome
A three-dimensional pharmacophore model for 5-hydroxytryptamine6 (5-HT6) receptor antagonists.
J Med Chem 48: 4216-9 (2005)
Universidad Complutense
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.
J Med Chem 48: 4212-5 (2005)
Vernalis (R&D)
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.
J Med Chem 48: 4208-11 (2005)
Johnson & Johnson Pharmaceutical
Ligand binding analysis for human alpha5beta1 integrin: strategies for designing new alpha5beta1 integrin antagonists.
J Med Chem 48: 4204-7 (2005)
Università
Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.
J Med Chem 48: 4200-3 (2005)
Eli Lilly
Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase.
J Enzyme Inhib Med Chem 20: 135-41 (2005)
Cardiff University
3-(1,2,3-Triazol-1-yl)-1-thio-galactosides as small, efficient, and hydrolytically stable inhibitors of galectin-3.
Bioorg Med Chem Lett 15: 3344-6 (2005)
Lund University
Rhodanine derivatives as inhibitors of JSP-1.
Bioorg Med Chem Lett 15: 3374-9 (2005)
Ceptyr
Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1.
Cancer Res 65: 5399-407 (2005)
Cyclacel
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.
Bioorg Med Chem Lett 15: 3407-11 (2005)
Glaxosmithkline
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.
Bioorg Med Chem Lett 15: 3338-43 (2005)
The Institute Of Cancer Research
RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.
Bioorg Med Chem 13: 4835-41 (2005)
Hoffmann-La Roche
Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis.
Bioorg Med Chem Lett 15: 3691-5 (2005)
Pharmacopeia Drug Discovery
Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886.
Bioorg Med Chem Lett 15: 3352-5 (2005)
Merck Frosst Centre For Therapeutic Research
Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13.
Bioorg Med Chem Lett 15: 3385-8 (2005)
Pfizer
Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to kappa-opioid receptors.
Biochemistry 44: 8643-51 (2005)
Case Western Reserve University
Differential effects of the 5-hydroxytryptamine (5-HT)1A receptor inverse agonists Rec 27/0224 and Rec 27/0074 on electrophysiological responses to 5-HT1A receptor activation in rat dorsal raphe nucleus and hippocampus in vitro.
J Pharmacol Exp Ther 315: 109-17 (2005)
Universit&Aagrove
Lecozotan (SRA-333): a selective serotonin 1A receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties.
J Pharmacol Exp Ther 314: 1274-89 (2005)
Wyeth
Deoxyribosyl analogues of methionyl and isoleucyl sulfamate adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.
Bioorg Med Chem Lett 15: 3389-93 (2005)
Seoul National University
1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.
Bioorg Med Chem Lett 15: 3430-3 (2005)
Merck Research Laboratories
Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists.
Bioorg Med Chem Lett 15: 3685-90 (2005)
Neurocrine Biosciences
Isomeric thiazole derivatives as ligands for the neuropeptide Y5 receptor.
Bioorg Med Chem Lett 15: 3446-9 (2005)
F. Hoffmann-La Roche
Structure-driven HtL: design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity.
Bioorg Med Chem Lett 15: 3459-62 (2005)
Astrazeneca
Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 15: 3434-8 (2005)
Neurocrine Biosciences
Synthesis and structure-activity relationships of biarylcarboxamide bis-aminopyrrolidine urea derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).
Bioorg Med Chem Lett 15: 3439-45 (2005)
Neurocrine Biosciences
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.
Bioorg Med Chem Lett 15: 3402-6 (2005)
Glaxosmithkline
(2R)-2-methylchromane-2-carboxylic acids: discovery of selective PPARalpha agonists as hypolipidemic agents.
Bioorg Med Chem Lett 15: 3347-51 (2005)
Merck Research Laboratories
Identification of aminopiperidine benzamides as MCHr1 antagonists.
Bioorg Med Chem Lett 15: 3412-6 (2005)
Abbott Laboratories
Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease.
Biochem Biophys Res Commun 333: 194-9 (2005)
National Taiwan University
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
J Pharmacol Exp Ther 314: 1310-21 (2005)
Vrije Universiteit Amsterdam
Carboxylate bioisosteres of gabapentin.
Bioorg Med Chem Lett 16: 2333-6 (2006)
Pfizer
Rapid computational identification of the targets of protein kinase inhibitors.
J Med Chem 48: 4138-52 (2005)
University Of Iowa
Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.
J Med Chem 48: 4100-10 (2005)
Neurocrine Biosciences
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
J Med Chem 48: 4087-99 (2005)
Arizona State University
Novel nonsteroidal antiinflammatory drugs possessing a nitric oxide donor diazen-1-ium-1,2-diolate moiety: design, synthesis, biological evaluation, and nitric oxide release studies.
J Med Chem 48: 4061-7 (2005)
University Of Alberta
Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.
J Med Chem 48: 4049-60 (2005)
Universit£
Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4. An unexpected effect of the chirality of Trp8 on NMR spectra in methanol.
J Med Chem 48: 4025-30 (2005)
University Of Pennsylvania
New selective AT2 receptor ligands encompassing a gamma-turn mimetic replacing the amino acid residues 4-5 of angiotensin II act as agonists.
J Med Chem 48: 4009-24 (2005)
Uppsala University
Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.
J Med Chem 48: 3991-4008 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.
J Med Chem 48: 3980-90 (2005)
Abbott Laboratories
ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.
J Med Chem 48: 3953-79 (2005)
Wyeth Research
Examination of phosphoryl-mimicking functionalities within a macrocyclic Grb2 SH2 domain-binding platform.
J Med Chem 48: 3945-8 (2005)
National Cancer Institute-Frederick
Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia.
Bioorg Med Chem Lett 15: 3197-200 (2005)
Merck Research Laboratories
Sialyl Lewis(x) analogs based on a quinic acid scaffold as the fucose mimic.
Bioorg Med Chem Lett 15: 3224-8 (2005)
National Chemical Engineering Institute In Paris
Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists.
Bioorg Med Chem Lett 15: 3229-32 (2005)
Glaxosmithkline
A three-residue, continuous binding epitope peptidomimetic of ShK toxin as a Kv1.3 inhibitor.
Bioorg Med Chem Lett 15: 3193-6 (2005)
Institute Of Medical Research
Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2.
Bioorg Med Chem Lett 15: 3279-83 (2005)
Fujisawa Pharmaceutical
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
Bioorg Med Chem Lett 15: 3284-7 (2005)
Fujisawa Pharmaceutical
Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist.
Bioorg Med Chem Lett 15: 3292-5 (2005)
Roche Palo Alto
Ethers of 3-hydroxyphenylacetic acid as selective gamma-hydroxybutyric acid receptor ligands.
Bioorg Med Chem Lett 15: 3201-2 (2005)
University Of Maryland
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.
Bioorg Med Chem Lett 15: 3271-5 (2005)
National Health Research Institutes
6-(2-Phenylethyl)nicotine: a novel nicotinic cholinergic receptor ligand.
Bioorg Med Chem Lett 15: 3237-40 (2005)
Virginia Commonwealth University
Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives.
Bioorg Med Chem Lett 15: 3241-6 (2005)
Semmelweis University
Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.
Bioorg Med Chem Lett 15: 3203-6 (2005)
Glaxosmithkline
Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors.
Bioorg Med Chem Lett 15: 3257-62 (2005)
Peking University
Novel phomactin analogues as PAF receptor ligands.
Bioorg Med Chem Lett 15: 3263-6 (2005)
The University Of Nottingham
Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents.
Bioorg Med Chem Lett 15: 3296-301 (2005)
Merck Research Laboratories
Petrosamine B, an inhibitor of the Helicobacter pylori enzyme aspartyl semialdehyde dehydrogenase from the Australian sponge Oceanapia sp.
J Nat Prod 68: 804-6 (2005)
Griffith University
Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound.
J Nat Prod 68: 674-7 (2005)
University Of Antwerp
Structural bioinformatics-based design of selective, irreversible kinase inhibitors.
Science 308: 1318-21 (2005)
University Of California
3-[4-(methylsulfonyl)phenyl]-5-(trifluoromethyl)(2-pyridyl) phenyl ketone as a potent and orally active cyclooxygenase-2 selective inhibitor: synthesis and biological evaluation.
J Med Chem 48: 3930-4 (2005)
Nitromed
Inhibition of herpes simplex virus thymidine kinases by 2-phenylamino-6-oxopurines and related compounds: structure-activity relationships and antiherpetic activity in vivo.
J Med Chem 48: 3919-29 (2005)
Glsynthesis
Synthesis and Src kinase inhibitory activity of 2-phenyl- and 2-thienyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles.
J Med Chem 48: 3891-902 (2005)
Wyeth Research
Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives.
J Med Chem 48: 3858-73 (2005)
Universit£
Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds.
J Med Chem 48: 3852-7 (2005)
Research Triangle Institute
Design, synthesis and antiviral activity of novel 4,5-disubstituted 7-(beta-D-ribofuranosyl)pyrrolo[2,3-d][1,2,3]triazines and the novel 3-amino-5-methyl-1-(beta-D-ribofuranosyl)- and 3-amino-5-methyl-1-(2-deoxy-beta-D-ribofuranosyl)-1,5-dihydro-1,4,5,6,7,8-hexaazaacenaphthylene as analogues of tri
J Med Chem 48: 3840-51 (2005)
University Of Michigan
Design of small-sized libraries by combinatorial assembly of linkers and functional groups to a given scaffold: application to the structure-based optimization of a phosphodiesterase 4 inhibitor.
J Med Chem 48: 3816-22 (2005)
Umr Cnrs 7081
Predictive three-dimensional quantitative structure-activity relationship of cytochrome P450 1A2 inhibitors.
J Med Chem 48: 3808-15 (2005)
University Of Kuopio
Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity.
J Med Chem 48: 3776-83 (2005)
Cephalon
Comparison of ligand-based and structure-based 3D-QSAR approaches: a case study on (aryl-)bridged 2-aminobenzonitriles inhibiting HIV-1 reverse transcriptase.
J Med Chem 48: 3756-67 (2005)
University Of Perugia
Decoys for docking.
J Med Chem 48: 3714-28 (2005)
University Of California San Francisco
Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.
J Med Chem 48: 3704-13 (2005)
University Of Washington At Seattle
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.
J Med Chem 48: 3696-9 (2005)
Friedrich-Alexander University
Synthesis and structure-activity relationship of 4-substituted 2-(2-acetyloxyethyl)-8-(morpholine-4-sulfonyl)pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors.
J Med Chem 48: 3680-3 (2005)
Chemical Diversity Research Institute
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
J Med Chem 48: 3663-79 (2005)
National Institute On Drug Abuse-Intramural Research Program
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
Bioorg Med Chem Lett 15: 3091-5 (2005)
Fujisawa Pharmaceutical
Synthetic lanostane-type triterpenoids as inhibitors of DNA topoisomerase II.
Bioorg Med Chem Lett 15: 2966-9 (2005)
Osaka University Of Pharmaceutical Sciences
New piperidinyl- and 1,2,3,6-tetrahydropyridinyl-pyrimidine derivatives as selective 5-HT1A receptor agonists with highly potent anti-ischemic effects.
Bioorg Med Chem Lett 15: 2990-3 (2005)
Daiichi Suntory Biomedical Research
4-Substituted (benzo[b]thiophene-2-carbonyl)guanidines as novel Na+/H+ exchanger isoform-1 (NHE-1) inhibitors.
Bioorg Med Chem Lett 15: 2998-3001 (2005)
Korea Research Institute Of Chemical Technology
Structure-based design and synthesis of pyrazinones containing novel P1 'side pocket' moieties as inhibitors of TF/VIIa.
Bioorg Med Chem Lett 15: 3006-11 (2005)
Pfizer
Synthesis and characterization of azole isoflavone inhibitors of aromatase.
Bioorg Med Chem 13: 4063-70 (2005)
Ohio State University
Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity.
Bioorg Med Chem Lett 15: 2926-31 (2005)
Merck Research Laboratories
Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity.
Bioorg Med Chem Lett 15: 2918-22 (2005)
Abbott Laboratories
Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists.
Bioorg Med Chem Lett 15: 2910-3 (2005)
Vrije Universiteit Amsterdam
New inhibitors of rabbit muscle triose-phosphate isomerase.
Bioorg Med Chem Lett 15: 2906-9 (2005)
Paris-Sud University
Novel 2-N,N-dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo[2,3-d]oxepin derivatives displaying combined norepinephrine reuptake inhibition and 5-HT2A/2C receptor antagonism.
Bioorg Med Chem Lett 15: 2898-901 (2005)
Janssen-Cilag
Synthesis, in vivo and in vitro biological activity of novel azaline B analogs.
Bioorg Med Chem Lett 15: 2894-7 (2005)
Salk Institute
Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators.
Bioorg Med Chem Lett 15: 2891-3 (2005)
Chinese Academy Of Sciences
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
Bioorg Med Chem Lett 15: 2886-90 (2005)
Reverse Proteomics Research Institute
Evaluation of 3-substituted arginine analogs as selective inhibitors of human nitric oxide synthase isozymes.
Bioorg Med Chem Lett 15: 2881-5 (2005)
Nagoya City University
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides.
Bioorg Med Chem Lett 15: 2870-5 (2005)
Pfizer
Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Bioorg Med Chem Lett 15: 2865-9 (2005)
Wyeth Research
Synthesis and biological evaluation of chromone carboxamides as calpain inhibitors.
Bioorg Med Chem Lett 15: 2857-60 (2005)
Institute Of Science & Technology
Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization.
Bioorg Med Chem Lett 15: 2840-4 (2005)
The Scripps Research Institute
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
Bioorg Med Chem Lett 15: 2824-8 (2005)
Merck Research Laboratories
Design, synthesis, and evaluation of proline based melanocortin receptor ligands.
Bioorg Med Chem Lett 15: 2819-23 (2005)
Procter & Gamble Pharmaceuticals
Inhibitors of HCV NS5B polymerase. Part 2: Evaluation of the northern region of (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid.
Bioorg Med Chem Lett 15: 2812-8 (2005)
Pfizer
Discovery of 3,3-dimethyl-5-hydroxypipecolic hydroxamate-based inhibitors of aggrecanase and MMP-13.
Bioorg Med Chem Lett 15: 2808-11 (2005)
Pfizer
Synthesis and biological evaluation of 6,7-disubstituted 4-aminopyrido[2,3-d]pyrimidines as adenosine kinase inhibitors.
Bioorg Med Chem Lett 15: 2803-7 (2005)
Abbott Laboratories
P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.
Bioorg Med Chem Lett 15: 2771-5 (2005)
Merck Research Laboratories
Synthesis and biological studies of yohimbine derivatives on human alpha2C-adrenergic receptors.
Bioorg Med Chem Lett 15: 2758-60 (2005)
University Of Tennessee
Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Bioorg Med Chem Lett 15: 2752-7 (2005)
Abbott Laboratories
Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase.
Bioorg Med Chem Lett 15: 2734-7 (2005)
Aventis Pharmaceuticals
Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-alpha converting enzyme.
Bioorg Med Chem Lett 15: 2970-3 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.
Bioorg Med Chem Lett 15: 2974-9 (2005)
Pfizer
The synthesis of substituted bipiperidine amide compounds as CCR3 ligands: antagonists versus agonists.
Bioorg Med Chem Lett 15: 3020-3 (2005)
Schering-Plough Research Institute
Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 15: 3048-52 (2005)
Merck Research Laboratories
Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff's bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes.
Bioorg Med Chem Lett 15: 3096-101 (2005)
Ospedale San Lazzaro
QSAR analysis of thiazole benzenesulfonamide substituted 3-pyridylethanolamines as beta3-adrenergic receptor agonist.
Bioorg Med Chem Lett 15: 3167-73 (2005)
S.G.S.I.T.S.
Carbonic anhydrase inhibitors. Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with boron-containing sulfonamides, sulfamides, and sulfamates: toward agents for boron neutron capture therapy of hypoxic tumors.
Bioorg Med Chem Lett 15: 3302-6 (2005)
Università
Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX.
Bioorg Med Chem Lett 15: 3102-8 (2005)
Universit£
Bile salt export pump (BSEP/ABCB11) can transport a nonbile acid substrate, pravastatin.
J Pharmacol Exp Ther 314: 876-82 (2005)
University Of Tokyo
NAD+-dependent DNA Ligase (Rv3014c) from Mycobacterium tuberculosis. Crystal structure of the adenylation domain and identification of novel inhibitors.
J Biol Chem 280: 30273-81 (2005)
India Central Drug Research Institute
Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors.
Bioorg Med Chem Lett 15: 3058-62 (2005)
Development Center For Biotechnology
Acyclic cyanamide-based inhibitors of cathepsin K.
Bioorg Med Chem Lett 15: 3039-43 (2005)
Glaxosmithkline
Structure-activity relationship of N-methyl-bisindolylmaleimide derivatives as cell death inhibitors.
Bioorg Med Chem Lett 15: 3109-13 (2005)
Tohoku University
Glutamylsulfamoyladenosine and pyroglutamylsulfamoyladenosine are competitive inhibitors of E. coli glutamyl-tRNA synthetase.
J Enzyme Inhib Med Chem 20: 61-7 (2005)
Crefsip
Synthesis and inhibitory potential towards acetylcholinesterase, butyrylcholinesterase and lipoxygenase of some variably substituted chalcones.
J Enzyme Inhib Med Chem 20: 41-7 (2005)
Quaid-I-Azam University
Beta-lactam compounds as apparently uncompetitive inhibitors of HIV-1 protease.
Bioorg Med Chem Lett 15: 3086-90 (2005)
University Of Debrecen
Hologram quantitative structure-activity relationships for a series of farnesoid X receptor activators.
Bioorg Med Chem Lett 15: 3119-25 (2005)
Universidade De SãO Paulo
4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 2. SAR.
Bioorg Med Chem Lett 15: 3053-7 (2005)
Bayer Research Center
Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.
J Med Chem 48: 3654-8 (2005)
Universidad Central De Venezuela
Are L-adenosine and its derivatives substrates for S-adenosyl-L-homocysteine hydrolase?
J Med Chem 48: 3649-53 (2005)
Florida International University
A new structural motif for mu-opioid antagonists.
J Med Chem 48: 3644-8 (2005)
Vrije Universiteit Brussel
Optimization of amide-based inhibitors of soluble epoxide hydrolase with improved water solubility.
J Med Chem 48: 3621-9 (2005)
Department Of Entomology And University Of California Davis Cancer Center
Stereoselective binding of indomethacin ethanolamide derivatives to cyclooxygenase-1.
J Med Chem 48: 3613-20 (2005)
Vanderbilt University
Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist.
J Med Chem 48: 3605-12 (2005)
Eli Lilly
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.
J Med Chem 48: 3586-604 (2005)
Central Pharmaceutical Research Institute
Structure-based design: synthesis and biological evaluation of a series of novel cycloamide-derived HIV-1 protease inhibitors.
J Med Chem 48: 3576-85 (2005)
University Of Illinois At Chicago
Further studies on the interaction of the 5-hydroxytryptamine3 (5-HT3) receptor with arylpiperazine ligands. development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory properties.
J Med Chem 48: 3564-75 (2005)
Universit£
AFMoC enhances predictivity of 3D QSAR: a case study with DOXP-reductoisomerase.
J Med Chem 48: 3547-63 (2005)
Philipps University
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
J Med Chem 48: 3478-80 (2005)
Glaxosmithkline
Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation.
J Med Chem 48: 3474-7 (2005)
Pfizer
Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.
J Med Chem 48: 3467-70 (2005)
Wyeth Research
Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative diseases.
J Med Chem 48: 3463-6 (2005)
University Of Southern California
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
J Med Chem 48: 3449-62 (2005)
Monash University (Parkville Campus)
Pyrazole derivatives as photosynthetic electron transport inhibitors: new leads and structure-activity relationship.
J Agric Food Chem 53: 3848-55 (2005)
Universit£
Recognition of benztropine by the dopamine transporter (DAT) differs from that of the classical dopamine uptake inhibitors cocaine, methylphenidate, and mazindol as a function of a DAT transmembrane 1 aspartic acid residue.
J Pharmacol Exp Ther 314: 575-83 (2005)
Duquesne University
Preclinical profile of ciclesonide, a novel corticosteroid for the treatment of asthma.
J Pharmacol Exp Ther 314: 568-74 (2005)
Imperial College
Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives.
Bioorg Med Chem Lett 15: 2790-4 (2005)
Chinese Academy Of Sciences
Synthesis of tricyclic analogs of stephaoxocanidine and their evaluation as acetylcholinesterase inhibitors.
Bioorg Med Chem Lett 15: 2711-5 (2005)
Universidad Nacional De Rosario
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.
Bioorg Med Chem Lett 15: 2943-7 (2005)
Merck Research Laboratories
Total asymmetric synthesis of (-)-conduramine B-1 and of its enantiomer. N-Benzyl derivatives of conduramine B-1 are beta-glucosidase inhibitors.
Bioorg Med Chem Lett 15: 3071-5 (2005)
Ecole Polytechnique FéDéRale De Lausanne (Epfl)
Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones.
Bioorg Med Chem Lett 15: 3137-42 (2005)
Wyeth Research
A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential.
Bioorg Med Chem Lett 15: 3081-5 (2005)
Novartis Institutes For Biomedical Research
The dietary polyphenol ellagic acid is a potent inhibitor of hOAT1.
Drug Metab Dispos 33: 1097-100 (2005)
Medical University Of South Carolina
Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2).
Bioorg Med Chem Lett 15: 2761-5 (2005)
Mclean Hospital
First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors.
Biochemistry 44: 6858-66 (2005)
University Of Bath
Aryl sulfones: a new class of gamma-secretase inhibitors.
Bioorg Med Chem Lett 15: 2685-8 (2005)
Merck Sharp & Dohme Research Laboratories
Non-peptidic alpha(v)beta3 antagonists containing indol-1-yl propionic acids.
Bioorg Med Chem Lett 15: 2679-84 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Identification of chemokine receptor CCR4 antagonist.
Bioorg Med Chem Lett 15: 2669-72 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of novel diphenacoum-derived, conformation-restricted vitamin K 2,3-epoxide reductase inhibitors.
Bioorg Med Chem Lett 15: 2665-8 (2005)
Tunghai University
Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity.
Bioorg Med Chem Lett 15: 2647-52 (2005)
Adolor
Geometry, topology, and atom-weights assembly descriptors to predicting A1 adenosine receptors agonists.
Bioorg Med Chem Lett 15: 2641-5 (2005)
Experimental Sugar Cane Station
5-Lipoxygenase inhibitors: convenient synthesis of 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues.
Bioorg Med Chem Lett 15: 2611-5 (2005)
Pfizer
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Bioorg Med Chem Lett 15: 2565-9 (2005)
Taisho Pharmaceutical
A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice.
Bioorg Med Chem Lett 15: 2541-6 (2005)
Neurocrine Biosciences
Design, new synthesis, and calcilytic activity of substituted 3H-pyrimidin-4-ones.
Bioorg Med Chem Lett 15: 2537-40 (2005)
Nps Pharmaceuticals
Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 15: 2533-6 (2005)
Merck Research Laboratories
4-Alkyl and 4,4'-dialkyl 1,2-bis(4-chlorophenyl)pyrazolidine-3,5-dione derivatives as new inhibitors of bacterial cell wall biosynthesis.
Bioorg Med Chem Lett 15: 2527-31 (2005)
Wyeth Research
Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists.
Bioorg Med Chem Lett 15: 2523-6 (2005)
Roche Palo Alto
Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers.
Bioorg Med Chem Lett 15: 2519-22 (2005)
Neurocrine Biosciences
Structure-based design of protein tyrosine phosphatase-1B inhibitors.
Bioorg Med Chem Lett 15: 2503-7 (2005)
Astrazeneca
Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid.
Bioorg Med Chem Lett 15: 2481-6 (2005)
Pfizer
Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers.
Bioorg Med Chem Lett 15: 2471-5 (2005)
University Of Arizona
6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides.
Bioorg Med Chem Lett 15: 2467-9 (2005)
University Of Catania
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.
Bioorg Med Chem Lett 15: 2461-5 (2005)
Acenta Discovery
1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors.
Bioorg Med Chem Lett 15: 2441-5 (2005)
Mitsubishi Pharma
Selective PPARgamma modulators with improved pharmacological profiles.
Bioorg Med Chem Lett 15: 2437-40 (2005)
Merck Research Laboratories
Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues.
J Med Chem 48: 3438-42 (2005)
The Danish University Of Pharmaceutical Sciences
Computational strategies in discovering novel non-nucleoside inhibitors of HIV-1 RT.
J Med Chem 48: 3433-7 (2005)
Universita Di Messina
1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors.
J Med Chem 48: 3428-32 (2005)
Sapienza University Of Rome
C-5-disubstituted barbiturates as potential molecular probes for noninvasive matrix metalloproteinase imaging.
J Med Chem 48: 3400-9 (2005)
University Hospital Of The Westf£Lische Wilhelms-Universit£T
Adenosine kinase inhibitors. 4. 6,8-Disubstituted purine nucleoside derivatives. Synthesis, conformation, and enzyme inhibition.
J Med Chem 48: 3389-99 (2005)
Metabasis Therapeutics
Design of benzophenone-containing photoactivatable linear vasopressin antagonists: pharmacological and photoreactive properties.
J Med Chem 48: 3379-88 (2005)
University Of Montpellier
Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.
J Med Chem 48: 3372-8 (2005)
Sapienza University Of Rome
Symmetrical bis-quinolinium compounds: new human choline kinase inhibitors with antiproliferative activity against the HT-29 cell line.
J Med Chem 48: 3354-63 (2005)
Universidad De Granada
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
J Med Chem 48: 3344-53 (2005)
Sapienza University Of Rome
Synthesis and pharmacology of 6-substituted benztropines: discovery of novel dopamine uptake inhibitors possessing low binding affinity to the dopamine transporter.
J Med Chem 48: 3337-43 (2005)
Universit£
N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.
J Med Chem 48: 3328-36 (2005)
University Of Florida
Structure-activity relationships of fluorinated lysophosphatidic acid analogues.
J Med Chem 48: 3319-27 (2005)
The University Of Utah
Conformation mining: an algorithm for finding biologically relevant conformations.
J Med Chem 48: 3313-8 (2005)
Rational Discovery
Structural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring functions.
J Med Chem 48: 3290-312 (2005)
Aventis Pharma Deutschland
Identification of novel low molecular weight CXCR4 antagonists by structural tuning of cyclic tetrapeptide scaffolds.
J Med Chem 48: 3280-9 (2005)
Kyoto University
Ligand-based prediction of active conformation by 3D-QSAR flexibility descriptors and their application in 3+3D-QSAR models.
J Med Chem 48: 3239-50 (2005)
University Of Szeged
Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 2. Identification of small-molecule inhibitors via coupling with virtual screening.
J Med Chem 48: 3221-30 (2005)
Protana
Successful in silico discovery of novel nonsteroidal ligands for human sex hormone binding globulin.
J Med Chem 48: 3203-13 (2005)
University Of British Columbia
Synthesis and antibacterial activity of 1-(2-fluorovinyl)-7-substituted-4-quinolone-3-carboxylic acid derivatives, conformationally restricted analogues of fleroxacin.
J Med Chem 48: 3194-202 (2005)
Kyorin Pharmaceutical
Enantiomerically pure hexahydropyrazinoquinolines as potent and selective dopamine 3 subtype receptor ligands.
J Med Chem 48: 3171-81 (2005)
University Of Michigan
Morphiceptin analogues containing a dipeptide mimetic structure: an investigation on the bioactive topology at the mu-receptor.
J Med Chem 48: 3153-63 (2005)
Università
Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.
J Med Chem 48: 3141-52 (2005)
The Institute For Diabetes Discovery
1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyanopyrazin-2-yl)ureas [correction of cyanopyrazi] as potent and selective inhibitors of Chk1 kinase: synthesis, preliminary SAR, and biological activities.
J Med Chem 48: 3118-21 (2005)
Abbott Laboratories
Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor.
J Med Chem 48: 3114-7 (2005)
Karo Bio
Toward a novel class of antithrombotic compounds with dual function. Discovery of 1,4-benzoxazin-3(4H)-one derivatives possessing thrombin inhibitory and fibrinogen receptor antagonistic activities.
J Med Chem 48: 3110-3 (2005)
University Of Ljubljana
Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.
J Med Chem 48: 3107-9 (2005)
Gsk
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
J Med Chem 48: 3103-6 (2005)
Fujisawa Pharmaceutical
Discovery of a beta-MSH-derived MC-4R selective agonist.
J Med Chem 48: 3095-8 (2005)
Eli Lilly
Pharmacodynamic characterization of ZP120 (Ac-RYYRWKKKKKKK-NH2), a novel, functionally selective nociceptin/orphanin FQ peptide receptor partial agonist with sodium-potassium-sparing aquaretic activity.
J Pharmacol Exp Ther 314: 652-60 (2005)
Louisiana State University
Chemistry and biology of dihydroisoxazole derivatives: selective inhibitors of human transglutaminase 2.
Chem Biol 12: 469-75 (2005)
Stanford University
Switching between allosteric and dimerization inhibition of HIV-1 protease.
Chem Biol 12: 439-44 (2005)
Purdue University
Novel behavior of O-methylated beta-cyclodextrins in inclusion of meso-tetraarylporphyrins.
J Org Chem 70: 3667-73 (2005)
Doshisha University
Structures and aldose reductase inhibitory effects of bromophenols from the red alga Symphyocladia latiuscula.
J Nat Prod 68: 620-2 (2005)
Jilin Province Academy Of Traditional Chinese Medicine And Materia Medica
Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand.
J Nat Prod 68: 617-9 (2005)
Merck Research Laboratories
Tenellones A and B from a Diaporthe sp.: two highly substituted benzophenone inhibitors of parasite cGMP-dependent protein kinase activity.
J Nat Prod 68: 611-3 (2005)
Merck Research Laboratories
The psammaplysenes, specific inhibitors of FOXO1a nuclear export.
J Nat Prod 68: 574-6 (2005)
Harvard Medical School
Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata.
J Nat Prod 68: 572-3 (2005)
Mitsubishi Pharma
QSAR for phospholipase A2 inhibitions by 1-acyloxy-3-N-n-octylcarbamyl-benzenes.
Bioorg Med Chem Lett 15: 2405-8 (2005)
National Chung-Hsing University
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.
Bioorg Med Chem Lett 15: 2399-403 (2005)
Procter And Gamble Pharmaceuticals
2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.
Bioorg Med Chem Lett 15: 2385-8 (2005)
Merck Research Laboratories
New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors.
Bioorg Med Chem Lett 15: 2381-4 (2005)
RhôNe-Poulenc Rorer
Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors.
Bioorg Med Chem Lett 15: 2371-4 (2005)
Pfizer
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
Bioorg Med Chem Lett 15: 2365-9 (2005)
Schering-Plough Research Institute
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating thioureido-sulfanilyl scaffolds.
Bioorg Med Chem Lett 15: 2359-64 (2005)
Ospedale San Lazzaro
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with N-hydroxysulfamides--a new zinc-binding function in the design of inhibitors.
Bioorg Med Chem Lett 15: 2353-8 (2005)
Universit£
Carbonic anhydrase inhibitors. Inhibition of the cytosolic and tumor-associated carbonic anhydrase isozymes I, II, and IX with a series of 1,3,4-thiadiazole- and 1,2,4-triazole-thiols.
Bioorg Med Chem Lett 15: 2347-52 (2005)
University Of Bucharest
Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies.
Bioorg Med Chem Lett 15: 2315-20 (2005)
University Of Naples Federico Ii
A new development of matrix metalloproteinase inhibitors: twin hydroxamic acids as potent inhibitors of MMPs.
Bioorg Med Chem Lett 15: 2311-4 (2005)
Università
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase.
Bioorg Med Chem Lett 15: 2305-9 (2005)
Gsk
Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor.
Bioorg Med Chem Lett 15: 2295-9 (2005)
Celltech R&D
Oximinoarylsulfonamides as potent HIV protease inhibitors.
Bioorg Med Chem Lett 15: 2275-8 (2005)
Abbott Laboratories
Benzimidazoles as non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 3: Discovery of 1-(1H-benzimidazol-5-yl)-3-tert-butylurea derivatives.
Bioorg Med Chem Lett 15: 2265-9 (2005)
Kyoto 619-0216
Novel approach to pro-drugs of lactones: water soluble imidate and ortho-ester derivatives of a furanone-based COX-2 selective inhibitor.
Bioorg Med Chem Lett 15: 2259-63 (2005)
Merck Research Laboratories
Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole.
Bioorg Med Chem Lett 15: 2253-8 (2005)
Merck Research Laboratories
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.
Bioorg Med Chem Lett 15: 2249-52 (2005)
Berlex Biosciences
Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.
Bioorg Med Chem Lett 15: 2235-8 (2005)
Kudos Horsham
NMDA-NR2B subtype selectivity of stereoisomeric 2-(1,2,3,4-tetrahydro-1-isoquinolyl)ethanol derivatives.
Bioorg Med Chem Lett 15: 2231-4 (2005)
Ludwig-Maximilians-UniversitäT MüNchen
Novel 2-amino-4-oxo-5-arylthio-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase.
Bioorg Med Chem Lett 15: 2225-30 (2005)
Duquesne University
3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.
Bioorg Med Chem Lett 15: 2221-4 (2005)
Johnson & Johnson Pharmaceutical
Studies on the reactivity of CDDO, a promising new chemopreventive and chemotherapeutic agent: implications for a molecular mechanism of action.
Bioorg Med Chem Lett 15: 2215-9 (2005)
Dartmouth College
A structural screening approach to ketoamide-based inhibitors of cathepsin K.
Bioorg Med Chem Lett 15: 2209-13 (2005)
Glaxosmithkline
Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors.
Bioorg Med Chem Lett 15: 2203-7 (2005)
Glaxosmithkline
Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.
J Pharmacol Exp Ther 314: 77-85 (2005)
Taisho Pharmaceutical
Synthesis and anticancer activity of new pyrrolocarbazoles and pyrrolo-beta-carbolines.
Bioorg Med Chem 13: 2263-83 (2005)
Cnrs
Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition.
J Med Chem 48: 3080-4 (2005)
Nerviano Medical Sciences
Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.
J Med Chem 48: 3076-9 (2005)
Lundbeck Research Usa
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.
J Med Chem 48: 3060-75 (2005)
University Of Florida
Applying linear interaction energy method for rational design of noncompetitive allosteric inhibitors of the sarco- and endoplasmic reticulum calcium-ATPase.
J Med Chem 48: 3005-14 (2005)
Johns Hopkins University
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
J Med Chem 48: 2972-84 (2005)
University Of Maryland
Dimeric zanamivir conjugates with various linking groups are potent, long-lasting inhibitors of influenza neuraminidase including H5N1 avian influenza.
J Med Chem 48: 2964-71 (2005)
Glaxosmithkline
Pyridinium-1-yl bisphosphonates are potent inhibitors of farnesyl diphosphate synthase and bone resorption.
J Med Chem 48: 2957-63 (2005)
University Of Illinois At Urbana-Champaign
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.
J Med Chem 48: 2944-56 (2005)
Nerviano Medical Sciences
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.
J Med Chem 48: 2936-43 (2005)
Università
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.
J Med Chem 48: 2906-15 (2005)
University Of Mississippi
Evaluation of 8-arylsulfanyl, 8-arylsulfoxyl, and 8-arylsulfonyl adenine derivatives as inhibitors of the heat shock protein 90.
J Med Chem 48: 2892-905 (2005)
Memorial Sloan-Kettering Cancer Center
(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1.
J Med Chem 48: 2882-91 (2005)
Korea Research Institute Of Chemical Technology
Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol.
J Med Chem 48: 2876-81 (2005)
Medical University Of South Carolina
Design, synthesis, and antiviral activity of adenosine 5'-phosphonate analogues as chain terminators against hepatitis C virus.
J Med Chem 48: 2867-75 (2005)
Valeant Pharmaceuticals International
N-terminal sugar conjugation and C-terminal Thr-for-Thr(ol) exchange in radioiodinated Tyr3-octreotide: effect on cellular ligand trafficking in vitro and tumor accumulation in vivo.
J Med Chem 48: 2778-89 (2005)
Technische Universit£T M£Nchen
Novel and potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors.
J Med Chem 48: 2759-62 (2005)
University Of Bath
Terephthalamide derivatives as mimetics of helical peptides: disruption of the Bcl-x(L)/Bak interaction.
J Am Chem Soc 127: 5463-8 (2005)
Yale University
Synthesis and evaluation of potential inhibitors of eIF4E cap binding to 7-methyl GTP.
Bioorg Med Chem Lett 15: 2177-80 (2005)
University Of Minnesota
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
Bioorg Med Chem Lett 15: 2163-7 (2005)
Merck Research Laboratories
The role of QSAR in dopamine interactions.
Bioorg Med Chem Lett 15: 2149-57 (2005)
Pomona College
Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.
Bioorg Med Chem Lett 15: 2129-34 (2005)
Merck Research Laboratories
6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists.
Bioorg Med Chem Lett 15: 2119-22 (2005)
Schering-Plough Research Institute
Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.
Bioorg Med Chem Lett 15: 2107-10 (2005)
Rensselaer Polytechnic Institute
Discovery, synthesis and biological evaluation of novel glucokinase activators.
Bioorg Med Chem Lett 15: 2103-6 (2005)
Astrazeneca
QSAR analyses of conformationally restricted 1,5-diaryl pyrazoles as selective COX-2 inhibitors: application of connection table representation of ligands.
Bioorg Med Chem Lett 15: 2097-102 (2005)
Devi Ahilya Vishwavidyalaya
Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine.
Bioorg Med Chem Lett 15: 2093-6 (2005)
Ranbaxy Research Laboratories
Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport.
Bioorg Med Chem Lett 15: 2087-91 (2005)
Genzyme
2-(Arylmethyl)-3-substituted quinuclidines as selective alpha 7 nicotinic receptor ligands.
Bioorg Med Chem Lett 15: 2073-7 (2005)
Targacept
Inhibitory activities against topoisomerase I and II by isoaurostatin derivatives and their structure-activity relationships.
Bioorg Med Chem Lett 15: 2065-8 (2005)
Kumamoto University
A general carbometalation, three component coupling strategy for the synthesis of alpha,beta-unsaturated gamma-sultines including thio-rofecoxib, a selective COX-2 inhibitor.
Bioorg Med Chem Lett 15: 2057-60 (2005)
Methylgene
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
Bioorg Med Chem Lett 15: 2041-5 (2005)
Merck Research Laboratories
Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.
Bioorg Med Chem Lett 15: 2033-9 (2005)
Abbott Laboratories
Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase.
Bioorg Med Chem Lett 15: 1997-2001 (2005)
Merck Research Laboratories
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
Bioorg Med Chem Lett 15: 1993-6 (2005)
Merck Research Laboratories
Binding of isotryptamines and indenes at h5-HT6 serotonin receptors.
Bioorg Med Chem Lett 15: 1987-91 (2005)
Virginia Commonwealth University
Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors.
Bioorg Med Chem Lett 15: 1973-7 (2005)
Bayer Research Center
Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors.
Bioorg Med Chem Lett 15: 1969-72 (2005)
Miikana Therapeutics
Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase.
J Med Chem 48: 2695-700 (2005)
Biota
Anchor-GRIND: filling the gap between standard 3D QSAR and the GRid-INdependent descriptors.
J Med Chem 48: 2687-94 (2005)
Imim/Universitat Pompeu Fabra
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
J Med Chem 48: 2678-86 (2005)
Mitsubishi Pharma
Preparation and pharmacological characterization of trans-2-amino-5(6)-fluoro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as D2-like dopamine receptor agonists.
J Med Chem 48: 2646-54 (2005)
Universit£
Synthesis, structure-activity relationships at the GABA(A) receptor in rat brain, and differential electrophysiological profile at the recombinant human GABA(A) receptor of a series of substituted 1,2-diphenylimidazoles.
J Med Chem 48: 2638-45 (2005)
Universit£
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
J Med Chem 48: 2627-37 (2005)
University Walk
Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents.
J Med Chem 48: 2559-70 (2005)
Columbia University College Of Physicians And Surgeons
Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors.
J Med Chem 48: 2548-2558 (2005)
TBA
Virtual screening workflow development guided by the"receiver operating characteristic" curve approach. Application to high-throughput docking on metabotropic glutamate receptor subtype 4.
J Med Chem 48: 2534-47 (2005)
Universit£
Substituted 5,5'-diphenyl-2-thioxoimidazolidin-4-one as CB1 cannabinoid receptor ligands: synthesis and pharmacological evaluation.
J Med Chem 48: 2509-17 (2005)
Université
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.
J Med Chem 48: 2493-508 (2005)
Friedrich-Alexander University
Architecture of the human urotensin II receptor: comparison of the binding domains of peptide and non-peptide urotensin II agonists.
J Med Chem 48: 2480-92 (2005)
Università
Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach.
J Med Chem 48: 2469-79 (2005)
Molecular Discovery
LEA3D: a computer-aided ligand design for structure-based drug design.
J Med Chem 48: 2457-68 (2005)
University Of Montpellier
Synthesis of 3-arylpiperazinylalkylpyrrolo[3,2-d]pyrimidine-2,4-dione derivatives as novel, potent, and selective alpha1-adrenoceptor ligands.
J Med Chem 48: 2420-31 (2005)
Università
Sulfur-substituted alpha-alkyl phenethylamines as selective and reversible MAO-A inhibitors: biological activities, CoMFA analysis, and active site modeling.
J Med Chem 48: 2407-19 (2005)
Universidad De Chile
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.
J Med Chem 48: 2388-406 (2005)
Pfizer
Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.
J Med Chem 48: 2371-87 (2005)
Pfizer
Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex.
J Med Chem 48: 2336-45 (2005)
Decode Biostructures
Enantiospecificity of glutamate carboxypeptidase II inhibition.
J Med Chem 48: 2319-24 (2005)
Guilford Pharmaceuticals
9-hydroxyazafluorenes and their use in thrombin inhibitors.
J Med Chem 48: 2282-93 (2005)
Merck Research Laboratories
Virtual docking approaches to protein kinase B inhibition.
J Med Chem 48: 2278-81 (2005)
The Burnham Institute
Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics.
J Med Chem 48: 2274-7 (2005)
Schering-Plough Research Institute
Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy.
J Med Chem 48: 2270-3 (2005)
Eli Lilly
3-Substituted imidazo[1,2-d][1,2,4]-thiadiazoles: a novel class of factor XIIIa inhibitors.
J Med Chem 48: 2266-9 (2005)
Apotex Research
Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.
J Med Chem 48: 2262-5 (2005)
Merck Research Laboratories
Discovery of a fluoroindolo[2,3-a]carbazole clinical candidate with broad spectrum antitumor activity in preclinical tumor models superior to the marketed oncology drug, CPT-11.
J Med Chem 48: 2258-61 (2005)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2.
J Pharmacol Exp Ther 314: 244-51 (2005)
Kyowa Hakko Kogyo
High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.
J Biol Chem 280: 21847-53 (2005)
University Of Texas Southwestern Medical Center
Sesquiterpenoids and plasmin-inhibitory flavonoids from Blumea balsamifera.
J Nat Prod 68: 447-9 (2005)
Chiba University
Terphenylquinone inhibitors of the src protein tyrosine kinase from Stilbella sp.
J Nat Prod 68: 323-6 (2005)
Boehringer Ingelheim Pharma
Hepatic glucocorticoid receptor antagonism is sufficient to reduce elevated hepatic glucose output and improve glucose control in animal models of type 2 diabetes.
J Pharmacol Exp Ther 314: 191-200 (2005)
Abbott Laboratories
UDP-glucuronosyltransferases and clinical drug-drug interactions.
Pharmacol Ther 106: 97-132 (2005)
The University Of British Columbia
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.
Bioorg Med Chem Lett 15: 1943-7 (2005)
Eli Lilly
Carbonic anhydrase inhibitors: X-ray crystal structure of a benzenesulfonamide strong CA II and CA IX inhibitor bearing a pentafluorophenylaminothioureido tail in complex with isozyme II.
Bioorg Med Chem Lett 15: 1937-42 (2005)
University Of Naples 'Federico Ii
Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1.
Bioorg Med Chem Lett 15: 1931-5 (2005)
University Of Auckland
Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V and IX with complex fluorides, chlorides and cyanides.
Bioorg Med Chem Lett 15: 1909-13 (2005)
Università
Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain.
Bioorg Med Chem Lett 15: 1901-7 (2005)
Merck Research Laboratories
Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.
Bioorg Med Chem Lett 15: 1895-9 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Molecular-modeling based design, synthesis, and activity of substituted piperidines as gamma-secretase inhibitors.
Bioorg Med Chem Lett 15: 1891-4 (2005)
Wyeth Research
Structure-activity relationship study of novel tissue transglutaminase inhibitors.
Bioorg Med Chem Lett 15: 1885-9 (2005)
Harvard Medical School
Synthesis of 15R-PGD2: a potential DP2 receptor agonist.
Bioorg Med Chem Lett 15: 1873-6 (2005)
Florida Institute Of Technology
Structure-based design of derivatives of tyropeptin A as the potent and selective inhibitors of mammalian 20S proteasome.
Bioorg Med Chem Lett 15: 1867-71 (2005)
Numazu Bio-Medical Research Institute
Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists.
Bioorg Med Chem Lett 15: 1857-61 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.
Bioorg Med Chem Lett 15: 1847-50 (2005)
Lanzhou University
1,3-Dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines as potent caspase-3 inhibitors.
Bioorg Med Chem Lett 15: 1841-5 (2005)
Chemical Diversity Research Institute
Novel heterocyclic thyromimetics.
Bioorg Med Chem Lett 15: 1835-40 (2005)
Bayer Healthcare
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.
Bioorg Med Chem Lett 15: 1829-33 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel and potent cyclic cyanamide-based cathepsin K inhibitors.
Bioorg Med Chem Lett 15: 1815-9 (2005)
Glaxosmithkline
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.
Bioorg Med Chem Lett 15: 1807-10 (2005)
Pfizer
Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues.
Bioorg Med Chem Lett 15: 1799-802 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents.
Bioorg Med Chem Lett 15: 1793-7 (2005)
National Institute Of Pharmaceutical Education And Research (Niper)
Structure-activity relationships of the oxindole growth hormone secretagogues.
Bioorg Med Chem Lett 15: 1789-92 (2005)
Sumitomo Pharmaceuticals
QSAR-by-NMR: quantitative insights into structural determinants for binding affinity by analysis of 1H/15N chemical shift differences in MMP-3 ligands.
Bioorg Med Chem Lett 15: 1779-83 (2005)
Aventis Pharma Deutschland
18F-labeled sufentanil for PET-imaging of mu-opioid receptors.
Bioorg Med Chem Lett 15: 1773-7 (2005)
Technische Universit£T M£Nchen
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
J Biol Chem 280: 19867-74 (2005)
Berlex Biosciences
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.
J Med Chem 48: 2248-50 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.
J Med Chem 48: 2243-7 (2005)
Glaxosmithkline Research & Development
Development of low molecular weight HIV-1 protease dimerization inhibitors.
J Med Chem 48: 2239-42 (2005)
Purdue University
4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists.
J Med Chem 48: 2229-38 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.
J Med Chem 48: 2194-211 (2005)
Pharmaceutical Research Institute
Norpiperidine imidazoazepines as a new class of potent, selective, and nonsedative H1 antihistamines.
J Med Chem 48: 2154-66 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.
J Med Chem 48: 2134-53 (2005)
Janssen-Cilag
Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
J Med Chem 48: 2126-33 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties.
J Med Chem 48: 2121-5 (2005)
Universita Degli Studi Di Firenze
Development of spin-labeled probes for adenosine receptors.
J Med Chem 48: 2108-14 (2005)
University Of Bonn
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.
J Med Chem 48: 2100-7 (2005)
Vrije Universiteit Amsterdam
Synthesis of new benzoxazinone derivatives as neuropeptide Y5 antagonists for the treatment of obesity.
J Med Chem 48: 2080-92 (2005)
Laboratorios Dr. Esteve
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
J Med Chem 48: 2054-71 (2005)
Janssen-Cilag
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
J Med Chem 48: 2045-53 (2005)
Leiden/Amsterdam Center For Drug Research
Biological properties of D- and L-1-deoxyazasugars.
J Med Chem 48: 2036-44 (2005)
Toyama Medical And Pharmaceutical University
Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.
J Med Chem 48: 2026-35 (2005)
University Of Ferrara
Novel diamino derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
J Med Chem 48: 2009-18 (2005)
Biogen Idec
In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.
J Med Chem 48: 1984-2008 (2005)
Johnson & Johnson Pharmaceutical
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
J Med Chem 48: 1965-73 (2005)
Tibotec
Comparison of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II by using topiramate as a structural platform.
J Med Chem 48: 1941-7 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Design and optimization of tricyclic phtalimide analogues as novel inhibitors of HIV-1 integrase.
J Med Chem 48: 1930-40 (2005)
Tibotec
Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors.
J Med Chem 48: 1919-29 (2005)
Universita Di Siena
Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.
J Med Chem 48: 1886-900 (2005)
Johnson & Johnson Pharmaceutical
Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles.
J Med Chem 48: 1873-85 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.
J Med Chem 48: 1857-72 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.
J Med Chem 48: 1849-56 (2005)
The Scripps Research Institute
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
J Med Chem 48: 1839-48 (2005)
University Of Arizona
Bioisosteric replacements of the pyrazole moiety of rimonabant: synthesis, biological properties, and molecular modeling investigations of thiazoles, triazoles, and imidazoles as potent and selective CB1 cannabinoid receptor antagonists.
J Med Chem 48: 1823-38 (2005)
Solvay Pharma
Nanomolar inhibitors of CNS epinephrine biosynthesis: (R)-(+)-3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines as potent and highly selective inhibitors of phenylethanolamine N-methyltransferase1.
J Med Chem 48: 1806-12 (2005)
University Of Kansas
Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.
J Med Chem 48: 1796-805 (2005)
Saarland University
Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands.
J Med Chem 48: 1781-95 (2005)
Laboratorios Dr. Esteve
Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.
J Med Chem 48: 1768-80 (2005)
University Of Antwerp
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
J Med Chem 48: 1745-58 (2005)
National Institute Of Diabetes And Digestive And Kidney Diseases
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
J Med Chem 48: 1729-44 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.
J Med Chem 48: 1725-8 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.
J Med Chem 48: 1721-4 (2005)
University Of Illinois At Chicago
2-Hydroxy-4,6-diamino-[1,3,5]triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors.
J Med Chem 48: 1717-20 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
J Med Chem 48: 1709-12 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.
J Med Chem 48: 1705-8 (2005)
Università
Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.
J Med Chem 48: 1701-4 (2005)
Universitat De Barcelona
Identification of substituted 6-amino-4-phenyltetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptor.
J Med Chem 48: 1697-700 (2005)
Research And Development
Desensitization of the human motilin receptor by motilides.
J Pharmacol Exp Ther 313: 1397-405 (2005)
Katholieke Universiteit Leuven
Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase.
Bioorg Med Chem 13: 2665-78 (2005)
Biocryst Pharmaceuticals
Discovery of novel non-peptidic ketopiperazine-based renin inhibitors.
Bioorg Med Chem 13: 2657-64 (2005)
Pfizer
Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.
Bioorg Med Chem Lett 15: 1749-53 (2005)
Athersys
Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor.
Bioorg Med Chem Lett 15: 1743-7 (2005)
Wyeth-Ayerst Research
A two-state homology model of the hERG K+ channel: application to ligand binding.
Bioorg Med Chem Lett 15: 1737-41 (2005)
Johnson & Johnson Pharmaceutical Research & Development
Novel beta-(imidazol-4-yl)-beta-amino acids: solid-phase synthesis and study of their inhibitory activity against geranylgeranyl protein transferase type I.
Bioorg Med Chem Lett 15: 1713-9 (2005)
Janssen Research Foundation
1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands.
Bioorg Med Chem Lett 15: 1707-11 (2005)
Virginia Commonwealth University
Design, synthesis and structure-activity relationship studies of hexahydropyrazinoquinolines as a novel class of potent and selective dopamine receptor 3 (D3) ligands.
Bioorg Med Chem Lett 15: 1701-5 (2005)
University Of Michigan
Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification.
Bioorg Med Chem Lett 15: 1697-700 (2005)
Roche Palo Alto
Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors.
Bioorg Med Chem Lett 15: 1687-91 (2005)
Johnson And Johnson Pharmaceutical Research And Development
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates.
Bioorg Med Chem Lett 15: 1683-6 (2005)
University Of Montpellier
Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs.
Bioorg Med Chem Lett 15: 1675-81 (2005)
Merck Research Laboratories
Potent and selective [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines as retinoic acid metabolic blocking agents (RAMBAs).
Bioorg Med Chem Lett 15: 1669-73 (2005)
Osi Pharmaceuticals
Combinatorial approaches towards the discovery of new tryptase inhibitors.
Bioorg Med Chem Lett 15: 1659-64 (2005)
University Of Barcelona
Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics.
Bioorg Med Chem Lett 15: 1647-50 (2005)
Merck Research Laboratories
Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors.
Bioorg Med Chem Lett 15: 1641-5 (2005)
Wyeth Research
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Bioorg Med Chem Lett 15: 1623-7 (2005)
Amgen
Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs).
Bioorg Med Chem Lett 15: 1619-21 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel and potent NPY5 receptor antagonists derived from virtual screening and iterative parallel chemistry design.
Bioorg Med Chem Lett 15: 1599-603 (2005)
F. Hoffmann-La Roche
Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Bioorg Med Chem Lett 15: 1587-90 (2005)
Pfizer
Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.
Bioorg Med Chem Lett 15: 1583-6 (2005)
Human Biomolecular Research Institute
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines.
Bioorg Med Chem Lett 15: 1577-82 (2005)
Abbott Laboratories
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators.
Bioorg Med Chem Lett 15: 1565-71 (2005)
Merck Research Laboratories
3H-Quinazolin-4-ones as a new calcilytic template for the potential treatment of osteoporosis.
Bioorg Med Chem Lett 15: 1557-60 (2005)
Nps Pharmaceuticals
Identification of small molecule inhibitors of the hepatitis C virus RNA-dependent RNA polymerase from a pyrrolidine combinatorial mixture.
Bioorg Med Chem Lett 15: 1553-6 (2005)
Glaxosmithkline
Functional selectivity of melanocortin 4 receptor peptide and nonpeptide agonists: evidence for ligand-specific conformational states.
J Pharmacol Exp Ther 313: 1281-8 (2005)
Neurocrine Biosciences
Endocrinological properties of two novel nonsteroidal progesterone receptor modulators, CP8816 and CP8863.
J Pharmacol Exp Ther 313: 916-20 (2005)
Meiji Seika Kaisha
Identification of small molecule chemical inhibitors of the collagen-specific chaperone Hsp47.
J Med Chem 48: 1680-4 (2005)
Mcmaster University
Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.
J Med Chem 48: 1676-9 (2005)
University Of Bath
Discovery of a novel class of reversible non-peptide caspase inhibitors via a structure-based approach.
J Med Chem 48: 1649-56 (2005)
Burnham Institute
3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.
J Med Chem 48: 1620-9 (2005)
University Of Medicine & Dentistry Of New Jersey-Robert Wood Johnson Medical School (Umdnj-Rwjms)
Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
J Med Chem 48: 1610-9 (2005)
Glaxosmithkline
Structure-based design, synthesis, and study of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III as potential antimicrobial agents.
J Med Chem 48: 1596-609 (2005)
Quorex Pharmaceuticals
Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
J Med Chem 48: 1563-75 (2005)
Saarland University
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.
J Med Chem 48: 1550-62 (2005)
Universit£
Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists.
J Med Chem 48: 1540-9 (2005)
Neurocrine Biosciences
Design and biological evaluation of linear and cyclic phosphopeptide ligands of the N-terminal SH2 domain of protein tyrosine phosphatase SHP-1.
J Med Chem 48: 1528-39 (2005)
Friedrich-Schiller-University
Novel ligands for the chemokine receptor-3 (CCR3): a receptor-modeling study based on 5D-QSAR.
J Med Chem 48: 1515-27 (2005)
Biographics Laboratory 3R
NMR studies reveal structural differences between the gallium and yttrium complexes of DOTA-D-Phe1-Tyr3-octreotide.
J Med Chem 48: 1506-14 (2005)
Technische Universit£T M£Nchen
Dynamic receptor-based pharmacophore model development and its application in designing novel HIV-1 integrase inhibitors.
J Med Chem 48: 1496-505 (2005)
University Of Houston
A shape-based 3-D scaffold hopping method and its application to a bacterial protein-protein interaction.
J Med Chem 48: 1489-95 (2005)
Wyeth Research
CoMFA and CoMSIA analyses of Pneumocystis carinii dihydrofolate reductase, Toxoplasma gondii dihydrofolate reductase, and rat liver dihydrofolate reductase.
J Med Chem 48: 1448-69 (2005)
Duquesne University
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
J Med Chem 48: 1421-7 (2005)
University Of Ferrara
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.
J Med Chem 48: 1367-83 (2005)
Merck Sharp & Dohme Research Laboratories
Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.
J Med Chem 48: 1359-66 (2005)
Kirin Brewery
Synthesis and biological evaluation of meperidine analogues at monoamine transporters.
J Med Chem 48: 1336-43 (2005)
University Of New Orleans
Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity.
J Med Chem 48: 1318-21 (2005)
Abbott Laboratories
Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase.
J Med Chem 48: 1314-7 (2005)
Irbm (Merck Research Laboratories Rome)
New approaches toward anti-HIV chemotherapy.
J Med Chem 48: 1297-313 (2005)
Katholieke Universiteit Leuven
From the insoluble dye indirubin towards highly active, soluble CDK2-inhibitors.
Chembiochem 6: 531-40 (2005)
Schering
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.
Chem Biol 12: 237-47 (2005)
National Institutes Of Health
Structural basis for the highly selective inhibition of MMP-13.
Chem Biol 12: 181-9 (2005)
Aventis Pharma Deutschland
Bioactive constituents from Boswellia papyrifera.
J Nat Prod 68: 189-93 (2005)
University Of Karachi
Development of a technique to determine bicyclomycin-rho binding and stoichiometry by isothermal titration calorimetry and mass spectrometry.
J Am Chem Soc 127: 2741-51 (2005)
University Of North Carolina
Use of binding enthalpy to drive an allosteric transition.
Biochemistry 44: 3112-21 (2005)
University Of Maryland
CH...O and CH...N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor.
J Med Chem 48: 1278-81 (2005)
Vertex Pharmaceuticals
Amino acid ester prodrugs of the antiviral agent 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole as potential substrates of hPEPT1 transporter.
J Med Chem 48: 1274-7 (2005)
University Of Michigan
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyladenine: highly potent and selective PDE4 inhibitors.
J Med Chem 48: 1237-43 (2005)
Purdue Pharma
Chiral DNA gyrase inhibitors. 3. Probing the chiral preference of the active site of DNA gyrase. Synthesis of 10-fluoro-6-methyl-6,7-dihydro-9-piperazinyl- 2H-benzo[a]quinolizin-20-one-3-carboxylic acid analogues.
J Med Chem 48: 1229-36 (2005)
University Of Kansas
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists.
J Med Chem 48: 1221-8 (2005)
Research Triangle Institute
3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.
J Med Chem 48: 1169-78 (2005)
Neurocrine Biosciences
Synthesis and biological evaluation of a new series of 2,3,5-substituted [1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action.
J Med Chem 48: 1145-51 (2005)
Leiden/Amsterdam Center For Drug Research
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.
J Med Chem 48: 1107-31 (2005)
Wyeth Research
Synthesis and biological evaluation of dimeric RGD peptide-paclitaxel conjugate as a model for integrin-targeted drug delivery.
J Med Chem 48: 1098-106 (2005)
University Of Southern California
Structure-based drug discovery using GPCR homology modeling: successful virtual screening for antagonists of the alpha1A adrenergic receptor.
J Med Chem 48: 1088-97 (2005)
Aventis Pharma Deutschland
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.
J Med Chem 48: 1019-32 (2005)
Nagoya City University
Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.
J Med Chem 48: 986-94 (2005)
National Institute On Aging
Application of a flexible synthesis of (5R)-thiolactomycin to develop new inhibitors of type I fatty acid synthase.
J Med Chem 48: 946-61 (2005)
Johns Hopkins University
Design, synthesis, and biological evaluation of novel potent and selective alphavbeta3/alphavbeta5 integrin dual inhibitors with improved bioavailability. Selection of the molecular core.
J Med Chem 48: 926-34 (2005)
Johnson And Johnson Pharmaceutical Research & Development
Three-dimensional structure-activity relationships of nonsteroidal ligands in complex with androgen receptor ligand-binding domain.
J Med Chem 48: 917-25 (2005)
Csc-Scientific Computing
Improving specificity vs bacterial thymidylate synthases through N-dansyl modulation of didansyltyrosine.
J Med Chem 48: 913-6 (2005)
Università
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.
J Med Chem 48: 909-12 (2005)
Johnson & Johnson Pharmaceutical
Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors.
J Med Chem 48: 905-8 (2005)
Pfizer
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
J Med Chem 48: 897-900 (2005)
7Tm Pharma
(E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors.
Bioorg Med Chem Lett 15: 1525-7 (2005)
National Research Laboratory Of Lipid Metabolism And Atherosclerosis
Lysine derivatives as potent HIV protease inhibitors. Discovery, synthesis and structure-activity relationship studies.
Bioorg Med Chem Lett 15: 1509-13 (2005)
Pharmacor
Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo.
Bioorg Med Chem Lett 15: 1505-7 (2005)
Chinese Academy Of Sciences
Glucokinase-activating ureas.
Bioorg Med Chem Lett 15: 1501-4 (2005)
Osi Pharmaceuticals
Structure-activity relationships of dimeric PPAR agonists.
Bioorg Med Chem Lett 15: 1497-500 (2005)
Novo Nordisk
Aglycon specificity profiling of alpha-glucosidases using synthetic probes.
Bioorg Med Chem Lett 15: 1489-92 (2005)
Institute Of Physical And Chemical Research (Riken)
Crystal structures of human HSP90alpha-complexed with dihydroxyphenylpyrazoles.
Bioorg Med Chem Lett 15: 1475-8 (2005)
Genomics Institute Of The Novartis Research Foundation
Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity.
Bioorg Med Chem Lett 15: 1467-70 (2005)
Arena Pharmaceuticals
Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor alpha/beta agonist scaffold.
Bioorg Med Chem Lett 15: 1463-6 (2005)
Ligand Pharmaceuticals
Synthesis and evaluation of azalanstat analogues as heme oxygenase inhibitors.
Bioorg Med Chem Lett 15: 1457-61 (2005)
Queen'S University
Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.
Bioorg Med Chem Lett 15: 1441-6 (2005)
Merck Research Laboratories
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.
Bioorg Med Chem Lett 15: 1435-40 (2005)
Bristol-Myers Squibb
Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.
Bioorg Med Chem Lett 15: 1429-33 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity.
Bioorg Med Chem Lett 15: 1423-8 (2005)
The Scripps Research Institute
Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists.
Bioorg Med Chem Lett 15: 1407-11 (2005)
Neurocrine Biosciences
Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
Bioorg Med Chem Lett 15: 1401-5 (2005)
Merck Research Laboratories
Utilization of a nitrobenzoxadiazole (NBD) fluorophore in the design of a Grb2 SH2 domain-binding peptide mimetic.
Bioorg Med Chem Lett 15: 1385-8 (2005)
Nih
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P2 alpha-amino acid by a alpha-hydroxy acid.
Bioorg Med Chem Lett 15: 1379-83 (2005)
Maxim Pharmaceuticals
The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists.
Bioorg Med Chem Lett 15: 1375-8 (2005)
Schering-Plough Research Institute
Novel and orally bioavailable inducible nitric oxide synthase inhibitors: synthesis and evaluation of optically active 4,5-dialkyl-2-iminoselenazolidine derivatives.
Bioorg Med Chem Lett 15: 1361-6 (2005)
Dainippon Pharmaceutical
(R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents.
Bioorg Med Chem Lett 15: 1345-9 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors.
Bioorg Med Chem Lett 15: 1337-40 (2005)
Korea Research Institute Of Chemical Technology
cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition.
Bioorg Med Chem Lett 15: 1327-31 (2005)
Amura Therapeutics
N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.
Bioorg Med Chem Lett 15: 1321-6 (2005)
Universit£
Benzodipyrazoles: a new class of potent CDK2 inhibitors.
Bioorg Med Chem Lett 15: 1315-9 (2005)
Nerviano Medical Sciences
Amino acid conjugates as kappa opioid receptor agonists.
Bioorg Med Chem Lett 15: 1279-82 (2005)
Adolor
A small molecule-kinase interaction map for clinical kinase inhibitors.
Nat Biotechnol 23: 329-36 (2005)
Ambit Biosciences
Demonstration of isoleucine 199 as a structural determinant for the selective inhibition of human monoamine oxidase B by specific reversible inhibitors.
J Biol Chem 280: 15761-6 (2005)
Emory University
Structure-aided optimization of kinase inhibitors derived from alsterpaullone.
Chembiochem 6: 541-9 (2005)
Technische UniversitÄT Braunschweig
Inhibition of angiogenesis-relevant receptor tyrosine kinases by sulindac analogues.
Chembiochem 6: 527-31 (2005)
Max-Planck-Institut FÜR Molekulare Physiologie
Carbocyclic[g]indole inhibitors of human nonpancreatic s-PLA2.
J Med Chem 48: 893-6 (2005)
Eli Lilly
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
J Med Chem 48: 849-56 (2005)
Unibioscreen
Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.
J Med Chem 48: 839-48 (2005)
National Institute On Drug Abuse-Intramural Research Program
Design and synthesis of conformationally constrained Grb2 SH2 domain binding peptides employing alpha-methylphenylalanyl based phosphotyrosyl mimetics.
J Med Chem 48: 764-72 (2005)
National Cancer Institute-Frederick
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
J Med Chem 48: 744-52 (2005)
Abbott Laboratories
Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin.
J Med Chem 48: 737-43 (2005)
Lawrence Berkeley National Laboratory
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
J Med Chem 48: 694-709 (2005)
Friedrich-Alexander University
Mechanism of CDK5/p25 binding by CDK inhibitors.
J Med Chem 48: 671-9 (2005)
European Institute Of Oncology
Alkylamino derivatives of 4-aminomethylpyridine as inhibitors of copper-containing amine oxidases.
J Med Chem 48: 664-70 (2005)
Universit£
Structure of human cytidine deaminase bound to a potent inhibitor.
J Med Chem 48: 658-60 (2005)
Harvard University
Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.
J Med Chem 48: 655-7 (2005)
Shanghai Institute Of Materia Medica
N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase.
Bioorg Med Chem Lett 15: 1235-8 (2005)
Novartis Institutes For Biomedical Research
Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists.
Bioorg Med Chem Lett 15: 1225-8 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors.
Bioorg Med Chem Lett 15: 1221-4 (2005)
National Institute Of Diabetes And Digestive And Kidney Diseases
1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1.
Bioorg Med Chem Lett 15: 1217-20 (2005)
Novartis Institutes For Biomedical Research
Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists.
Bioorg Med Chem Lett 15: 1201-4 (2005)
Abbott Laboratories
Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Bioorg Med Chem Lett 15: 1197-200 (2005)
Merck Research Laboratories
1,2,4-Benzothiadiazine derivatives as alpha1 and 5-HT1A receptor ligands.
Bioorg Med Chem Lett 15: 1185-8 (2005)
Universit£
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Bioorg Med Chem Lett 15: 1173-80 (2005)
Merck Frosst Centre For Therapeutic Research
Synthesis and structure-activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H1 antagonists.
Bioorg Med Chem Lett 15: 1165-7 (2005)
RhôNe-Poulenc Rorer
De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold.
Bioorg Med Chem Lett 15: 1161-4 (2005)
Cerep
2,3-Diarylthiophenes as selective EP1 receptor antagonists.
Bioorg Med Chem Lett 15: 1155-60 (2005)
Merck Frosst Centre For Therapeutic Research
Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Bioorg Med Chem Lett 15: 1149-54 (2005)
Universit£
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.
Bioorg Med Chem Lett 15: 1143-7 (2005)
University Of Kansas
Synthesis of half-mustard combi-molecules with fluorescence properties: correlation with EGFR status.
Bioorg Med Chem Lett 15: 1135-8 (2005)
Mcgill University/Royal Victoria Hospital
Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency.
Bioorg Med Chem Lett 15: 1131-3 (2005)
Yale University
Reversal of anticancer drug resistance by COTC based on intracellular glutathione and glyoxalase I.
Bioorg Med Chem Lett 15: 1111-4 (2005)
Keio University
Human immunodeficiency virus-reverse transcriptase inhibition and hepatitis C virus RNA-dependent RNA polymerase inhibition activities of fullerene derivatives.
Bioorg Med Chem Lett 15: 1107-9 (2005)
Kyoritsu University Of Pharmacy
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).
Bioorg Med Chem Lett 15: 1101-6 (2005)
Pharmaceutical Research Institute
Synthesis and evaluation of novel peripherally restricted kappa-opioid receptor agonists.
Bioorg Med Chem Lett 15: 1091-5 (2005)
Adolor
5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.
Bioorg Med Chem Lett 15: 1083-5 (2005)
Ucb Pharma
Tryptamine-based human beta3-adrenergic receptor agonists. Part 3: improved oral bioavailability via modification of the sulfonamide moiety.
Bioorg Med Chem Lett 15: 1061-4 (2005)
Dainippon Pharmaceutical
Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent.
Bioorg Med Chem Lett 15: 1055-9 (2005)
Dainippon Pharmaceutical
Antimitotic activity and reversal of breast cancer resistance protein-mediated drug resistance by stilbenoids from Bletilla striata.
Bioorg Med Chem Lett 15: 1051-4 (2005)
Hokkaido University
Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparative molecular similarity indices analysis (CoMSIA).
Bioorg Med Chem Lett 15: 1027-32 (2005)
National Institute Of Pharmaceutical Education And Research (Niper)
Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists.
Bioorg Med Chem Lett 15: 999-1004 (2005)
Neurocrine Biosciences
Two new irreversible inhibitors of dihydrodipicolinate synthase: diethyl (E,E)-4-oxo-2,5-heptadienedioate and diethyl (E)-4-oxo-2-heptenedioate.
Bioorg Med Chem Lett 15: 995-8 (2005)
University Of Sydney
Molecular docking of the highly hypolipidemic agent alpha-asarone with the catalytic portion of HMG-CoA reductase.
Bioorg Med Chem Lett 15: 989-94 (2005)
Universidad Nacional AutóNoma De MéXico
Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane.
Bioorg Med Chem Lett 15: 977-82 (2005)
Merck Research Laboratories
Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides.
Bioorg Med Chem Lett 15: 971-6 (2005)
Universit£
Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
Bioorg Med Chem Lett 15: 963-9 (2005)
Universit£
QSAR of estrogen receptor modulators: exploring selectivity requirements for ER(alpha) versus ER(beta) binding of tetrahydroisoquinoline derivatives using E-state and physicochemical parameters.
Bioorg Med Chem Lett 15: 957-61 (2005)
University Of Calcutta
A rate determining step change in the pre-steady state of acetylcholinesterase inhibitions by 1,n-alkane-di-N-butylcarbamates.
Bioorg Med Chem Lett 15: 951-5 (2005)
National Chung-Hsing University
Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP.
Bioorg Med Chem Lett 15: 945-9 (2005)
Yale University
Studies towards the next generation of antidepressants. Part 4: derivatives of 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine with affinity for the serotonin transporter and the 5-HT1A receptor.
Bioorg Med Chem Lett 15: 911-4 (2005)
Wyeth Research
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.
Bioorg Med Chem Lett 15: 905-9 (2005)
Merck Research Laboratories
The development of potent and selective bisarylmaleimide GSK3 inhibitors.
Bioorg Med Chem Lett 15: 899-903 (2005)
Lilly Research Laboratories
6'-Methylpyrido[3,4-b]norhomotropane: synthesis and outstanding potency in relation to the alpha4beta2 nicotinic receptor pharmacophore model.
Bioorg Med Chem Lett 15: 877-81 (2005)
University Of California
4'C-ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase.
Bioorg Med Chem Lett 15: 869-71 (2005)
Universit£T Konstanz
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.
Bioorg Med Chem Lett 15: 863-7 (2005)
Vernalis (R&D)
A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design.
Nat Biotechnol 23: 201-7 (2005)
Plexxikon
Lanostane triterpenoids and triterpene glycosides from the fruit body of Fomitopsis pinicola and their inhibitory activity against COX-1 and COX-2.
J Nat Prod 68: 69-73 (2005)
Tokushima Bunri University
Potent CYP3A4 inhibitory constituents of Piper cubeba.
J Nat Prod 68: 64-8 (2005)
Toyama Medical And Pharmaceutical University
Demonstration of a specific site of covalent labeling of the human motilin receptor using a biologically active photolabile motilin analog.
J Pharmacol Exp Ther 313: 1101-8 (2005)
Mayo Clinic
Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists.
J Pharmacol Exp Ther 313: 831-9 (2005)
Taisho Pharmaceutical
Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives.
Bioorg Med Chem 13: 949-61 (2005)
Yamanouchi Pharmaceutical
Vectorial transport of the peptide CCK-8 by double-transfected MDCKII cells stably expressing the organic anion transporter OATP1B3 (OATP8) and the export pump ABCC2.
J Pharmacol Exp Ther 313: 549-56 (2005)
German Cancer Research Center
Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines.
Bioorg Med Chem Lett 15: 833-7 (2005)
Neurocrine Biosciences
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.
Bioorg Med Chem Lett 15: 823-5 (2005)
Martin-Luther-University Halle-Wittenberg
Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
Bioorg Med Chem Lett 15: 817-22 (2005)
F. Hoffmann-La Roche
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 2: Benzimidazole-5-sulfonamides.
Bioorg Med Chem Lett 15: 805-7 (2005)
Kyoto 619-0216
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides.
Bioorg Med Chem Lett 15: 799-803 (2005)
Kyoto 619-0216
Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
Bioorg Med Chem Lett 15: 793-7 (2005)
University Of Michigan
N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists.
Bioorg Med Chem Lett 15: 787-91 (2005)
Dbristol-Myers Squibb
Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.
Bioorg Med Chem Lett 15: 783-6 (2005)
Schering-Plough Research Institute
Non-peptidic small molecule inhibitors of XIAP.
Bioorg Med Chem Lett 15: 771-5 (2005)
Abbott Laboratories
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
Bioorg Med Chem Lett 15: 761-4 (2005)
Merck Research Laboratories
Quinazolinethiones and quinazolinediones, novel inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.
Bioorg Med Chem Lett 15: 751-4 (2005)
Celltech R And D
Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT(7) receptor.
Bioorg Med Chem Lett 15: 747-50 (2005)
Uppsala University
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
Bioorg Med Chem Lett 15: 737-41 (2005)
Glaxosmithkline
Active site directed inhibitors of replication-specific bacterial DNA polymerases.
Bioorg Med Chem Lett 15: 729-32 (2005)
Glsynthesis
4-(2-Pyridyl)piperazine-1-benzimidazoles as potent TRPV1 antagonists.
Bioorg Med Chem Lett 15: 719-23 (2005)
Purdue Pharma
Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
Bioorg Med Chem Lett 15: 715-8 (2005)
Merck Research Laboratories
A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists.
Bioorg Med Chem Lett 15: 693-8 (2005)
Neurocrine Biosciences
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
Bioorg Med Chem Lett 15: 687-91 (2005)
National Health Research Institutes
Parallel synthesis of pteridine derivatives as potent inhibitors for hepatitis C virus NS5B RNA-dependent RNA polymerase.
Bioorg Med Chem Lett 15: 675-8 (2005)
Valeant Pharmaceuticals International
Pyrrolidinohydroquinazolines--a novel class of CCR3 modulators.
Bioorg Med Chem Lett 15: 669-73 (2005)
Boehringer Ingelheim Pharma Gmbh And
Pharmacophore identification of alpha(1A)-adrenoceptor antagonists.
Bioorg Med Chem Lett 15: 657-64 (2005)
China Pharmaceutical University
Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.
Bioorg Med Chem Lett 15: 645-51 (2005)
Merck Research Laboratories
Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1: SAR studies on the determination of the key scaffold.
Bioorg Med Chem Lett 15: 635-8 (2005)
Chinese Academy Of Sciences
Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands.
Bioorg Med Chem Lett 15: 631-4 (2005)
Seoul National University
The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.
Bioorg Med Chem Lett 15: 609-12 (2005)
Cv Therapeutics
Studies on the structure-activity relationship of 2',6'-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H-Dmt-NH-CH(3).
Bioorg Med Chem Lett 15: 599-602 (2005)
Kobe Gakuin University
Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.
Bioorg Med Chem Lett 15: 589-93 (2005)
Organon Laboratories
Generation of a new class of hNK(2) receptor ligands using the 'fragment approach'.
Bioorg Med Chem Lett 15: 585-8 (2005)
Menarini Ricerche
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates.
Bioorg Med Chem Lett 15: 579-84 (2005)
Universit£
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates.
Bioorg Med Chem Lett 15: 573-8 (2005)
Università
Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V, and IX with anions isosteric and isoelectronic with sulfate, nitrate, and carbonate.
Bioorg Med Chem Lett 15: 567-71 (2005)
Universit£
Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP(3) antagonists.
Bioorg Med Chem Lett 15: 527-30 (2005)
Merck Frosst Centre For Therapeutic Research
Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B.
Bioorg Med Chem Lett 15: 523-6 (2005)
Chinese Academy Of Sciences
Synthesis of alkyne derivatives of a novel triazolopyrazine as A(2A) adenosine receptor antagonists.
Bioorg Med Chem Lett 15: 511-5 (2005)
Biogen Idec
Enhanced ligand affinity for receptors in which components of the binding site are independently mobile.
Chem Biol 12: 89-97 (2005)
University Of Sheffield
Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.
Chem Biol 12: 65-76 (2005)
University Of Dundee
Synthesis and biological evaluation of thienopyrrolizines, a new family of CDK/GSK-3 inhibitors.
J Enzyme Inhib Med Chem 19: 585-93 (2004)
UniversitÉ
Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2.
J Med Chem 48: 586-92 (2005)
Kobe Gakuin University
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.
J Med Chem 48: 569-85 (2005)
Newcastle University
Further naphthylcombretastatins. An investigation on the role of the naphthalene moiety.
J Med Chem 48: 556-68 (2005)
Universidad De Salamanca
Sulfonamide drugs binding to the colchicine site of tubulin: thermodynamic analysis of the drug-tubulin interactions by isothermal titration calorimetry.
J Med Chem 48: 547-55 (2005)
Institute
Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
J Med Chem 48: 515-22 (2005)
Salk Institute
Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
J Med Chem 48: 507-14 (2005)
Salk Institute
Identification of 4-substituted 1,2,3-triazoles as novel oxazolidinone antibacterial agents with reduced activity against monoamine oxidase A.
J Med Chem 48: 499-506 (2005)
Astrazeneca Discovery
Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells.
J Med Chem 48: 483-98 (2005)
University Institute Of Pathology
Investigations on the effects of basic side chains on the hormonal profile of (4R,5S)/(4S,5R)-4,5-bis(4-hydroxyphenyl)-2-imidazolines.
J Med Chem 48: 466-74 (2005)
Free University Of Berlin
Quantitative structure-activity relationship (5D-QSAR) study of combretastatin-like analogues as inhibitors of tubulin assembly.
J Med Chem 48: 457-65 (2005)
University Of Salford
Quantitative structure-activity relationship analysis of inhibitors of the nicotine metabolizing CYP2A6 enzyme.
J Med Chem 48: 440-9 (2005)
University Of Kuopio
Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation.
J Med Chem 48: 414-26 (2005)
Astex
Aminoimidazolylmethyluracil analogues as potent inhibitors of thymidine phosphorylase and their bioreductive nitroimidazolyl prodrugs.
J Med Chem 48: 392-402 (2005)
University Of Manchester
Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131.
J Med Chem 48: 380-91 (2005)
Kyoto University
Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
J Med Chem 48: 364-79 (2005)
Novartis Pharmaceuticals
Rational approach to discover multipotent anti-Alzheimer drugs.
J Med Chem 48: 360-3 (2005)
University Of Bologna
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
J Med Chem 48: 353-6 (2005)
Wyeth Research
Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist.
J Med Chem 48: 345-8 (2005)
The University Of Melbourne
Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002.
J Biol Chem 280: 13728-34 (2005)
Vertex Pharmaceuticals
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
Br J Pharmacol 144: 317-22 (2005)
University Of Nottingham
Cyclic sulfamide HIV-1 protease inhibitors, with sidechains spanning from P2/P2' to P1/P1'.
Bioorg Med Chem 13: 755-64 (2005)
Uppsala University
Transport of the dopamine D2 agonist pramipexole by rat organic cation transporters OCT1 and OCT2 in kidney.
Drug Metab Dispos 33: 495-9 (2005)
Tokyo University Of Science
Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors.
J Med Chem 48: 330-4 (2005)
Université
Inhibition of nucleoside transport proteins by C8-alkylamine-substituted purines.
J Med Chem 48: 321-9 (2005)
Leiden University
2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.
J Med Chem 48: 306-11 (2005)
Novo Nordisk
Structure-activity relationships and effects on neuroactive steroid synthesis in a series of 2-phenylimidazo[1,2-a]pyridineacetamide peripheral benzodiazepine receptors ligands.
J Med Chem 48: 292-305 (2005)
Università
Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators.
J Med Chem 48: 287-91 (2005)
Institut Claudius Regaud
Design and NMR characterization of active analogues of compstatin containing non-natural amino acids.
J Med Chem 48: 274-86 (2005)
University Of California Riverside
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
J Med Chem 48: 266-73 (2005)
Universit£
Discovery of corticotropin releasing factor 2 receptor selective sauvagine analogues for treatment of skeletal muscle atrophy.
J Med Chem 48: 262-5 (2005)
Procter & Gamble Pharmaceuticals
5-substituted, 6-substituted, and unsubstituted 3-heteroaromatic pyridine analogues of nicotine as selective inhibitors of cytochrome P-450 2A6.
J Med Chem 48: 224-39 (2005)
Human Biomolecular Research Institute
Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants.
J Med Chem 48: 163-70 (2005)
Max-Planck-Institut Fuer Biochemie
Combined target-based and ligand-based drug design approach as a tool to define a novel 3D-pharmacophore model of human A3 adenosine receptor antagonists: pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as a key study.
J Med Chem 48: 152-62 (2005)
Università
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
J Med Chem 48: 141-51 (2005)
Merck Research Laboratories
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.
J Med Chem 48: 134-40 (2005)
University Of Kansas
Beta-diketo acid pharmacophore hypothesis. 1. Discovery of a novel class of HIV-1 integrase inhibitors.
J Med Chem 48: 111-20 (2005)
University Of Southern California
Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study.
J Med Chem 48: 100-10 (2005)
National Center For Scientific Research Demokritos
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
J Med Chem 48: 71-90 (2005)
Amgen
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
J Med Chem 48: 38-55 (2005)
Abbott Laboratories
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.
J Med Chem 48: 24-7 (2005)
University Of Bologna
Control of hepatitis C: a medicinal chemistry perspective.
J Med Chem 48: 1-20 (2005)
University Of Wollongong
A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.
J Biol Chem 280: 9160-9 (2005)
Genentech
In vitro and in vivo pharmacological characterization of BM-613 [N-n-pentyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl]urea], a novel dual thromboxane synthase inhibitor and thromboxane receptor antagonist.
J Pharmacol Exp Ther 313: 293-301 (2005)
University Of Li&Eagrove;Ge
Meroterpenoid MAPKAP (MK2) inhibitors isolated from the indonesian marine sponge Acanthodendrilla sp.
J Nat Prod 67: 2127-9 (2004)
University Of British Columbia
A phthalide with in vitro growth inhibitory activity from an oidiodendron strain.
J Nat Prod 67: 2086-9 (2004)
Cetek
Laurenditerpenol, a new diterpene from the tropical marine alga Laurenciaintricata that potently inhibits HIF-1 mediated hypoxic signaling in breast tumor cells.
J Nat Prod 67: 2002-7 (2004)
University Of Mississippi
Rat renal organic anion transporter rOAT1 mediates transport of urinary-excreted cephalosporins, but not of biliary-excreted cefoperazone.
Drug Metab Pharmacokinet 17: 125-9 (2002)
Kyoto University Hospital
The potential for an interaction between MRP2 (ABCC2) and various therapeutic agents: probenecid as a candidate inhibitor of the biliary excretion of irinotecan metabolites.
Drug Metab Pharmacokinet 17: 23-33 (2002)
University Of Tokyo
Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1.
Drug Metab Dispos 33: 537-46 (2005)
Pfizer
Synthesis and in vitro antifolate activity of rotationally restricted aminopterin and methotrexate analogues.
J Med Chem 47: 6958-63 (2004)
Harvard Medical School
Bioisosteric modifications of 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5.
J Med Chem 47: 6948-57 (2004)
The Danish University Of Pharmaceutical Sciences
Insertion of an aspartic acid moiety into cyclic pseudopeptides: synthesis and biological characterization of potent antagonists for the human Tachykinin NK-2 receptor.
J Med Chem 47: 6935-47 (2004)
Menarini Ricerche
Design, synthesis, and biological activity of novel, potent, and selective (benzoylaminomethyl)thiophene sulfonamide inhibitors of c-Jun-N-terminal kinase.
J Med Chem 47: 6921-34 (2004)
Serono Pharmaceutical Research Institute
Synthesis of classical, three-carbon-bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.
J Med Chem 47: 6893-901 (2004)
Duquesne University
A screening library for peptide activated G-protein coupled receptors. 1. The test set.
J Med Chem 47: 6864-74 (2004)
Neurocrine Biosciences
Potent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3).
J Med Chem 47: 6854-63 (2004)
The Johns Hopkins University
4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a potent and selective melanocortin-4 receptor antagonist--design, synthesis, and characterization.
J Med Chem 47: 6821-30 (2004)
Neurocrine Biosciences
Design, synthesis, and 3D QSAR of novel potent and selective aromatase inhibitors.
J Med Chem 47: 6792-803 (2004)
University Of Bari
Charge and substituent effects on affinity and metabolism of benzbromarone-based CYP2C19 inhibitors.
J Med Chem 47: 6768-76 (2004)
Washington State University
Design, synthesis, and pharmacological evaluation of pyridinic analogues of nimesulide as cyclooxygenase-2 selective inhibitors.
J Med Chem 47: 6749-59 (2004)
Université
Benzoyl ring halogenated classical 2-amino-6-methyl-3,4-dihydro-4-oxo-5-substituted thiobenzoyl-7H-pyrrolo[2,3-d]pyrimidine antifolates as inhibitors of thymidylate synthase and as antitumor agents.
J Med Chem 47: 6730-9 (2004)
Duquesne University
Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice.
J Med Chem 47: 6716-29 (2004)
University Of Maryland
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
J Med Chem 47: 6702-10 (2004)
University Of Florida
Coaxing a pyridine nucleus to give up its aromaticity: synthesis and pharmacological characterization of novel conformationally restricted analogues of nicotine and anabasine.
J Med Chem 47: 6691-701 (2004)
Indian Institute Of Technology
Virtual screening of human 5-aminoimidazole-4-carboxamide ribonucleotide transformylase against the NCI diversity set by use of AutoDock to identify novel nonfolate inhibitors.
J Med Chem 47: 6681-90 (2004)
The Scripps Research Institute
A novel class of inhibitors of peptide deformylase discovered through high-throughput screening and virtual ligand screening.
J Med Chem 47: 6669-72 (2004)
Stine-Haskell Research Center
Identification of 7-phenylaminothieno- [3,2-b]pyridine-6-carbonitriles as a new class of Src kinase inhibitors.
J Med Chem 47: 6666-8 (2004)
Wyeth Research
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
J Med Chem 47: 6662-5 (2004)
Merck Research Laboratories
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
J Med Chem 47: 6658-61 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation.
J Med Chem 47: 6655-7 (2004)
Abbott Laboratories
Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.
J Pharmacol Exp Ther 313: 165-75 (2005)
Abbott Laboratories
5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.
Bioorg Med Chem Lett 15: 459-65 (2004)
Pfizer
Potent Kv1.3 inhibitors from correolide-modification of the C18 position.
Bioorg Med Chem Lett 15: 447-51 (2004)
Merck Research Laboratories
Design and synthesis of (E)-1,1,2-triarylethenes: novel inhibitors of the cyclooxygenase-2 (COX-2) isozyme.
Bioorg Med Chem Lett 15: 439-42 (2004)
University Of Alberta
Optimization of CRF1R binding affinity of 2-(2,4,6-trichlorophenyl)-4-trifluoromethyl-5-aminomethylthiazoles through rapid and selective parallel synthesis.
Bioorg Med Chem Lett 15: 431-4 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
3D QSAR studies on GSK-3 inhibition by aloisines.
Bioorg Med Chem Lett 15: 395-9 (2005)
Zhejiang University
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.
Bioorg Med Chem Lett 15: 389-93 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Saucerneol B derivatives as human acyl-CoA: cholesterol acyltransferase inhibitors.
Bioorg Med Chem Lett 15: 385-8 (2004)
Korea Research Institute Of Bioscience And Biotechnology
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.
Bioorg Med Chem Lett 15: 379-83 (2004)
Wyeth Research
A novel series of potent gamma-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core.
Bioorg Med Chem Lett 15: 373-8 (2004)
Merck Sharp & Dohme Research Laboratories
Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic isozymes I and II, and the tumor-associated isozyme IX.
Bioorg Med Chem Lett 15: 367-72 (2004)
Harran University
(S,E)-N-[1-(3-heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity.
Bioorg Med Chem Lett 15: 363-6 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Benzoyl 2-methyl indoles as selective PPARgamma modulators.
Bioorg Med Chem Lett 15: 357-62 (2004)
Merck Research Laboratories
Isoterreulactone A, a novel meroterpenoid with anti-acetylcholinesterase activity produced by Aspergillus terreus.
Bioorg Med Chem Lett 15: 353-6 (2004)
Korea Research Institute Of Bioscience And Biotechnology
(2S,1'S,2'R,3'R)-2(2'-Carboxy-3'-hydroxymethylcyclopropyl)glycine-[3H], a potent and selective radioligand for labeling group 2 and 3 metabotropic glutamate receptors.
Bioorg Med Chem Lett 15: 349-51 (2004)
Eli Lilly
Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design.
Bioorg Med Chem Lett 15: 331-5 (2005)
Nagoya City University
QSAR studies on structurally similar 2-(4-methanesulfonylphenyl)pyran-4-ones as selective COX-2 inhibitors: a Hansch approach.
Bioorg Med Chem Lett 15: 313-20 (2004)
Devi Ahilya Vishwavidyalaya
Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers.
Bioorg Med Chem Lett 15: 283-6 (2004)
Korea Institute Of Science & Technology
The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors.
Bioorg Med Chem Lett 15: 277-81 (2004)
Athersys
Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.
Bioorg Med Chem Lett 15: 271-6 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.
Bioorg Med Chem Lett 15: 251-4 (2004)
Fujisawa Pharmaceutical
Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate.
Bioorg Med Chem 13: 425-32 (2005)
Mitsubishi Pharma
Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.
J Pharmacol Exp Ther 313: 410-21 (2005)
I.G.B.M.C.
Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.
J Med Chem 47: 6645-8 (2004)
University Of Bath
Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.
J Med Chem 47: 6616-24 (2004)
Università
Identification of novel parasitic cysteine protease inhibitors using virtual screening. 1. The ChemBridge database.
J Med Chem 47: 6609-15 (2004)
University Of Mississippi
Discovery of pyrano[3,4-b]indoles as potent and selective HCV NS5B polymerase inhibitors.
J Med Chem 47: 6603-8 (2004)
Wyeth Research
Design, synthesis and evaluation of a PLG tripeptidomimetic based on a pyridine scaffold.
J Med Chem 47: 6595-602 (2004)
G£Teborg University
A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors.
J Med Chem 47: 6584-94 (2004)
Boehringer Ingelheim (Canada)
Structure-activity relationship of 6-methylidene penems bearing tricyclic heterocycles as broad-spectrum beta-lactamase inhibitors: crystallographic structures show unexpected binding of 1,4-thiazepine intermediates.
J Med Chem 47: 6556-68 (2004)
Wyeth Research
Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.
J Med Chem 47: 6541-6 (2004)
University Of Cagliary
2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
J Med Chem 47: 6529-40 (2004)
Leiden/Amsterdam Center For Drug Research
Antiestrogen binding site and estrogen receptor mediate uptake and distribution of 4-hydroxytamoxifen-targeted doxorubicin-formaldehyde conjugate in breast cancer cells.
J Med Chem 47: 6509-18 (2004)
University Of Colorado
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.
J Med Chem 47: 6490-8 (2004)
University Of Bologna
Stereochemical analysis of (hydroxyethyl)urea peptidomimetic inhibitors of gamma-secretase.
J Med Chem 47: 6485-9 (2004)
Harvard Medical School
Catecholic flavonoids acting as telomerase inhibitors.
J Med Chem 47: 6466-75 (2004)
Bu-Nerviano Medical Sciences
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.
J Med Chem 47: 6455-8 (2004)
University Of Illinois At Chicago
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).
J Med Chem 47: 6447-50 (2004)
Merck Research Laboratories
The design and enzyme-bound crystal structure of indoline based peptidomimetic inhibitors of hepatitis C virus NS3 protease.
J Med Chem 47: 6443-6 (2004)
Mrl Rome
2,3-diaminopyridine bradykinin B1 receptor antagonists.
J Med Chem 47: 6439-42 (2004)
Merck Research Laboratories
Synthesis and activity of substituted 4-(indazol-3-yl)phenols as pathway-selective estrogen receptor ligands useful in the treatment of rheumatoid arthritis.
J Med Chem 47: 6435-8 (2004)
Wyeth Research
Identification and characterization of nonsubstrate based inhibitors of the essential dengue and West Nile virus proteases.
Bioorg Med Chem 13: 257-64 (2005)
University Of Alabama At Birmingham
Synthesis and aminoacyl-tRNA synthetase inhibitory activity of aspartyl adenylate analogs.
Bioorg Med Chem 13: 69-75 (2005)
Crefsip
The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors.
Bioorg Med Chem 13: 59-68 (2005)
Pfizer
Antitumor agents. Part 236: Synthesis of water-soluble colchicine derivatives.
Bioorg Med Chem Lett 15: 235-8 (2004)
University Of North Carolina
2,3-Diphenylpropionic acids as potent VLA-4 antagonists.
Bioorg Med Chem Lett 15: 217-20 (2004)
Kaken Pharmaceutical
Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.
Bioorg Med Chem Lett 15: 211-5 (2004)
Kyoto Pharmaceutical University
Amino-substituted heterocycles as isosteres of trans-cinnamides: design and synthesis of heterocyclic biaryl sulfides as potent antagonists of LFA-1/ICAM-1 binding.
Bioorg Med Chem Lett 15: 195-201 (2004)
Abbott Laboratories
Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors.
Bioorg Med Chem Lett 15: 185-9 (2004)
Central Pharmaceutical Research Institute
N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide, a novel hydroxamic acid-based inhibitor of aminopeptidase N and its anti-angiogenic activity.
Bioorg Med Chem Lett 15: 181-3 (2004)
Sejong University
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
Bioorg Med Chem Lett 15: 171-5 (2004)
Merck Research Laboratories
Synthesis of digalactosyl diacylglycerols and their structure-inhibitory activity on human lanosterol synthase.
Bioorg Med Chem Lett 15: 159-62 (2004)
National Institute Of Health Sciences
Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Bioorg Med Chem Lett 15: 153-8 (2004)
Abbott Laboratories
Synthesis and activity of 8-substituted benzo[c]quinolizin-3-ones as dual inhibitors of human 5alpha-reductases 1 and 2.
Bioorg Med Chem Lett 15: 145-8 (2004)
Polo Scientifico Università
New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties.
Bioorg Med Chem Lett 15: 135-8 (2004)
University Of The Mediterranean
Design, synthesis, and structural analysis of inhibitors of influenza neuraminidase containing a 2,3-disubstituted tetrahydrofuran-5-carboxylic acid core.
Bioorg Med Chem Lett 15: 125-8 (2004)
Abbott Laboratories
Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain.
Bioorg Med Chem Lett 15: 121-3 (2004)
University Of California San Francisco
Aminothiazole inhibitors of HCV RNA polymerase.
Bioorg Med Chem Lett 15: 115-9 (2004)
Neogenesis Pharmaceuticals
Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.
Bioorg Med Chem Lett 15: 107-13 (2004)
Merck Research Laboratories
Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase.
Bioorg Med Chem Lett 15: 103-6 (2004)
The Scripps Research Institute
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Bioorg Med Chem Lett 15: 93-8 (2004)
Abbott Laboratories
Synthesis and biological evaluation of novel steroidal pyrazoles as substrates for bile acid transporters.
Bioorg Med Chem Lett 15: 85-7 (2004)
Xenoport
Optimization of pyrrolidinone based HIV protease inhibitors.
Bioorg Med Chem Lett 15: 81-4 (2005)
Glaxosmithkline
2,3-Ethylene- and 2,3-trimethylene-bridged analogues of the group III metabotropic glutamate receptor ligand 2-amino-4-phosphonobutanoic acid.
Bioorg Med Chem Lett 15: 57-60 (2004)
University Of Minnesota
2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.
Bioorg Med Chem Lett 15: 51-5 (2004)
Eli Lilly
Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist.
Bioorg Med Chem Lett 15: 41-5 (2004)
Daiichi Pharmaceutical
5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.
Bioorg Med Chem Lett 15: 29-35 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas.
Bioorg Med Chem Lett 15: 25-8 (2004)
Astrazeneca
Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase).
Bioorg Med Chem Lett 15: 15-20 (2005)
University Of Illinois At Chicago
Structural basis for the activity of drugs that inhibit phosphodiesterases.
Structure 12: 2233-47 (2004)
Plexxikon
Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors.
J Nat Prod 67: 1882-5 (2004)
Instituto De Qu£Mica Da Universidade Estadual Paulista
Isolation of cytochrome P450 inhibitors from strawberry fruit, Fragaria ananassa.
J Nat Prod 67: 1839-41 (2004)
Kanazawa University
Estrogenic and anticarcinogenic properties of kurarinone, a lavandulyl flavanone from the roots of Sophora flavescens.
J Nat Prod 67: 1829-32 (2004)
Ghent University
Mechanism-based inactivation of COX-1 by red wine m-hydroquinones: a structure-activity relationship study.
J Nat Prod 67: 1777-82 (2004)
University Of Pennsylvania School Of Medicine
Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1.
Eur J Pharm Biopharm 59: 17-24 (2004)
Biozentrum Of The Martin-Luther-University Halle-Wittenberg
Discovery of novel phenolic antioxidants as inhibitors of vascular cell adhesion molecule-1 expression for use in chronic inflammatory diseases.
J Med Chem 47: 6420-32 (2004)
Atherogenics
Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.
J Med Chem 47: 6401-9 (2004)
Research Triangle Institute
New constrained"molecular tongs" designed to dissociate HIV-1 protease dimer.
J Med Chem 47: 6392-400 (2004)
Paris-Sud University
Synthesis of tropeines and allosteric modulation of ionotropic glycine receptors.
J Med Chem 47: 6384-91 (2004)
Hungarian Academy Of Sciences
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.
J Med Chem 47: 6363-72 (2004)
Merck Research Laboratories
Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives.
J Med Chem 47: 6326-37 (2004)
RhôNe-Poulenc Rorer
Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position.
J Med Chem 47: 6311-25 (2004)
Eberhard-Karls-University TüBingen
An in silico approach to discovering novel inhibitors of human sirtuin type 2.
J Med Chem 47: 6292-8 (2004)
University Of Kuopio
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.
J Med Chem 47: 6283-91 (2004)
Bristol-Myers Squibb
Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-alpha converting enzyme and matrix metalloproteinase inhibitors.
J Med Chem 47: 6255-69 (2004)
Wyeth Research
Acetylcholinesterase inhibitory activity of scopolin and scopoletin discovered by virtual screening of natural products.
J Med Chem 47: 6248-54 (2004)
Leopold-Franzens University Of Innsbruck
Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole.
J Med Chem 47: 6239-47 (2004)
Università
Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists.
J Med Chem 47: 6218-29 (2004)
Biogen Idec
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
J Med Chem 47: 6195-206 (2004)
Université
Discovery of bicyclic thymidine analogues as selective and high-affinity inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase.
J Med Chem 47: 6187-94 (2004)
Ghent University
alpha 2-adrenoreceptors profile modulation. 2. Biphenyline analogues as tools for selective activation of the alpha 2C-subtype.
J Med Chem 47: 6160-73 (2004)
Universit£
Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl)propyl]bis(4-fluorophenyl)amines as potential irreversible ligands for the dopamine transporter.
J Med Chem 47: 6128-36 (2004)
National Institute On Drug Abuse
Lactams as EP4 prostanoid receptor agonists. 3. Discovery of N-ethylbenzoic acid 2-pyrrolidinones as subtype selective agents.
J Med Chem 47: 6124-7 (2004)
Roche Palo Alto
Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases.
J Med Chem 47: 6117-9 (2004)
Merck Research Laboratories
The complex of a bivalent derivative of galanthamine with torpedo acetylcholinesterase displays drastic deformation of the active-site gorge: implications for structure-based drug design.
J Am Chem Soc 126: 15405-11 (2004)
Weizmann Institute Of Science
Functional cloning of Bacillus anthracis dihydrofolate reductase and confirmation of natural resistance to trimethoprim.
Antimicrob Agents Chemother 48: 4643-9 (2004)
Oklahoma State University At Stillwater
Pharmacological inhibitors of glycogen synthase kinase 3.
Trends Pharmacol Sci 25: 471-80 (2004)
The Rockefeller University
Synthesis and urease enzyme inhibitory effects of some dicoumarols.
J Enzyme Inhib Med Chem 19: 367-71 (2004)
University Of Karachi
Conversion of human-selective PPARalpha agonists to human/mouse dual agonists: a molecular modeling analysis.
Bioorg Med Chem Lett 14: 6113-6 (2004)
Eli Lilly
The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
Bioorg Med Chem Lett 14: 6107-11 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.
Bioorg Med Chem Lett 14: 6095-9 (2004)
Avenida De La Industria
QSAR modelling of HIV-1 reverse transcriptase inhibition by benzoxazinones using a combination of P_VSA and pharmacophore feature descriptors.
Bioorg Med Chem Lett 14: 6089-94 (2004)
S.G.S.I.T.S.
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.
Bioorg Med Chem Lett 14: 6083-7 (2004)
University Of Newcastle
Novel diarylsulfonylurea derivatives as potent antimitotic agents.
Bioorg Med Chem Lett 14: 6075-8 (2004)
Lg Life Sciences
Structure-based virtual screening and biological evaluation of potent and selective ADAM12 inhibitors.
Bioorg Med Chem Lett 14: 6071-4 (2004)
Department Of Life Science And National Research Laboratory Of Proteolysis
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.
Bioorg Med Chem Lett 14: 6061-6 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design of bivalent ligands using hydrogen bond linkers: synthesis and evaluation of inhibitors for human beta-tryptase.
Bioorg Med Chem Lett 14: 6053-6 (2004)
Aventis Pharmaceuticals
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors.
Bioorg Med Chem Lett 14: 6049-52 (2004)
Nitromed
Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.
Bioorg Med Chem Lett 14: 6045-8 (2004)
Merck Research Laboratories
Antiviral compounds from traditional Chinese medicines Galla Chinese as inhibitors of HCV NS3 protease.
Bioorg Med Chem Lett 14: 6041-4 (2004)
Peking University
CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability.
Bioorg Med Chem Lett 14: 6017-21 (2004)
Cv Therapeutics
Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists.
Bioorg Med Chem Lett 14: 6011-6 (2004)
Eli Lilly
Synthesis of 8-thiabicyclo[3.2.1]oct-2-enes and their binding affinity for the dopamine and serotonin transporters.
Bioorg Med Chem Lett 14: 6007-10 (2004)
Organix
Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides.
Bioorg Med Chem Lett 14: 6001-6 (2004)
Pennsylvania State University
Alpha-1-C-alkyl-1-deoxynojirimycin derivatives as potent and selective inhibitors of intestinal isomaltase: remarkable effect of the alkyl chain length on glycosidase inhibitory profile.
Bioorg Med Chem Lett 14: 5991-5 (2004)
Universit£
Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists.
Bioorg Med Chem Lett 14: 5975-8 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Tryptamine-based human beta3-adrenergic receptor agonists. Part 2: SAR of the methylene derivatives.
Bioorg Med Chem Lett 14: 5963-6 (2004)
Dainippon Pharmaceutical
Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring.
Bioorg Med Chem Lett 14: 5959-62 (2004)
Dainippon Pharmaceutical
A new class of acyclic 2-alkyl-1,1,2-triaryl (Z)-olefins as selective cyclooxygenase-2 inhibitors.
J Med Chem 47: 6108-11 (2004)
University Of Alberta
Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain.
J Med Chem 47: 6070-81 (2004)
Universit£
Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane.
J Med Chem 47: 6034-41 (2004)
Virginia Commonwealth University
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
J Med Chem 47: 6025-33 (2004)
University Of Florida
AT2-selective angiotensin II analogues containing tyrosine-functionalized 5,5-bicyclic thiazabicycloalkane dipeptide mimetics.
J Med Chem 47: 6009-19 (2004)
Uppsala University
Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.
J Med Chem 47: 5995-6008 (2004)
Uppsala University
Building predictive models for protein tyrosine phosphatase 1B inhibitors based on discriminating structural features by reassembling medicinal chemistry building blocks.
J Med Chem 47: 5984-94 (2004)
Leadscope
5-substituted tetrazoles as bioisosteres of carboxylic acids. Bioisosterism and mechanistic studies on glutathione reductase inhibitors as antimalarials.
J Med Chem 47: 5972-83 (2004)
Université
Tetrahydrobiopterin binding to aromatic amino acid hydroxylases. Ligand recognition and specificity.
J Med Chem 47: 5962-71 (2004)
University Of Bergen
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
J Med Chem 47: 5953-61 (2004)
Uppsala University
Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.
J Med Chem 47: 5945-52 (2004)
University Of Bologna
Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1.
J Med Chem 47: 5912-22 (2004)
University Of Oxford
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.
J Med Chem 47: 5894-911 (2004)
Bristol-Myers Squibb
Fluorinated phenylcyclopropylamines. 2. Effects of aromatic ring substitution and of absolute configuration on inhibition of microbial tyramine oxidase.
J Med Chem 47: 5860-71 (2004)
Universit£T M£Nster
Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.
J Med Chem 47: 5833-6 (2004)
Novartis Institutes For Biomedical Research
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
J Med Chem 47: 5829-32 (2004)
Merck Sharp & Dohme Research Laboratories
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
J Med Chem 47: 5825-8 (2004)
Merck Research Laboratories
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.
J Med Chem 47: 5821-4 (2004)
Acenta Discovery
Inhibition of wild-type and mutant human immunodeficiency virus type 1 proteases by GW0385 and other arylsulfonamides.
Biochemistry 43: 14500-7 (2004)
Glaxosmithkline
Synthesis and biological evaluation of 4-imidazolylflavans as nonsteroidal aromatase inhibitors.
Bioorg Chem 32: 494-503 (2004)
BiomolÉCules Et Cibles Cellulaires Tumorales
Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).
J Mol Biol 344: 527-47 (2004)
Celera
Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.
Bioorg Med Chem 12: 6171-82 (2004)
Yamanouchi Pharmaceutical
The core structures of roseophilin and the prodigiosin alkaloids define a new class of protein tyrosine phosphatase inhibitors.
Chembiochem 5: 1575-9 (2004)
Max-Planck-Institut FÜR Kohlenforschung
[(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a highly potent and selective agonist of the nociceptin/orphanin FQ receptor.
J Pharmacol Exp Ther 312: 1114-23 (2005)
Section Of Pharmacology
Efficient evaluation of binding free energy using continuum electrostatics solvation.
J Med Chem 47: 5791-7 (2004)
University Of ZüRich
Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.
J Med Chem 47: 5783-90 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Studies of targeting and intracellular trafficking of an anti-androgen doxorubicin-formaldehyde conjugate in PC-3 prostate cancer cells bearing androgen receptor-GFP chimera.
J Med Chem 47: 5690-9 (2004)
University Of Colorado
Structural characterization and pharmacology of a potent (Cys101-Cys119, Cys110-Cys117) bicyclic agouti-related protein (AGRP) melanocortin receptor antagonist.
J Med Chem 47: 5662-73 (2004)
University Of Florida
Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.
J Med Chem 47: 5620-9 (2004)
Budapest University Of Technology And Economics
Benzoxepin-derived estrogen receptor modulators: a novel molecular scaffold for the estrogen receptor.
J Med Chem 47: 5612-5 (2004)
Trinity College Dublin
A cyclopent-2-enecarbonyl group mimics proline at the P2 position of prolyl oligopeptidase inhibitors.
J Med Chem 47: 5605-7 (2004)
University Of Kuopio
NO-sartans: a new class of pharmacodynamic hybrids as cardiovascular drugs.
J Med Chem 47: 5597-600 (2004)
Universit£
Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha.
J Med Chem 47: 5593-6 (2004)
X-Ceptor Therapeutics
Factors controlling the complex architecture of native and modified cyclodextrins with dipeptide (Z-Glu-Tyr) studied by microcalorimetry and NMR spectroscopy: critical effects of peripheral bis-trimethylamination and cavity size.
J Am Chem Soc 126: 14224-33 (2004)
Nagoya Institute Of Technology
1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability.
Bioorg Med Chem Lett 14: 5937-41 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic.
Bioorg Med Chem Lett 14: 5925-9 (2004)
Kyoto Pharmaceutical University
Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases.
Bioorg Med Chem Lett 14: 5907-11 (2004)
Merck Research Laboratories
Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability.
Bioorg Med Chem Lett 14: 5899-902 (2004)
Schering-Plough Research Institute
Tetrahydroisoquinoline derivatives as melatonin MT2 receptor antagonists.
Bioorg Med Chem Lett 14: 5881-4 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators.
Bioorg Med Chem Lett 14: 5867-72 (2004)
Merck Research Laboratories
The impact of spacer structure on 5-HT7 and 5-HT1A receptor affinity in the group of long-chain arylpiperazine ligands.
Bioorg Med Chem Lett 14: 5863-6 (2004)
Polish Academy Of Sciences
Evaluation of by disubstituted acridone derivatives as telomerase inhibitors: the importance of G-quadruplex binding.
Bioorg Med Chem Lett 14: 5845-9 (2004)
University Of London
Synthesis and alpha4beta2 nicotinic affinity of 2-pyrrolidinylmethoxyimines and prolinal oxime ethers.
Bioorg Med Chem Lett 14: 5827-30 (2004)
Università
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.
Bioorg Med Chem Lett 14: 5817-22 (2004)
Merck
Design, synthesis, and evaluation of hexahydrobenz[f]isoquinolines as a novel class of dopamine 3 receptor ligands.
Bioorg Med Chem Lett 14: 5813-6 (2004)
University Of Michigan
Synthesis of small molecule CDC25 phosphatases inhibitors.
Bioorg Med Chem Lett 14: 5809-12 (2004)
Institut Henri Beaufour
Inactivation of human S-adenosylhomocysteine hydrolase by covalent labeling of cysteine 195 with thionucleoside derivatives.
Bioorg Med Chem Lett 14: 5803-7 (2004)
Umr 6519
Inactivation of S-adenosylhomocysteine hydrolase with haloethyl and dihalocyclopropyl esters derived from homoadenosine-6'-carboxylic acid.
Bioorg Med Chem Lett 14: 5799-802 (2004)
Umr 6519
Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases.
Bioorg Med Chem Lett 14: 5793-7 (2004)
Novartis Institutes For Biomedical Research
Carbonic anhydrase inhibitors. Design of anticonvulsant sulfonamides incorporating indane moieties.
Bioorg Med Chem Lett 14: 5781-6 (2004)
Universit£
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide.
Bioorg Med Chem Lett 14: 5775-80 (2004)
Universit£
Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions.
Bioorg Med Chem Lett 14: 5769-73 (2004)
Universit£
Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with phosphates, carbamoyl phosphate, and the phosphonate antiviral drug foscarnet.
Bioorg Med Chem Lett 14: 5763-7 (2004)
Università
Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex.
Bioorg Med Chem Lett 14: 5751-5 (2004)
Schering-Plough Research Institute
Haloperidol: towards further understanding of the structural contributions of its pharmacophoric elements at D2-like receptors.
Bioorg Med Chem Lett 14: 5739-42 (2004)
Florida A&M University
Benzolamide is not a membrane-impermeant carbonic anhydrase inhibitor.
J Enzyme Inhib Med Chem 19: 269-73 (2004)
UniversitÀ Degli Studi Di Firenze
DNA polymerase beta lyase inhibitors from Maytenus putterlickoides.
J Nat Prod 67: 1744-7 (2004)
University Of Virginia
Marine sesquiterpenoids that inhibit the lyase activity of DNA polymerase beta.
J Nat Prod 67: 1716-8 (2004)
Virginia Polytechnic Institute And State University
Inhibition of the human chemokine receptor CCR5 by variecolin and variecolol and isolation of four new variecolin analogues, emericolins A-D, from Emericella aurantiobrunnea.
J Nat Prod 67: 1681-4 (2004)
Merlion Pharmaceuticals
Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A).
Eur J Pharmacol 503: 25-30 (2004)
Kyoto University Hospital
Dihydrexidine--the first full dopamine D1 receptor agonist.
CNS Drug Rev 10: 230-42 (2004)
Karolinska Institutet
Role of inhibitor aliphatic chain in the thermodynamics of inhibitor binding to Escherichia coli enoyl-ACP reductase and the Phe203Leu mutant: a proposed mechanism for drug resistance.
Biochemistry 43: 13380-9 (2004)
University Of Alabama At Birmingham
Multicopy suppressors for novel antibacterial compounds reveal targets and drug efflux susceptibility.
Chem Biol 11: 1423-30 (2004)
Mcmaster University
Disruption of protein-membrane binding and identification of small-molecule inhibitors of coagulation factor VIII.
Chem Biol 11: 1413-22 (2004)
University Of Washington
Synthesis, radiolabeling, and preliminary biological evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X7 receptor.
Bioorg Med Chem Lett 14: 5709-12 (2004)
Università
Carbonic anhydrase inhibitors: inhibition of human cytosolic isozyme II and mitochondrial isozyme V with a series of benzene sulfonamide derivatives.
Bioorg Med Chem Lett 14: 5703-7 (2004)
Università
Azepinone as a conformational constraint in the design of kappa-opioid receptor agonists.
Bioorg Med Chem Lett 14: 5693-7 (2004)
Adolor
Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties.
Bioorg Med Chem Lett 14: 5689-92 (2004)
Glaxosmithkline
Potent inhibitors of the HIV-1 protease incorporating cyclic urea P1-P2 scaffold.
Bioorg Med Chem Lett 14: 5685-7 (2004)
Glaxosmithkline
Myxopyronin B analogs as inhibitors of RNA polymerase, synthesis and biological evaluation.
Bioorg Med Chem Lett 14: 5667-72 (2004)
Anadys Pharmaceuticals
Synthesis and CYP24 inhibitory activity of 2-substituted-3,4-dihydro-2H-naphthalen-1-one (tetralone) derivatives.
Bioorg Med Chem Lett 14: 5651-4 (2004)
Cardiff University
Synthesis of 5'-substituted fluoro-neplanocin A analogues: importance of a hydrogen bonding donor at 5'-position for the inhibitory activity of S-adenosylhomocysteine hydrolase.
Bioorg Med Chem Lett 14: 5641-4 (2004)
Pusan National University
Synthesis and amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents.
Bioorg Med Chem Lett 14: 5635-9 (2004)
Harvard Medical School
Synthesis of 61-bis(1-adamantylcarbamoyl)-1,2-methano[60]fullerene and its antagonistic effect on haloperidol-induced catalepsy in mice.
Bioorg Med Chem Lett 14: 5619-21 (2004)
Kyushu University
QSAR modeling of the MAO inhibitory activity of xanthones derivatives.
Bioorg Med Chem Lett 14: 5611-7 (2004)
Unne
Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 14: 5605-9 (2004)
Neurocrine Biosciences
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists.
Bioorg Med Chem Lett 14: 5599-603 (2004)
Merck Research Laboratories
Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin.
Bioorg Med Chem Lett 14: 5595-8 (2004)
National Cancer Institute-Frederick
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.
Bioorg Med Chem Lett 14: 5591-4 (2004)
Ucb Pharma
Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics.
Bioorg Med Chem Lett 14: 5573-7 (2004)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors.
Bioorg Med Chem Lett 14: 5543-6 (2004)
Abbott Laboratories
Novel fibrinogen receptor antagonists. RGDF mimetics, derivatives of 4-(isoindoline-5-yl)amino-4-oxobutyric acid.
Bioorg Med Chem Lett 14: 5533-5 (2004)
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine
Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.
Bioorg Med Chem Lett 14: 5521-5 (2004)
Pfizer
Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists.
Bioorg Med Chem Lett 14: 5513-9 (2004)
Purdue Pharma
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.
Bioorg Med Chem Lett 14: 5509-12 (2004)
Pfizer
A 13C NMR approach to categorizing potential limitations of alpha,beta-unsaturated carbonyl systems in drug-like molecules.
Bioorg Med Chem Lett 14: 5503-7 (2004)
Abbott Bioresearch Center
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands.
Bioorg Med Chem Lett 14: 5499-502 (2004)
Wyeth Research
Parallel methods for the preparation and SAR exploration of N-ethyl-4-[(8-alkyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-aryl-methyl]-benzamides, powerful mu and delta opioid agonists.
Bioorg Med Chem Lett 14: 5493-8 (2004)
Johnson And Johnson Pharmaceutical Research And Development
Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors.
Bioorg Med Chem Lett 14: 5489-91 (2004)
Dupont Pharmaceuticals
Expedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology.
Bioorg Med Chem Lett 14: 5485-8 (2004)
Merck Research Laboratories
Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.
Bioorg Med Chem Lett 14: 5481-4 (2004)
Merck Research Laboratories
3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
Bioorg Med Chem Lett 14: 5477-80 (2004)
Merck Research Laboratories
2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
Bioorg Med Chem Lett 14: 5473-6 (2004)
Merck Research Laboratories
Evaluation of lactam-bridged neurotensin analogues adjusting psi(Pro10) close to the experimentally derived bioactive conformation of NT(8-13).
J Med Chem 47: 5587-90 (2004)
Friedrich-Alexander University
Spectroscopic studies of diketoacids-metal interactions. A probing tool for the pharmacophoric intermetallic distance in the HIV-1 integrase active site.
J Med Chem 47: 5583-6 (2004)
Université
Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring.
J Med Chem 47: 5555-66 (2004)
Yale University
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.
J Med Chem 47: 5535-40 (2004)
Universit£
A docking score function for estimating ligand-protein interactions: application to acetylcholinesterase inhibition.
J Med Chem 47: 5492-500 (2004)
University Of Kansas
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.
J Med Chem 47: 5467-81 (2004)
Pfizer
Novel 5-HT7 receptor inverse agonists. Synthesis and molecular modeling of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides.
J Med Chem 47: 5451-66 (2004)
State University Of Groningen
Inhibition of nucleoside transport by new analogues of 4-nitrobenzylthioinosine: replacement of the ribose moiety by substituted benzyl groups.
J Med Chem 47: 5441-50 (2004)
Leiden University
Influence of the linker in bispyridium compounds on the inhibition of human choline kinase.
J Med Chem 47: 5433-40 (2004)
Universidad De Grenada
A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors.
J Med Chem 47: 5418-26 (2004)
Walter Reed Army Institute Of Research
Identification and specificity studies of small-molecule ligands for SH3 protein domains.
J Med Chem 47: 5405-17 (2004)
The University Of Adelaide
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
J Med Chem 47: 5393-404 (2004)
National Institute Of Diabetes And Digestive And Kidney Diseases
Successful virtual screening for a submicromolar antagonist of the neurokinin-1 receptor based on a ligand-supported homology model.
J Med Chem 47: 5381-92 (2004)
Philipps-Universit£T Marburg
Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
J Med Chem 47: 5367-80 (2004)
Eli Lilly
Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.
J Med Chem 47: 5356-66 (2004)
Boehringer Ingelheim Pharmaceuticals
Validation of model of cytochrome P450 2D6: an in silico tool for predicting metabolism and inhibition.
J Med Chem 47: 5340-6 (2004)
University Of Leicester
HCV NS5b RNA-dependent RNA polymerase inhibitors: from alpha,gamma-diketoacids to 4,5-dihydroxypyrimidine- or 3-methyl-5-hydroxypyrimidinonecarboxylic acids. Design and synthesis.
J Med Chem 47: 5336-9 (2004)
Italy. Vinc
Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist.
Br J Pharmacol 143: 649-61 (2004)
Johnson & Johnson Pharmaceutical Research And Development
BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.
Cancer Res 64: 7099-109 (2004)
Bayer Pharmaceuticals
5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors.
J Med Chem 47: 5318-29 (2004)
Instituto De Qu£Mica M£Dica (Csic)
Design and synthesis of novel indole beta-diketo acid derivatives as HIV-1 integrase inhibitors.
J Med Chem 47: 5298-310 (2004)
Università
Synthesis and evaluation of nitrofuranylamides as novel antituberculosis agents.
J Med Chem 47: 5276-83 (2004)
University Of Tennessee Health Science Center
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.
J Med Chem 47: 5258-64 (2004)
University Of Pennsylvania
Stereoselective synthesis of sugar-modified enyne analogues of adenosine and uridine. Interaction with S-adenosyl-L-homocysteine hydrolase and antiviral and cytotoxic effects.
J Med Chem 47: 5251-7 (2004)
Florida International University
Subtype selective substrates for histone deacetylases.
J Med Chem 47: 5235-43 (2004)
Westf£Lische Wilhelms-Universit£T M£Nster
Carbonic anhydrase inhibitors: the first on-resin screening of a 4-sulfamoylphenylthiourea library.
J Med Chem 47: 5224-9 (2004)
University Of Florence
Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-].
J Med Chem 47: 5198-203 (2004)
Universit£
Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element.
J Med Chem 47: 5167-82 (2004)
Daiichi Pharmaceutical
Effects of altering the electronics of 2-methoxyestradiol on cell proliferation, on cytotoxicity in human cancer cell cultures, and on tubulin polymerization.
J Med Chem 47: 5126-39 (2004)
Purdue University
Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl)benzylamine with elucidation of bioactive conformation: discovery of 1,4-diazabicyclo[3.3.1]nonane derivatives and evaluation of their biological properties for the monoamine transporters.
J Med Chem 47: 5101-13 (2004)
Wayne State University
Identification and characterization of small molecule inhibitors of the calcium-dependent S100B-p53 tumor suppressor interaction.
J Med Chem 47: 5085-93 (2004)
University Of Maryland
Soft docking and multiple receptor conformations in virtual screening.
J Med Chem 47: 5076-84 (2004)
University Of California San Francisco
Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
J Med Chem 47: 5069-75 (2004)
University Of Bath
Ketoamide-based inhibitors of cysteine protease, cathepsin K: P3 modifications.
J Med Chem 47: 5057-68 (2004)
Glaxosmithkline
Potent and selective ketoamide-based inhibitors of cysteine protease, cathepsin K.
J Med Chem 47: 5049-56 (2004)
Glaxosmithkline
Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.
J Med Chem 47: 5021-40 (2004)
Wyeth Research
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.
J Med Chem 47: 5009-20 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies.
J Med Chem 47: 4998-5008 (2004)
Università
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor.
J Med Chem 47: 4985-8 (2004)
The Pennsylvania State University
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 14: 5445-8 (2004)
Glaxosmithkline
Carbonic anhydrase inhibitors. Inhibition of the newly isolated murine isozyme XIII with anions.
Bioorg Med Chem Lett 14: 5435-9 (2004)
Universit£
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties.
Bioorg Med Chem Lett 14: 5427-33 (2004)
Universit£
Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure-activity relationships of diamine derivatives.
Bioorg Med Chem Lett 14: 5413-6 (2004)
Deltagen Research Laboratories
Small molecule inhibitors of the CCR2b receptor. Part 1: Discovery and optimization of homopiperazine derivatives.
Bioorg Med Chem Lett 14: 5407-11 (2004)
Institute For Bio-Medical Research
Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase.
Bioorg Med Chem Lett 14: 5389-94 (2004)
Astrazeneca
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.
Bioorg Med Chem Lett 14: 5383-7 (2004)
Astrazeneca
Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.
Bioorg Med Chem Lett 14: 5377-81 (2004)
Research Triangle Institute
Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors.
Bioorg Med Chem Lett 14: 5371-6 (2004)
Abbott Laboratories
Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors.
Bioorg Med Chem Lett 14: 5367-70 (2004)
Abbott Laboratories
Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones.
Bioorg Med Chem Lett 14: 5343-6 (2004)
Crest Research Project
Three new compounds from the plant Lippia alva as inhibitors of chemokine receptor 5 (CCR5).
Bioorg Med Chem Lett 14: 5339-42 (2004)
Schering-Plough Research Institute
HCV NS5B polymerase-bound conformation of a soluble sulfonamide inhibitor by 2D transferred NOESY.
Bioorg Med Chem Lett 14: 5333-7 (2004)
Virochem Pharma
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones.
Bioorg Med Chem Lett 14: 5329-32 (2004)
Merck Research Laboratories
Substrate analogs for the investigation of deoxyxylulose 5-phosphate reductoisomerase inhibition: synthesis and evaluation.
Bioorg Med Chem Lett 14: 5309-12 (2004)
Oregon State University
More potent linear peptide inhibitors of mammalian ribonucleotide reductase.
Bioorg Med Chem Lett 14: 5301-4 (2004)
University Of Pennsylvania
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group.
Bioorg Med Chem Lett 14: 5295-300 (2004)
Maxim Pharmaceuticals
Synthesis and structure-activity investigation of iodinated arylhydantoins and arylthiohydantoins for development as androgen receptor radioligands.
Bioorg Med Chem Lett 14: 5285-8 (2004)
The University Of Michigan Medical School
Novel aryloxy-8-azabicyclo[3.2.1]oct-3-enes with 5-HT transporter and 5-HT1A affinity.
Bioorg Med Chem Lett 14: 5281-4 (2004)
Wyeth Research
Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.
Bioorg Med Chem Lett 14: 5275-9 (2004)
Purdue Pharma
5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa.
Bioorg Med Chem Lett 14: 5269-73 (2004)
Bristol-Myers Squibb
SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.
Bioorg Med Chem Lett 14: 5263-7 (2004)
Bristol-Myers Squibb
Synthesis and enzymatic evaluation of xanthine oxidase-activated prodrugs based on inhibitors of thymidine phosphorylase.
Bioorg Med Chem Lett 14: 5247-50 (2004)
University Of Manchester
Design and synthesis of indole and tetrahydroisoquinoline hydantoin derivatives as human chymase inhibitors.
J Enzyme Inhib Med Chem 19: 137-43 (2004)
UniversitÉ
Biscoumarin derivatives from Edgeworthia gardneri that inhibit the lyase activity of DNA polymerase beta.
J Nat Prod 67: 1608-10 (2004)
University Of Virginia
BI-32169, a bicyclic 19-peptide with strong glucagon receptor antagonist activity from Streptomyces sp.
J Nat Prod 67: 1528-31 (2004)
Boehringer Ingelheim Pharma Gmbh And
Interactions of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen with P-glycoprotein and CYP3A.
Biopharm Drug Dispos 25: 283-9 (2004)
Tufts University School Of Medicine
Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo.
J Pharmacol Exp Ther 312: 220-30 (2005)
Temple University
Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins.
Bioorg Med Chem Lett 14: 5227-32 (2004)
Johnson & Johnson Pharmaceutical Research And Development
Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists.
Bioorg Med Chem Lett 14: 5223-6 (2004)
Abbott Laboratories
Facile incorporation of urea pseudopeptides into protease substrate analogue inhibitors.
Bioorg Med Chem Lett 14: 5219-22 (2004)
Purdue University
Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.
Bioorg Med Chem Lett 14: 5215-8 (2004)
Upres Ea 1085 BiomoléCules Et Cibles Cellulaires Tumorales
Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent.
Bioorg Med Chem Lett 14: 5205-9 (2004)
University Of Mainz
Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.
Bioorg Med Chem Lett 14: 5199-203 (2004)
University Of California San Francisco
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
Bioorg Med Chem Lett 14: 5193-8 (2004)
Daiichi Pharmaceutical
Synthesis of 5a-carba-hexopyranoses and hexopyranosylamines, as well as 5a,5a'-dicarbadisaccharides, from 3,8-dioxatricyclo[4.2.1.0(2,4)]nonan-9-ol: glycosidase inhibitory activity of N-substituted 5a-carba-beta-gluco- and beta-galactopyranosylamines, and derivatives thereof.
Bioorg Med Chem Lett 14: 5183-8 (2004)
Keio University
Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.
Bioorg Med Chem Lett 14: 5171-4 (2004)
Central Pharmaceutical Research Institute
N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide: an orally bioavailable melatonin receptor agonist.
Bioorg Med Chem Lett 14: 5157-60 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Potent and selective proline derived dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 14: 5151-5 (2004)
Merck
Glycosylated dihydrochalcones as potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitors.
Bioorg Med Chem Lett 14: 5121-5 (2004)
Johnson & Johnson Pharmaceutical Research And Development
Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I).
Bioorg Med Chem Lett 14: 5113-6 (2004)
University Of Southern California
Benzothiophene and naphthalene derived constrained SERMs.
Bioorg Med Chem Lett 14: 5103-6 (2004)
Eli Lilly
Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.
Bioorg Med Chem Lett 14: 5095-8 (2004)
Abbott Laboratories
Active site inhibitors of HCV NS5B polymerase. The development and pharmacophore of 2-thienyl-5,6-dihydroxypyrimidine-4-carboxylic acid.
Bioorg Med Chem Lett 14: 5085-8 (2004)
Mrl Rome
Development of a polyvalent assay system for lead identification.
Bioorg Med Chem Lett 14: 5081-3 (2004)
Wyeth Research
4-Acylamino-and 4-ureidobenzamides as melanin-concentrating hormone (MCH) receptor 1 antagonists.
Bioorg Med Chem Lett 14: 5075-80 (2004)
7Tm Pharma
5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.
Bioorg Med Chem Lett 14: 5067-70 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor.
Bioorg Med Chem Lett 14: 5057-62 (2004)
Abbott Laboratories
1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor.
Bioorg Med Chem Lett 14: 5045-50 (2004)
Purdue Pharma
Comparing the accumulation of active- and nonactive-site mutations in the HIV-1 protease.
Biochemistry 43: 12141-51 (2004)
University Of Florida College Of Medicine
Molecular design of cholesterols as inhibitors of DNA polymerase alpha.
J Med Chem 47: 4971-4 (2004)
Frontier Research Center For Genome & Drug Discovery
A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma.
J Med Chem 47: 4950-7 (2004)
Novartis Institutes For Biomedical Research And Novartis Pharma Development
Macrocyclic inhibitors for peptide deformylase: a structure-activity relationship study of the ring size.
J Med Chem 47: 4941-9 (2004)
The Ohio State University
Novel synthesis of 3,4-diarylisoxazole analogues of valdecoxib: reversal cyclooxygenase-2 selectivity by sulfonamide group removal.
J Med Chem 47: 4881-90 (2004)
Università
Novel cyclooxygenase-1 inhibitors discovered using affinity fingerprints.
J Med Chem 47: 4875-80 (2004)
Telik
Conformationally constrained analogues of diacylglycerol (DAG). 23. Hydrophobic ligand-protein interactions versus ligand-lipid interactions of DAG-lactones with protein kinase C (PK-C).
J Med Chem 47: 4858-64 (2004)
National Cancer Institute-Frederick
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.
J Med Chem 47: 4829-37 (2004)
Merck Research Laboratories
Nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S.
J Med Chem 47: 4799-801 (2004)
Johnson & Johnson Pharmaceutical Research And Development
Bisubstrate inhibitors of the enzyme catechol O-methyltransferase (COMT): efficient inhibition despite the lack of a nitro group.
Chembiochem 5: 1270-4 (2004)
Laboratorium FÜR Organische Chemie
Inhibition of Golgi mannosidase II with mannostatin A analogues: synthesis, biological evaluation, and structure-activity relationship studies.
Chembiochem 5: 1220-7 (2004)
University Of Georgia
Transport characteristics of fexofenadine in the Caco-2 cell model.
Pharm Res 21: 1398-404 (2004)
Uppsala University
Non-peptide oxytocin agonists.
Bioorg Med Chem Lett 14: 4585-9 (2004)
Ferring Research
SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease.
Bioorg Med Chem Lett 14: 4575-9 (2004)
Merck Research Laboratories
Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors.
Bioorg Med Chem Lett 14: 4569-73 (2004)
Virginia Commonwealth University
Carbonic anhydrase inhibitors. Inhibition of the beta-class enzyme from the methanoarchaeon Methanobacterium thermoautotrophicum (Cab) with anions.
Bioorg Med Chem Lett 14: 4563-7 (2004)
Universit£
Discovery of new chemical leads for prostaglandin D2 receptor antagonists.
Bioorg Med Chem Lett 14: 4557-62 (2004)
Minase Research Institute
Design, synthesis, and biochemical evaluation of novel alpha V beta 3 integrin ligands.
Bioorg Med Chem Lett 14: 4553-5 (2004)
3-Dimensional Pharmaceuticals
Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporin A derivatives.
Bioorg Med Chem Lett 14: 4549-51 (2004)
Guilford Pharmaceuticals
Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase.
Bioorg Med Chem Lett 14: 4539-44 (2004)
Merck Research Laboratory
AL-12182, a novel 11-oxa prostaglandin analog with topical ocular hypotensive activity in the monkey.
Bioorg Med Chem Lett 14: 4525-8 (2004)
Alcon Research
Substituted 6-phenyl-pyridin-2-ylamines: selective and potent inhibitors of neuronal nitric oxide synthase.
Bioorg Med Chem Lett 14: 4511-4 (2004)
Pfizer
Isoindolinone ureas: a novel class of KDR kinase inhibitors.
Bioorg Med Chem Lett 14: 4505-9 (2004)
Abbott Laboratories
The purine transferase from Trypanosoma cruzi as a potential target for bisphosphonate-based chemotherapeutic compounds.
Bioorg Med Chem Lett 14: 4501-4 (2004)
Universidad De Buenos Aires
Ligand conformation has a definitive effect on 5-HT1A and serotonin reuptake affinity.
Bioorg Med Chem Lett 14: 4467-70 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents.
Bioorg Med Chem Lett 14: 4461-5 (2004)
Korea Research Institute Of Chemical Technology
Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors.
Bioorg Med Chem Lett 14: 4453-9 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors.
Bioorg Med Chem Lett 14: 4449-52 (2004)
Biovitrum
Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target.
Bioorg Med Chem Lett 14: 4445-8 (2004)
Biovitrum
Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 14: 4417-23 (2004)
Neurocrine Biosciences
Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone.
Bioorg Med Chem Lett 14: 4411-5 (2004)
Merck Research Laboratories
Identification of CJC-1131-albumin bioconjugate as a stable and bioactive GLP-1(7-36) analog.
Bioorg Med Chem Lett 14: 4395-8 (2004)
Conjuchem
Synthesis, receptor binding and functional studies of mesoridazine stereoisomers.
Bioorg Med Chem Lett 14: 4379-82 (2004)
Brigham & Women'S Hospital
Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.
Bioorg Med Chem Lett 14: 4375-8 (2004)
Glaxosmithkline
Heterologous expression of human {alpha}6{beta}4{beta}3{alpha}5 nicotinic acetylcholine receptors: binding properties consistent with their natural expression require quaternary subunit assembly including the {alpha}5 subunit.
J Pharmacol Exp Ther 312: 619-26 (2005)
Targacept
Development of the first ultra-potent "capsaicinoid" agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential.
J Pharmacol Exp Ther 312: 561-70 (2005)
University Of Piemonte Orientale
Crystal structure of avian aminoimidazole-4-carboxamide ribonucleotide transformylase in complex with a novel non-folate inhibitor identified by virtual ligand screening.
J Biol Chem 279: 50555-65 (2004)
The Scripps Research Institute
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.
Bioorg Med Chem Lett 14: 5007-11 (2004)
Eli Lilly
Estrone formate: a novel type of irreversible inhibitor of human steroid sulfatase.
Bioorg Med Chem Lett 14: 4999-5002 (2004)
Novartis Institutes For Biomedical Research Gdc
Synthesis of acyloxymethyl ester prodrugs of the transferable protein farnesyl transferase substrate farnesyl methylenediphosphonate.
Bioorg Med Chem Lett 14: 4979-82 (2004)
University Of Kentucky
Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5.
Bioorg Med Chem Lett 14: 4967-73 (2004)
Neurocrine Biosciences
The development of new bicyclic pyrazole-based cytokine synthesis inhibitors.
Bioorg Med Chem Lett 14: 4945-8 (2004)
Procter And Gamble Pharmaceuticals
Synthesis and evaluation of novel oxazoline MMP inhibitors.
Bioorg Med Chem Lett 14: 4935-9 (2004)
North Dakota State University
7-Substituted 2-phenyl-benzofurans as ER beta selective ligands.
Bioorg Med Chem Lett 14: 4925-9 (2004)
Wyeth Research
The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors.
Bioorg Med Chem Lett 14: 4915-8 (2004)
Athersys
A new class of acyclic 2-alkyl-1,2-diaryl (E)-olefins as selective cyclooxygenase-2 (COX-2) inhibitors.
Bioorg Med Chem Lett 14: 4911-4 (2004)
University Of Alberta
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.
Bioorg Med Chem Lett 14: 4903-6 (2004)
University Of Virginia
Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.
Bioorg Med Chem Lett 14: 4897-902 (2004)
Glaxosmithkline
Discovery of orally active prostaglandin D2 receptor antagonists.
Bioorg Med Chem Lett 14: 4891-5 (2004)
Minase Research Institute
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3.
Bioorg Med Chem Lett 14: 4883-6 (2004)
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.
Bioorg Med Chem Lett 14: 4879-82 (2004)
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.
Bioorg Med Chem Lett 14: 4873-7 (2004)
Abbott Laboratories
Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor.
Bioorg Med Chem Lett 14: 4867-72 (2004)
In Vivo Sciences Millennium Pharmaceuticals
Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Bioorg Med Chem Lett 14: 4861-6 (2004)
Merck Research Laboratories
Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.
Bioorg Med Chem Lett 14: 4851-4 (2004)
Ewha Womans University
N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists.
Bioorg Med Chem Lett 14: 4847-50 (2004)
Nps Pharmaceuticals
Modeling the binding affinities of beta-secretase inhibitors: application to subsite specificity.
Bioorg Med Chem Lett 14: 4843-6 (2004)
Johnson & Johnson Pharmaceutical Research And Development
End-capping of the modified melanocortin tetrapeptide (p-Cl)Phe-D-Phe-Arg-Trp-NH2 as a route to hMC4R agonists.
Bioorg Med Chem Lett 14: 4839-42 (2004)
University Of Cincinnati
Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists.
Bioorg Med Chem Lett 14: 4835-8 (2004)
Biogen Idec
Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles.
Bioorg Med Chem Lett 14: 4831-4 (2004)
Biogen Idec
Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation.
Bioorg Med Chem Lett 14: 4819-23 (2004)
Aventis Pharmaceuticals
Inhibition of the strand transfer step of HIV-1 integrase by non-natural dinucleotides.
Bioorg Med Chem Lett 14: 4815-7 (2004)
University Of Georgia
Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.
J Med Chem 47: 4787-98 (2004)
Neurocrine Biosciences
Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286).
J Med Chem 47: 4774-86 (2004)
Wyeth Research
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.
J Med Chem 47: 4766-73 (2004)
Cv Therapeutics
Dipeptidomimetic ketomethylene isosteres as pro-moieties for drug transport via the human intestinal di-/tripeptide transporter hPEPT1: design, synthesis, stability, and biological investigations.
J Med Chem 47: 4755-65 (2004)
University Of Tromsø
Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6h-purin-6-one and 3,7-dihydro-1h-purine-2,6-dione derivatives as corticotropin-releasing factor(1) receptor antagonists.
J Med Chem 47: 4741-54 (2004)
Pharmaceutical Research Institute
N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy.
J Med Chem 47: 4716-30 (2004)
Glaxosmithkline
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
J Med Chem 47: 4684-92 (2004)
Merck
Indolebutylamines as selective 5-HT(1A) agonists.
J Med Chem 47: 4677-83 (2004)
Merck
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
J Med Chem 47: 4645-8 (2004)
TBA
Potent and orally bioavailable non-peptide antagonists at the human bradykinin B(1) receptor based on a 2-alkylamino-5-sulfamoylbenzamide core.
J Med Chem 47: 4642-4 (2004)
TBA
Virulence regulation and quorum sensing in staphylococcal infections: competitive AgrC antagonists as quorum sensing inhibitors.
J Med Chem 47: 4633-41 (2004)
University Of Nottingham
Dysinosins B-D, inhibitors of factor VIIa and thrombin from the Australian sponge Lamellodysidea chlorea.
J Nat Prod 67: 1291-4 (2004)
Griffith University
An analysis of phakellin and oroidin structures stimulated by further study of an Agelas sponge.
J Nat Prod 67: 1256-61 (2004)
University Of California
Intrinsic and acquired forms of resistance against the anticancer ruthenium compound KP1019 [indazolium trans-[tetrachlorobis(1H-indazole)ruthenate (III)] (FFC14A).
J Pharmacol Exp Ther 312: 281-9 (2004)
Institute Of Cancer Research
Design and synthesis of substituted N-methylbenzamide analogues derived from SR 48,968 as neurokinin-2 receptor antagonists.
Bioorg Med Chem Lett 14: 4779-82 (2004)
St. John'S University
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
Bioorg Med Chem Lett 14: 4771-7 (2004)
China Pharmaceutical University
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 14: 4763-6 (2004)
Merck
Discovery of potent and selective beta-homophenylalanine based dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 14: 4759-62 (2004)
Merck
Rational design of 6-methylsulfonylindoles as selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 14: 4741-5 (2004)
Roche Palo Alto
A novel cyclic enkephalin analogue with potent opioid antagonist activity.
Bioorg Med Chem Lett 14: 4731-3 (2004)
Clinical Research Institute Of Montreal
3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase.
Bioorg Med Chem Lett 14: 4727-30 (2004)
Pfizer
Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.
Bioorg Med Chem Lett 14: 4705-10 (2004)
Novartis Horsham Research Centre
2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands.
Bioorg Med Chem Lett 14: 4697-9 (2004)
Virginia Commonwealth University
Synthesis of cinnamic acid derivatives and their inhibitory effects on LDL-oxidation, acyl-CoA:cholesterol acyltransferase-1 and -2 activity, and decrease of HDL-particle size.
Bioorg Med Chem Lett 14: 4677-81 (2004)
National Research Laboratory Of Lipid Metabolism And Atherosclerosis
Exploring QSAR with E-state index: selectivity requirements for COX-2 versus COX-1 binding of terphenyl methyl sulfones and sulfonamides.
Bioorg Med Chem Lett 14: 4665-70 (2004)
Jadavpur University
Synthesis and biological evaluation of stilbene-based pure estrogen antagonists.
Bioorg Med Chem Lett 14: 4659-63 (2004)
Universit£T Regensburg
P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.
Bioorg Med Chem Lett 14: 4651-4 (2004)
Merck Research Laboratories
Synthesis and evaluation of tacrine-E2020 hybrids as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
Bioorg Med Chem Lett 14: 4639-42 (2004)
Shanghai Institute Of Materia Medica
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives.
Bioorg Med Chem Lett 14: 4627-31 (2004)
Pfizer
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.
Bioorg Med Chem Lett 14: 4623-6 (2004)
Pfizer
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.
Bioorg Med Chem Lett 14: 4607-13 (2004)
Pfizer
Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors.
Bioorg Med Chem Lett 14: 4603-6 (2004)
Abbott Laboratories
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
Naunyn Schmiedebergs Arch Pharmacol 370: 114-23 (2004)
Vernalis Research
New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of"THIQ".
J Med Chem 47: 4613-26 (2004)
Uppsala University
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic antagonist.
J Med Chem 47: 4588-94 (2004)
Research Triangle Institute
Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists.
J Med Chem 47: 4570-87 (2004)
Taisho Pharmaceutical
Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid.
J Med Chem 47: 4559-69 (2004)
Universit£
High-resolution structures of human aldose reductase holoenzyme in complex with stereoisomers of the potent inhibitor Fidarestat: stereospecific interaction between the enzyme and a cyclic imide type inhibitor.
J Med Chem 47: 4530-7 (2004)
Monash University (Parkville Campus)
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.
J Med Chem 47: 4517-29 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
J Med Chem 47: 4494-506 (2004)
Glaxosmithkline
Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity toward the alpha2-adrenoceptor.
J Med Chem 47: 4483-93 (2004)
University Of Kansas
Modulation of binding strength in several classes of active site inhibitors of acetylcholinesterase studied by comparative binding energy analysis.
J Med Chem 47: 4471-82 (2004)
Universitat De Barcelona
Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
J Med Chem 47: 4417-26 (2004)
Abbott Laboratories
Molecular recognition in purinergic receptors. 2. Diastereoselectivity of the h-P2Y1-receptor.
J Med Chem 47: 4405-16 (2004)
Bar-Ilan University
Determinants of retinoid X receptor transcriptional antagonism.
J Med Chem 47: 4360-72 (2004)
Institute
Mechanism of the pharmacokinetic interaction between methotrexate and benzimidazoles: potential role for breast cancer resistance protein in clinical drug-drug interactions.
Cancer Res 64: 5804-11 (2004)
The Netherlands Cancer Institute
In vitro and in vivo characterization of a novel naphthylamide ATP-sensitive K+ channel opener, A-151892.
Br J Pharmacol 143: 81-90 (2004)
Abbott Laboratories
Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor.
J Med Chem 47: 4300-15 (2004)
Umr Cnrs/Ulp 7081
Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
J Med Chem 47: 4291-9 (2004)
Biogen Idec
Identification of structurally diverse growth hormone secretagogue agonists by virtual screening and structure-activity relationship analysis of 2-formylaminoacetamide derivatives.
J Med Chem 47: 4286-90 (2004)
Institute For Life Science Research
2-(1-adamantyl)-4-(thio)chromenone-6-carboxylic acids: potent reversible inhibitors of human steroid sulfatase.
J Med Chem 47: 4268-76 (2004)
Novartis Institute For Biomedical Research Vienna
Three-dimensional quantitative structure-activity relationship analysis of a set of Plasmodium falciparum dihydrofolate reductase inhibitors using a pharmacophore generation approach.
J Med Chem 47: 4258-67 (2004)
Università
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.
J Med Chem 47: 4247-57 (2004)
National Health Research Institutes
Design, synthesis, and biological evaluation of new cyclic disulfide decapeptides that inhibit the binding of AP-1 to DNA.
J Med Chem 47: 4239-46 (2004)
Toyama Chemical
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
J Med Chem 47: 4213-30 (2004)
Abbott Laboratories
Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity.
J Med Chem 47: 4202-12 (2004)
Universit£
A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells.
J Med Chem 47: 4163-5 (2004)
Virginia Commonwealth University
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.
J Med Chem 47: 4155-8 (2004)
Friedrich-Schiller-UniversitäT Jena
Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.
J Med Chem 47: 4151-4 (2004)
Fujisawa Pharmaceutical
Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site.
J Med Chem 47: 4147-50 (2004)
University Of Michigan
Prospects for inhibitors of protein tyrosine phosphatase 1B as antidiabetic drugs.
J Med Chem 47: 4142-6 (2004)
Serono Pharmaceutical Research Institute
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
J Med Chem 47: 4135-41 (2004)
Merck Research Laboratories
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
J Med Chem 47: 4118-27 (2004)
Glaxosmithkline
New crinine-type alkaloids with inhibitory effect on induction of inducible nitric oxide synthase from Crinum yemense.
J Nat Prod 67: 1119-24 (2004)
Mansoura University
Sesquiterpenes and flavonol glycosides from Zingiber aromaticum and their CYP3A4 and CYP2D6 inhibitory activities.
J Nat Prod 67: 1079-83 (2004)
Toyama Medical And Pharmaceutical University
Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists.
J Med Chem 47: 4083-8 (2004)
Neurocrine Biosciences
Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism.
J Med Chem 47: 4066-71 (2004)
University Of Cagliary
Probing the activity differences of simple and complex brominated aryl compounds against 15-soybean, 15-human, and 12-human lipoxygenase.
J Med Chem 47: 4060-5 (2004)
University Of California
Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.
J Med Chem 47: 4054-9 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor.
J Med Chem 47: 4041-53 (2004)
Iiqab (Csic)
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.
J Med Chem 47: 4032-40 (2004)
Ohio State University
Design, synthesis, and structure-activity relationship studies of 3,4,6-triphenylpyran-2-ones as selective cyclooxygenase-2 inhibitors.
J Med Chem 47: 3972-90 (2004)
University Of Alberta
A virtual screening approach to finding novel and potent antagonists at the melanin-concentrating hormone 1 receptor.
J Med Chem 47: 3962-71 (2004)
Argenta Discovery
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.
J Med Chem 47: 3934-7 (2004)
Eli Lilly
Discovery of a Subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase.
J Med Chem 47: 3931-3 (2004)
Harvard Medical School
Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.
J Med Chem 47: 3927-30 (2004)
Uppsala University
Design, synthesis, and evaluation of sugar amino acid based inhibitors of protein prenyl transferases PFT and PGGT-1.
J Med Chem 47: 3920-3 (2004)
Leiden University
Synthesis, biophysical and biological evaluation of 3,6-bis-amidoacridines with extended 9-anilino substituents as potent G-quadruplex-binding telomerase inhibitors.
Bioorg Med Chem Lett 14: 4347-51 (2004)
University Of London School Of Pharmacy
Design and synthesis of novel Cdc25A-inhibitors having phosphate group as a hydrophilic residue.
Bioorg Med Chem Lett 14: 4339-42 (2004)
The University Of Tokyo
P4 cap modified tetrapeptidyl alpha-ketoamides as potent HCV NS3 protease inhibitors.
Bioorg Med Chem Lett 14: 4333-8 (2004)
Eli Lilly
Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.
Bioorg Med Chem Lett 14: 4319-21 (2004)
Michigan State University
Synthesis and structure-activity relationships of 3,5-diarylisoxazoles and 3,5-diaryl-1,2,4-oxadiazoles, novel classes of small molecule interleukin-8 (IL-8) receptor antagonists.
Bioorg Med Chem Lett 14: 4307-11 (2004)
Johnson And Johnson Pharmaceutical Research And Development
A unidirectional crosslinking strategy for HIV-1 protease dimerization inhibitors.
Bioorg Med Chem Lett 14: 4297-300 (2004)
Purdue University
Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.
Bioorg Med Chem Lett 14: 4291-5 (2004)
Merck Frosst Centre For Therapeutic Research
Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa.
Bioorg Med Chem Lett 14: 4281-6 (2004)
Central Pharmaceutical Research Institute
Acyl-CoA: cholesterol acyltransferase inhibitory activities of fatty acid amides isolated from Mylabris phalerate Pallas.
Bioorg Med Chem Lett 14: 4277-80 (2004)
Korea Research Institute Of Bioscience And Biotechnology
Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential.
Bioorg Med Chem Lett 14: 4263-6 (2004)
Institute For Biological Research
Diaminopyrimidine and diaminopyridine 5-HT7 ligands.
Bioorg Med Chem Lett 14: 4249-52 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Aminotriazine 5-HT7 antagonists.
Bioorg Med Chem Lett 14: 4245-8 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.
Bioorg Med Chem Lett 14: 4237-40 (2004)
Cyclacel
Bis-quinolinium cyclophanes: toward a pharmacophore model for the blockade of apamin-sensitive SKCa channels in sympathetic neurons.
Bioorg Med Chem Lett 14: 4231-5 (2004)
Aristotelian University Of Thessaloniki
Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.
Bioorg Med Chem Lett 14: 4225-9 (2004)
Johnson And Johnson Pharmaceutical Research And Development
Identification of [(naphthalene-1-carbonyl)-amino]-acetic acid derivatives as nonnucleoside inhibitors of HCV NS5B RNA dependent RNA polymerase.
Bioorg Med Chem Lett 14: 4221-4 (2004)
Wyeth Research
Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.
Bioorg Med Chem Lett 14: 4217-20 (2004)
University Of Michigan
Copper dipicolinates as peptidomimetic ligands for the Src SH2 domain.
Bioorg Med Chem Lett 14: 4203-6 (2004)
Darmstadt Technical University
Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.
Bioorg Med Chem Lett 14: 4197-201 (2004)
Aventis Pharma Deutschland
Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.
Bioorg Med Chem Lett 14: 4191-5 (2004)
Aventis Pharma Deutschland
Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.
Bioorg Med Chem Lett 14: 4179-83 (2004)
Abbott Laboratories
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.
Bioorg Med Chem Lett 14: 4173-8 (2004)
Abbott Laboratories
Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators.
Bioorg Med Chem Lett 14: 4169-72 (2004)
Abbott Laboratories
Synthesis and biological evaluation of pteridine and pyrazolopyrimidine based adenosine kinase inhibitors.
Bioorg Med Chem Lett 14: 4165-8 (2004)
Abbott Laboratories
Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.
Bioorg Med Chem Lett 14: 4161-4 (2004)
Merck Research Laboratories
Benzodiazepine inhibitors of the MMPs and TACE. Part 2.
Bioorg Med Chem Lett 14: 4147-51 (2004)
Wyeth Research
Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor.
J Pharmacol Exp Ther 311: 537-46 (2004)
Neurocrine Biosciences
Fluorescence polarization assay and inhibitor design for MDM2/p53 interaction.
Anal Biochem 331: 138-46 (2004)
Schering-Plough Research Institute
Reversal of P-glycoprotein-mediated MDR by 5,7,3',4',5'-pentamethoxyflavone and SAR.
Biochem Biophys Res Commun 320: 672-9 (2004)
Chosun University
Synthesis and biological evaluation of 2-phenylpyran-4-ones: a new class of orally active cyclooxygenase-2 inhibitors.
J Med Chem 47: 3874-86 (2004)
RhôNe-Poulenc Rorer
Synthesis and biological evaluation of a new class of geldanamycin derivatives as potent inhibitors of Hsp90.
J Med Chem 47: 3865-73 (2004)
Conforma Therapeutics
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.
J Med Chem 47: 3853-64 (2004)
Abbott Laboratories
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
J Med Chem 47: 3823-42 (2004)
Wyeth Research
Novel azapeptide inhibitors of hepatitis C virus serine protease.
J Med Chem 47: 3788-99 (2004)
Boehringer Ingelheim (Canada)
Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors.
J Med Chem 47: 3730-43 (2004)
Fujisawa Pharmaceutical
N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2.
J Med Chem 47: 3710-22 (2004)
University Of Newcastle
New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.
J Med Chem 47: 3707-9 (2004)
University Of Leiden
Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists.
Bioorg Med Chem Lett 14: 4099-102 (2004)
Argenta Discovery
Synthesis and biological evaluation of the major metabolite of atomoxetine: elucidation of a partial kappa-opioid agonist effect.
Bioorg Med Chem Lett 14: 4083-5 (2004)
Johnson And Johnson Pharmaceutical
Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors.
Bioorg Med Chem Lett 14: 4075-8 (2004)
Abbott Laboratories
A novel series of 2-pyridyl-containing compounds as lysophosphatidic acid receptor antagonists: development of a nonhydrolyzable LPA3 receptor-selective antagonist.
Bioorg Med Chem Lett 14: 4069-74 (2004)
University Of Virginia
The synthesis and SAR of 2-arylsulfanyl-phenyl piperazinyl acetic acids as glyT-1 inhibitors.
Bioorg Med Chem Lett 14: 4027-30 (2004)
H. Lundbeck
Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents.
Bioorg Med Chem Lett 14: 4019-22 (2004)
Kyoto 619-0216
Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 2: Improvement of in vitro activity.
Bioorg Med Chem Lett 14: 4013-7 (2004)
Kyoto 619-0216
Quantitative structure-activity relationship analysis of a series of 2,3-diaryl benzopyran analogues as novel selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 14: 4005-11 (2004)
Devi Ahilya Vishwavidyalaya
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.
Bioorg Med Chem Lett 14: 3993-6 (2004)
Merck Research Laboratories
Aza-boronic acids as non-beta-lactam inhibitors of AmpC-beta-lactamase.
Bioorg Med Chem Lett 14: 3979-83 (2004)
Università
Rhodanine-3-acetic acid derivatives as inhibitors of fungal protein mannosyl transferase 1 (PMT1).
Bioorg Med Chem Lett 14: 3975-8 (2004)
Celltech R&D
Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-disubstituted ureas.
Bioorg Med Chem Lett 14: 3971-4 (2004)
Procyon Biopharma
Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.
Bioorg Med Chem Lett 14: 3967-70 (2004)
Schering-Plough Research Institute
Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype.
Bioorg Med Chem Lett 14: 3963-6 (2004)
University Of Erlangen-Nuremberg
Solution phase parallel synthesis and evaluation of MAPK inhibitory activities of close structural analogues of a Ras pathway modulator.
Bioorg Med Chem Lett 14: 3957-62 (2004)
Morphochem
Oxamides as novel NR2B selective NMDA receptor antagonists.
Bioorg Med Chem Lett 14: 3953-6 (2004)
Gedeon Richter
Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists.
Bioorg Med Chem Lett 14: 3943-7 (2004)
Neurocrine Biosciences
Definition of the heterocyclic pharmacophore of bacterial methionyl tRNA synthetase inhibitors: potent antibacterially active non-quinolone analogues.
Bioorg Med Chem Lett 14: 3937-41 (2004)
Glaxosmithkline
Cinnamic acid esters as potent inhibitors of fungal 17beta-hydroxysteroid dehydrogenase--a model enzyme of the short-chain dehydrogenase/reductase superfamily.
Bioorg Med Chem Lett 14: 3933-6 (2004)
University Of Ljubljana
Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors.
Bioorg Med Chem Lett 14: 3925-8 (2004)
Eli Lilly
4-Acylamino-6-arylfuro[2,3-d]pyrimidines: potent and selective glycogen synthase kinase-3 inhibitors.
Bioorg Med Chem Lett 14: 3907-11 (2004)
Tsukuba Research Laboratories
Privileged scaffolds for blocking protein-protein interactions: 1,4-disubstituted naphthalene antagonists of transcription factor complex HOX-PBX/DNA.
Bioorg Med Chem Lett 14: 3875-9 (2004)
The State University Of New York
Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor.
Bioorg Med Chem Lett 14: 3869-73 (2004)
Neurocrine Bioscience
Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains.
Bioorg Med Chem Lett 14: 3865-8 (2004)
Merck Research Laboratories
Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains.
Bioorg Med Chem Lett 14: 3861-4 (2004)
Merck Research Laboratories
Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms.
Chem Biol 11: 775-85 (2004)
Vernalis (R&D)
Isolation and structure of antagonists of chemokine receptor (CCR5).
J Nat Prod 67: 1036-8 (2004)
Merck Research Laboratories
First synthesis and determination of the absolute configuration of sulphostin, a novel inhibitor of dipeptidyl peptidase IV.
J Nat Prod 67: 999-1004 (2004)
Microbial Chemistry Research Center
New neolignans that inhibit DNA polymerase beta lyase.
J Nat Prod 67: 964-7 (2004)
Virginia Polytechnic Institute And State University
Synthesis and antibacterial activity of a novel series of potent DNA gyrase inhibitors. Pyrazole derivatives.
J Med Chem 47: 3693-6 (2004)
Dainippon Pharmaceutical
Design, synthesis, and biological evaluation of 2,4-diamino-5-methyl-6-substituted-pyrrolo[2,3-d]pyrimidines as dihydrofolate reductase inhibitors.
J Med Chem 47: 3689-92 (2004)
Duquesne University
Mechanism of inactivation of beta-lactamases by novel 6-methylidene penems elucidated using electrospray ionization mass spectrometry.
J Med Chem 47: 3674-88 (2004)
Wyeth Research
Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.
J Med Chem 47: 3642-57 (2004)
Merck Sharp And Dohme Research Laboratories
Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties.
J Med Chem 47: 3591-9 (2004)
Kobe Gakuin University
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.
J Med Chem 47: 3580-90 (2004)
Universit£
Computer-assisted design of selective imidazole inhibitors for cytochrome p450 enzymes.
J Med Chem 47: 3572-9 (2004)
University Of California
Synthesis, biological activity, and three-dimensional quantitative structure-activity relationship model for a series of benzo[c]quinolizin-3-ones, nonsteroidal inhibitors of human steroid 5alpha-reductase 1.
J Med Chem 47: 3546-60 (2004)
University Of Florence
Identification, synthesis, and characterization of new glycogen phosphorylase inhibitors binding to the allosteric AMP site.
J Med Chem 47: 3537-45 (2004)
Novo Nordisk
Identification of non-phosphate-containing small molecular weight inhibitors of the tyrosine kinase p56 Lck SH2 domain via in silico screening against the pY + 3 binding site.
J Med Chem 47: 3502-11 (2004)
University Of Maryland
Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization.
J Med Chem 47: 3491-4 (2004)
Wyeth Research
3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor.
J Med Chem 47: 3483-6 (2004)
Neurocrine Biosciences
Fragment-based drug discovery.
J Med Chem 47: 3463-82 (2004)
Sunesis Pharmaceuticals
Novel dual inhibitors of calpain and lipid peroxidation.
Bioorg Med Chem Lett 14: 3825-8 (2004)
Institut Henri Beaufour
Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.
Bioorg Med Chem Lett 14: 3799-802 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents.
Bioorg Med Chem Lett 14: 3793-7 (2004)
Cv Therapeutics
(+)-3-[2-(Benzo[b]thiophen-2-yl)-2-oxoethyl]-1-azabicyclo[2.2.2]octane as potent agonists for the alpha7 nicotinic acetylcholine receptor.
Bioorg Med Chem Lett 14: 3781-4 (2004)
Mitsubishi Pharma
Structure-activity relationships of adenosine A3 receptor ligands: new potential therapy for the treatment of glaucoma.
Bioorg Med Chem Lett 14: 3775-9 (2004)
Otsuka Pharmaceutical Factory
Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.
Bioorg Med Chem Lett 14: 3763-9 (2004)
Merck
Carbonic anhydrase inhibitors. Inhibition of cytosolic isozyme XIII with aromatic and heterocyclic sulfonamides: a novel target for the drug design.
Bioorg Med Chem Lett 14: 3757-62 (2004)
University Of Tampere
Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins.
Bioorg Med Chem Lett 14: 3753-5 (2004)
Merck Research Laboratories
Estrogen receptor ligands. Part 5: The SAR of dihydrobenzoxathiins containing modified basic side chains.
Bioorg Med Chem Lett 14: 3747-51 (2004)
Merck Research Laboratories
Structure activity studies of ring E analogues of methyllycaconitine. Part 2: Synthesis of antagonists to the alpha3beta4* nicotinic acetylcholine receptors through modifications to the ester.
Bioorg Med Chem Lett 14: 3739-42 (2004)
Ohio University
Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis.
Bioorg Med Chem Lett 14: 3727-31 (2004)
3-Dimensional Pharmaceuticals
Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R).
Bioorg Med Chem Lett 14: 3721-5 (2004)
Millennium Pharmaceuticals
Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition.
Bioorg Med Chem Lett 14: 3715-20 (2004)
Aventis Pharma Deutschland
Inhibition of monoamine oxidases by coumarin-3-acyl derivatives: biological activity and computational study.
Bioorg Med Chem Lett 14: 3697-703 (2004)
Sapienza University Of Rome
Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility.
Bioorg Med Chem Lett 14: 3669-73 (2004)
Neurocrine Biosciences
Antimitotic activity of glaupalol-related coumarins from Glaucidium palmatum.
Bioorg Med Chem Lett 14: 3665-8 (2004)
Hokkaido University
Structural variations in keto-glutamines for improved inhibition against hepatitis A virus 3C proteinase.
Bioorg Med Chem Lett 14: 3655-8 (2004)
University Of Alberta
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Bioorg Med Chem Lett 14: 3651-4 (2004)
Virginia Commonwealth University
Discovery of small molecule antagonists of TRPV1.
Bioorg Med Chem Lett 14: 3631-4 (2004)
Gsk
Synthesis of hydroxy derivatives of highly potent non-steroidal CYP 17 inhibitors as potential metabolites and evaluation of their activity by a non cellular assay using recombinant human enzyme.
J Enzyme Inhib Med Chem 19: 17-32 (2004)
Saarland University
Pharmacological characterization of human S1P4 using a novel radioligand, [4,5-3H]-dihydrosphingosine-1-phosphate.
Br J Pharmacol 142: 851-60 (2004)
Schering-Plough Research Institute
Novel pyridazino[4,3-b]indoles with dual inhibitory activity against Mycobacterium tuberculosis and monoamine oxidase.
J Med Chem 47: 3455-61 (2004)
Russian Academy Of Sciences
Selective inhibition of Trypanosoma brucei 6-phosphogluconate dehydrogenase by high-energy intermediate and transition-state analogues.
J Med Chem 47: 3427-37 (2004)
Cardiff University
Hybrids of [TSAO-T]-[foscarnet]: The first conjugate of foscarnet with a non-nucleoside reverse transcriptase inhibitor through a labile covalent ester bond.
J Med Chem 47: 3418-26 (2004)
Instituto De QuíMica MéDica (Csic)
On the function of the 14 A long internal cavity of histone deacetylase-like protein: implications for the design of histone deacetylase inhibitors.
J Med Chem 47: 3409-17 (2004)
University Of Notre Dame
Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation.
J Med Chem 47: 3388-98 (2004)
National Institute On Drug Abuse-Intramural Research Program
Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes.
J Med Chem 47: 3381-7 (2004)
Glaxosmithkline
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.
J Med Chem 47: 3367-80 (2004)
Pharmacia Italia
Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs.
J Med Chem 47: 3353-66 (2004)
Linkoping University
Pharmacological characterization of dihydromorphine, 6-acetyldihydromorphine and dihydroheroin analgesia and their differentiation from morphine.
Eur J Pharmacol 492: 123-30 (2004)
Memorial Sloan-Kettering Cancer Center
A mild, efficient and alpha-selective glycosidation by using potassium dodecatungstocobaltate trihydrate as catalyst.
Bioorg Med Chem Lett 14: 3611-4 (2004)
University Of Isfahan
SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.
Bioorg Med Chem Lett 14: 3601-5 (2004)
Novartis Institutes For Biomedical Research
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.
Bioorg Med Chem Lett 14: 3595-9 (2004)
Novartis Institutes For Biomedical Research
Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.
Bioorg Med Chem Lett 14: 3589-93 (2004)
Merck Research Laboratories
Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines.
Bioorg Med Chem Lett 14: 3585-8 (2004)
Eli Lilly
An aminomethylpyrimidine DPP-IV inhibitor with improved properties.
Bioorg Med Chem Lett 14: 3575-8 (2004)
F. Hoffmann-La Roche
Phosphonate inhibitors of antigen 85C, a crucial enzyme involved in the biosynthesis of the Mycobacterium tuberculosis cell wall.
Bioorg Med Chem Lett 14: 3559-62 (2004)
University Of Ljubljana
Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta.
Bioorg Med Chem Lett 14: 3549-53 (2004)
Bristol-Myers Squibb
Pseudodeflectusin, a novel isochroman derivative from Aspergillus pseudodeflectus a parasite of the sea weed, Sargassum fusiform, as a selective human cancer cytotoxin.
Bioorg Med Chem Lett 14: 3539-43 (2004)
Tokyo University Of Science
Synthesis and evaluation of aminophosphinic acid derivatives as inhibitors of renal dipeptidase.
Bioorg Med Chem Lett 14: 3531-3 (2004)
The Sidney Kimmel Comprehensive Cancer Center At Johns Hopkins
BMS-201620: a selective beta 3 agonist.
Bioorg Med Chem Lett 14: 3525-9 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators.
Bioorg Med Chem Lett 14: 3521-3 (2004)
Institut Henri Beaufour
Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
Bioorg Med Chem Lett 14: 3507-11 (2004)
Research Institute Of Tsinghua University
Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.
Bioorg Med Chem Lett 14: 3501-5 (2004)
Merck Research Laboratories
The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists.
Bioorg Med Chem Lett 14: 3495-9 (2004)
Merck Research Laboratories
Synthesis and anti-inflammatory effects of novel pimarane diterpenoid analogs.
Bioorg Med Chem Lett 14: 3487-90 (2004)
Seoul National University
Synthesis and biological activity of some known and putative duloxetine metabolites.
Bioorg Med Chem Lett 14: 3481-6 (2004)
Eli Lilly
Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1.
Bioorg Med Chem Lett 14: 3477-80 (2004)
Wyeth Research
Synthesis and biological evaluation of phosphonic and thiophosphoric acid derivatives of lysophosphatidic acid.
Bioorg Med Chem Lett 14: 3473-6 (2004)
Oxford University
Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors.
Bioorg Med Chem Lett 14: 3457-60 (2004)
Wyeth Research
Synthesis of S-alkyl L-homocysteine analogues of glutathione and their kinetic studies with gamma-glutamyl transpeptidase.
Bioorg Med Chem Lett 14: 3451-5 (2004)
Universit£
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.
Bioorg Med Chem Lett 14: 3441-4 (2004)
Merck Sharp & Dohme Research Laboratories
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.
Bioorg Med Chem Lett 14: 3425-9 (2004)
Glaxosmithkline
Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor.
Bioorg Med Chem Lett 14: 3419-24 (2004)
Merck Research Laboratories
Binding modes of 6,7 di-substituted 4-anilinoquinoline-3-carbonitriles to EGFR.
Bioorg Med Chem Lett 14: 3397-400 (2004)
Georgetown University
Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.
Bioorg Med Chem Lett 14: 3389-95 (2004)
Pfizer
6-Arylamino-7-chloro-quinazoline-5,8-diones as novel cytotoxic and DNA topoisomerase inhibitory agents.
Bioorg Med Chem Lett 14: 3385-8 (2004)
Ewha Womans University
3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers.
Bioorg Med Chem Lett 14: 3379-84 (2004)
Institute Of Science & Technology
Ligand-directed functional heterogeneity of histamine H1 receptors: novel dual-function ligands selectively activate and block H1-mediated phospholipase C and adenylyl cyclase signaling.
J Pharmacol Exp Ther 311: 274-81 (2004)
University Of North Carolina At Chapel Hill
Thioether metabolites of 3,4-methylenedioxyamphetamine and 3,4-methylenedioxymethamphetamine inhibit human serotonin transporter (hSERT) function and simultaneously stimulate dopamine uptake into hSERT-expressing SK-N-MC cells.
J Pharmacol Exp Ther 311: 298-306 (2004)
University Of Texas At Austin
Involvement of multispecific organic anion transporter, Oatp14 (Slc21a14), in the transport of thyroxine across the blood-brain barrier.
Endocrinology 145: 4384-91 (2004)
The University Of Tokyo
A new ursane triterpene from Monochaetum vulcanicum that inhibits DNA polymerase beta lyase.
J Nat Prod 67: 899-901 (2004)
Virginia Polytechnic Institute And State University
Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.
J Nat Prod 67: 872-4 (2004)
Merck Research Laboratories
Glycosidase-inhibiting pyrrolidines and pyrrolizidines with a long side chain in Scilla peruviana.
J Nat Prod 67: 846-50 (2004)
Hokuriku University
A new antimalarial quassinoid from Simaba orinocensis.
J Nat Prod 67: 772-7 (2004)
University Of Mississippi
Molecular-targeted antitumor agents: the Saururus cernuus dineolignans manassantin B and 4-O-demethylmanassantin B are potent inhibitors of hypoxia-activated HIF-1.
J Nat Prod 67: 767-71 (2004)
University Of Mississippi
2-aminopyridines as highly selective inducible nitric oxide synthase inhibitors. Differential binding modes dependent on nitrogen substitution.
J Med Chem 47: 3320-3 (2004)
Astrazeneca R&D Charnwood
Design, synthesis, and structure-activity relationships of haloenol lactones: site-directed and isozyme-selective glutathione S-transferase inhibitors.
J Med Chem 47: 3282-94 (2004)
Chinese Academy Of Sciences
Targeting the polyamine pathway with transition-state analogue inhibitors of 5'-methylthioadenosine phosphorylase.
J Med Chem 47: 3275-81 (2004)
Industrial Research
Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain.
J Med Chem 47: 3264-74 (2004)
University College London
(2R)-2-ethylchromane-2-carboxylic acids: discovery of novel PPARalpha/gamma dual agonists as antihyperglycemic and hypolipidemic agents.
J Med Chem 47: 3255-63 (2004)
Merck Research Laboratories
Conformationally constrained analogues of diacylglycerol. 21. A solid-phase method of synthesis of diacylglycerol lactones as a prelude to a combinatorial approach for the synthesis of protein kinase C isozyme-specific ligands.
J Med Chem 47: 3248-54 (2004)
National Cancer Institute At Frederick
Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime.
J Med Chem 47: 3242-7 (2004)
University Of Innsbruck
Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis.
J Med Chem 47: 3236-41 (2004)
Vanderbilt University School Of Medicine
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
J Med Chem 47: 3220-35 (2004)
Abbott Laboratories
Synthesis and structure-activity relationships of parasiticidal thiosemicarbazone cysteine protease inhibitors against Plasmodium falciparum, Trypanosoma brucei, and Trypanosoma cruzi.
J Med Chem 47: 3212-9 (2004)
University Of California San Francisco
Conformationally constrained peptide analogues of pTyr-Glu-Glu-Ile as inhibitors of the Src SH2 domain binding.
J Med Chem 47: 3131-41 (2004)
University Of Rhode Island
Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: an approach for inhibiting protein-protein interactions.
J Med Chem 47: 3111-30 (2004)
Sunesis Pharmaceuticals
New series of morpholine and 1,4-oxazepane derivatives as dopamine D4 receptor ligands: synthesis and 3D-QSAR model.
J Med Chem 47: 3089-104 (2004)
Neurosearch
Characterization of a ligand-receptor binding event using receptor-dependent four-dimensional quantitative structure-activity relationship analysis.
J Med Chem 47: 3075-88 (2004)
The University Of Illinois At Chicago
A molecular basis for the selectivity of thiadiazole urea inhibitors with stromelysin-1 and gelatinase-A from generalized born molecular dynamics simulations.
J Med Chem 47: 3065-74 (2004)
University Of California San Francisco
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
J Med Chem 47: 3019-31 (2004)
Università
Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring.
J Med Chem 47: 3009-18 (2004)
University Of Illinois At Chicago
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.
J Med Chem 47: 2995-3008 (2004)
Merck Research Laboratories
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
J Med Chem 47: 2984-94 (2004)
University Of Queensland
Sultam hydroxamates as novel matrix metalloproteinase inhibitors.
J Med Chem 47: 2981-3 (2004)
Bristol-Myers Squibb
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
J Med Chem 47: 2973-6 (2004)
Sri International
A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers.
J Med Chem 47: 2969-72 (2004)
University Of Minnesota
High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter.
Mol Pharmacol 65: 1485-95 (2004)
Membrane Research Group Of The Hungarian Academy Of Sciences
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
Bioorg Med Chem Lett 14: 3351-5 (2004)
Merck Research Laboratories
N2-benzyl-N1-(1-(1-naphthyl)ethyl)-3-phenylpropane-1,2-diamines and conformationally restrained indole analogues: development of calindol as a new calcimimetic acting at the calcium sensing receptor.
Bioorg Med Chem Lett 14: 3345-9 (2004)
Upr 2301 Centre National De La Recherche Scientifique
Thiol-based SAHA analogues as potent histone deacetylase inhibitors.
Bioorg Med Chem Lett 14: 3313-7 (2004)
Nagoya City University
Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities?
Bioorg Med Chem Lett 14: 3307-12 (2004)
F. Hoffmann-La Roche
New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors.
Bioorg Med Chem Lett 14: 3303-6 (2004)
Pfizer
The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor.
Bioorg Med Chem Lett 14: 3295-8 (2004)
National Institute On Drug Abuse-Intramural Research Program
Design and synthesis of dysidiolide analogs from vitamin D3: novel class of Cdc25A inhibitors.
Bioorg Med Chem Lett 14: 3291-4 (2004)
The University Of Tokyo
Carbonic anhydrase inhibitors: the first QSAR study on inhibition of tumor-associated isoenzyme IX with aromatic and heterocyclic sulfonamides.
Bioorg Med Chem Lett 14: 3283-90 (2004)
Laxmi Fumigation And Pest Control (P)
Long chain amines and long chain ammonium salts as novel inhibitors of dynamin GTPase activity.
Bioorg Med Chem Lett 14: 3275-8 (2004)
The University Of Newcastle
2,3-Dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid derivatives: a novel class of small molecule heparanase inhibitors.
Bioorg Med Chem Lett 14: 3269-73 (2004)
Celltech R&D
A novel 18 beta-glycyrrhetinic acid analogue as a potent and selective inhibitor of 11 beta-hydroxysteroid dehydrogenase 2.
Bioorg Med Chem Lett 14: 3263-7 (2004)
University Of Bath
The monoethyl ester of meconic acid is an active site inhibitor of HCV NS5B RNA-dependent RNA polymerase.
Bioorg Med Chem Lett 14: 3257-61 (2004)
Mrl Rome
Novel thrombin inhibitors incorporating weakly basic heterobicyclic P1-arginine mimetics: optimization via modification of P1 and P3 moieties.
Bioorg Med Chem Lett 14: 3251-6 (2004)
University Of Ljubljana
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.
Bioorg Med Chem Lett 14: 3245-50 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists.
Bioorg Med Chem Lett 14: 3235-40 (2004)
Pfizer
Synthesis and CB1 receptor activities of novel arachidonyl alcohol derivatives.
Bioorg Med Chem Lett 14: 3231-4 (2004)
University Of Kuopio
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.
Bioorg Med Chem Lett 14: 3227-30 (2004)
Pfizer
Critical structural motif for the catalytic inhibition of human topoisomerase II by UK-1 and analogs.
Bioorg Med Chem Lett 14: 3221-6 (2004)
University Of Maryland
1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors.
Bioorg Med Chem Lett 14: 3217-20 (2004)
Eli Lilly
Development of l-3-aminotyrosine suitably protected for the synthesis of a novel nonphosphorylated hexapeptide with low-nanomolar Grb2-SH2 domain-binding affinity.
Bioorg Med Chem Lett 14: 3205-8 (2004)
Institute Of Materia Medica
Benzimidazoles as new potent and selective DP antagonists for the treatment of allergic rhinitis.
Bioorg Med Chem Lett 14: 3195-9 (2004)
Merck Frosst Centre For Therapeutic Research
High-throughput identification of fucosyltransferase inhibitors using carbohydrate microarrays.
Bioorg Med Chem Lett 14: 3185-8 (2004)
The Scripps Research Institute
Design and synthesis of beta-amino-alpha-hydroxy amide derivatives as inhibitors of MetAP2 and HUVEC growth.
Bioorg Med Chem Lett 14: 3181-4 (2004)
Celera
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
Bioorg Med Chem Lett 14: 3173-6 (2004)
Fudan University
In vitro SAR of (5-(2H)-isoxazolonyl) ureas, potent inhibitors of hormone-sensitive lipase.
Bioorg Med Chem Lett 14: 3155-9 (2004)
Bayer Research Center
Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists.
Bioorg Med Chem Lett 14: 3143-6 (2004)
Johnson And Johnson Pharmaceutical Research And Development
2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents.
Bioorg Med Chem Lett 14: 3135-8 (2004)
University Of Bath
Novel nonpeptidic inhibitors of HIV-1 protease obtained via a new multicomponent chemistry strategy.
Bioorg Med Chem Lett 14: 3121-5 (2004)
Morphochem
Synthesis and activity of phosphinic tripeptide inhibitors of cathepsin C.
Bioorg Med Chem Lett 14: 3113-6 (2004)
Wroclaw University Of Technology
Human ACAT-1 and -2 inhibitory activities of saucerneol B, manassantin A and B isolated from Saururus chinensis.
Bioorg Med Chem Lett 14: 3109-12 (2004)
Korea Research Institute Of Bioscience And Biotechnology
SAR study of a subtype selective allosteric potentiator of metabotropic glutamate 2 receptor, N-(4-phenoxyphenyl)-N-(3-pyridinylmethyl)ethanesulfonamide.
Bioorg Med Chem Lett 14: 3099-102 (2004)
Eli Lilly
Molecular modeling studies on the active binding site of the blood-brain barrier choline transporter.
Bioorg Med Chem Lett 14: 3085-92 (2004)
Texas Tech University Health Sciences Center
A TOPS-MODE approach to predict adenosine kinase inhibition.
Bioorg Med Chem Lett 14: 3077-9 (2004)
Vigo University
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.
Bioorg Med Chem Lett 14: 3073-5 (2004)
Pfizer
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.
Bioorg Med Chem Lett 14: 3063-8 (2004)
Abbott Laboratories
Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors.
Bioorg Med Chem Lett 14: 3057-61 (2004)
Eli Lilly
N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1.
Bioorg Med Chem Lett 14: 3053-6 (2004)
Johnson & Johnson Pharmaceutical Research And Development
A novel series of potent and selective small molecule inhibitors of the complement component C1s.
Bioorg Med Chem Lett 14: 3043-7 (2004)
3-Dimensional Pharmaceuticals
Identification and optimization of novel partial agonists of neuromedin B receptor using parallel synthesis.
Bioorg Med Chem Lett 14: 3037-42 (2004)
Tularik
Crystal structure of human phosphodiesterase 3B: atomic basis for substrate and inhibitor specificity.
Biochemistry 43: 6091-100 (2004)
Merck Research Laboratories
Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin System.
J Pharmacol Exp Ther 311: 204-12 (2004)
Actelion Pharmaceuticals
3-[2-cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): a novel cannabinoid Cb1/Cb2 receptor partial agonist with antihyperalgesic and antiallodynic effects.
J Pharmacol Exp Ther 310: 620-32 (2004)
Bayer Healthcare
Discovery of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif.
J Med Chem 47: 2939-42 (2004)
Instituto De Qu£Mica M£Dica
Gamma-amino-substituted analogues of 1-[(S)-2,4-diaminobutanoyl]piperidine as highly potent and selective dipeptidyl peptidase II inhibitors.
J Med Chem 47: 2906-16 (2004)
University Of Antwerp
Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents.
J Med Chem 47: 2897-905 (2004)
National Health Research Institutes
Discovery of the first non-peptide full agonists for the human bradykinin B(2) receptor incorporating 4-(2-picolyloxy)quinoline and 1-(2-picolyl)benzimidazole frameworks.
J Med Chem 47: 2853-63 (2004)
Fujisawa Pharmaceutical
Interaction of cycloSal-pronucleotides with cholinesterases from different origins. A structure-activity relationship.
J Med Chem 47: 2839-52 (2004)
University Of Hamburg
1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.
J Med Chem 47: 2833-8 (2004)
Novo Nordisk
Carbamoylphosphonates, a new class of in vivo active matrix metalloproteinase inhibitors. 1. Alkyl- and cycloalkylcarbamoylphosphonic acids.
J Med Chem 47: 2826-32 (2004)
The Hebrew University Of Jerusalem
Incorporating molecular shape into the alignment-free Grid-Independent Descriptors.
J Med Chem 47: 2805-15 (2004)
Universitat Pompeu Fabra
Carbonic anhydrase inhibitors: synthesis and topical intraocular pressure lowering effects of fluorine-containing inhibitors devoid of enhanced reactivity.
J Med Chem 47: 2796-804 (2004)
Universit£
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.
J Med Chem 47: 2776-95 (2004)
Actelion Pharmaceuticals
BREED: Generating novel inhibitors through hybridization of known ligands. Application to CDK2, p38, and HIV protease.
J Med Chem 47: 2768-75 (2004)
Vertex Pharmaceuticals
Receptor flexibility in the in silico screening of reagents in the S1' pocket of human collagenase.
J Med Chem 47: 2761-7 (2004)
De Novo Pharmaceuticals
Chemical function based pharmacophore generation of endothelin-A selective receptor antagonists.
J Med Chem 47: 2750-60 (2004)
University Of Innsbruck
Comparative molecular active site analysis (CoMASA). 1. An approach to rapid evaluation of 3D QSAR.
J Med Chem 47: 2732-42 (2004)
Nippon Zoki Pharmaceutical
Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors.
J Med Chem 47: 2728-31 (2004)
Fujisawa Pharmaceutical
Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-alpha production.
J Med Chem 47: 2724-7 (2004)
Procter And Gamble Pharmaceuticals
Vanilloid receptor TRPV1 antagonists as the next generation of painkillers. Are we putting the cart before the horse?
J Med Chem 47: 2717-23 (2004)
Hospital Of The University Of Pennsylvania
SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.
J Pharmacol Exp Ther 310: 905-14 (2004)
Sanofi-Synthelabo Recherche
Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists.
Bioorg Med Chem Lett 14: 2987-9 (2004)
Johnson And Johnson Pharmaceutical Research And Development
Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.
Bioorg Med Chem Lett 14: 2973-7 (2004)
Bristol-Myers Squibb
Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C.
Bioorg Med Chem Lett 14: 2963-7 (2004)
Tohoku University
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
Bioorg Med Chem Lett 14: 2955-8 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis, and characterization of an ATP-peptide conjugate inhibitor of protein kinase A.
Bioorg Med Chem Lett 14: 2951-4 (2004)
Johns Hopkins University School Of Medicine
Synergetic inhibition of genistein and D-glucose on alpha-glucosidase.
Bioorg Med Chem Lett 14: 2947-50 (2004)
Sun Yat-Sen (Zhongshan) University
The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase.
Bioorg Med Chem Lett 14: 2941-5 (2004)
Merck Research Laboratories
Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives.
Bioorg Med Chem Lett 14: 2935-9 (2004)
Daiichi Pharmaceutical
Plasmepsin II inhibition and antiplasmodial activity of Primaquine-Statine 'double-drugs'.
Bioorg Med Chem Lett 14: 2931-4 (2004)
University Of Milan
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha2-adrenoceptor antagonistic activities. Part 2: Further exploration on the cinnamyl moiety.
Bioorg Med Chem Lett 14: 2917-22 (2004)
Janssen-Cilag
N-Aryl-gamma-lactams as integrin alphavbeta3 antagonists.
Bioorg Med Chem Lett 14: 2905-9 (2004)
Amgen
Reverse hydroxamate-based selective TACE inhibitors.
Bioorg Med Chem Lett 14: 2897-900 (2004)
Kaken Pharmaceutical
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
Bioorg Med Chem Lett 14: 2871-5 (2004)
Merck
Design, synthesis and structure-activity relationship studies of novel indazole analogues as DNA gyrase inhibitors with Gram-positive antibacterial activity.
Bioorg Med Chem Lett 14: 2857-62 (2004)
Dainippon Pharmaceutical
Silanediol peptidomimetics. Evaluation of four diastereomeric ACE inhibitors.
Bioorg Med Chem Lett 14: 2853-6 (2004)
State University Of New York
PDE2 inhibition by the PI3 kinase inhibitor LY294002 and analogues.
Bioorg Med Chem Lett 14: 2847-51 (2004)
Monash University
Solid-phase synthesis of kojic acid-tripeptides and their tyrosinase inhibitory activity, storage stability, and toxicity.
Bioorg Med Chem Lett 14: 2843-6 (2004)
Seoul National University
Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel.
Bioorg Med Chem Lett 14: 2823-7 (2004)
Aventis Pharma Deutschland
Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand.
Bioorg Med Chem Lett 14: 2801-5 (2004)
Aventis Pharma Deutschland
2,4-Bis(octadecanoylamino)benzenesulfonic acid sodium salt as a novel scavenger receptor inhibitor with low molecular weight.
Bioorg Med Chem Lett 14: 2791-5 (2004)
Organon K.K.
Synthesis and structure-activity relationship of 2-(aminoalkyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives: a novel series of 5-HT(2A/2C) receptor antagonists.
Bioorg Med Chem Lett 14: 2765-71 (2004)
Janssen-Cilag
Design and synthesis of benzofused heterocyclic RXR modulators.
Bioorg Med Chem Lett 14: 2759-63 (2004)
Eli Lilly
Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.
Bioorg Med Chem Lett 14: 2747-52 (2004)
Johnson & Johnson Pharmaceutical Research & Development
Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.
Bioorg Med Chem Lett 14: 2741-5 (2004)
Merck Research Laboratories
Initial structure-activity relationships of lysophosphatidic acid receptor antagonists: discovery of a high-affinity LPA1/LPA3 receptor antagonist.
Bioorg Med Chem Lett 14: 2735-40 (2004)
University Of Virginia
Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists.
Bioorg Med Chem Lett 14: 2729-33 (2004)
Pfizer
Synthesis and target identification of hymenialdisine analogs.
Chem Biol 11: 247-59 (2004)
Genomics Institute Of The Novartis Research Foundation
Systems-based design of bi-ligand inhibitors of oxidoreductases: filling the chemical proteomic toolbox.
Chem Biol 11: 185-94 (2004)
Triad Therapeutics
Structural determinants of CDK4 inhibition and design of selective ATP competitive inhibitors.
Chem Biol 11: 525-34 (2004)
Cyclacel
Lobeline analogs with enhanced affinity and selectivity for plasmalemma and vesicular monoamine transporters.
J Pharmacol Exp Ther 310: 1035-45 (2004)
University Of Kentucky
Identification and activity of a series of azole-based compounds with lactate dehydrogenase-directed anti-malarial activity.
J Biol Chem 279: 31429-39 (2004)
University Of Bristol
[1-(3,5-difluoro-4-hydroxyphenyl)-1H-pyrrol-3-yl]phenylmethanone as a bioisostere of a carboxylic acid aldose reductase inhibitor.
J Med Chem 47: 2706-9 (2004)
Aristotle University Of Thessaloniki
4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.
J Med Chem 47: 2678-87 (2004)
Freie UniversitäT Berlin
A new class of nonpeptide bradykinin B(2) receptor ligand, incorporating a 4-aminoquinoline framework. Identification of a key pharmacophore to determine species difference and agonist/antagonist profile.
J Med Chem 47: 2667-77 (2004)
Fujisawa Pharmaceutical
New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation.
J Med Chem 47: 2659-66 (2004)
Collegium Medicum Of The Jagiellonian University
Inhibitors of Sir2: evaluation of splitomicin analogues.
J Med Chem 47: 2635-44 (2004)
Fred Hutchinson Cancer Research Center
Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters.
J Med Chem 47: 2624-34 (2004)
National Institute Of Diabetes And Digestive And Kidney Diseases
Oral bioavailability of a new class of micro-opioid receptor agonists containing 3,6-bis[Dmt-NH(CH(2))(n)]-2(1H)-pyrazinone with central-mediated analgesia.
J Med Chem 47: 2599-610 (2004)
National Institutes Of Environmental Health Sciences
Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors.
J Med Chem 47: 2587-98 (2004)
Pharmaceutical Research Institute
Design, synthesis, structural studies, biological evaluation, and computational simulations of novel potent AT(1) angiotensin II receptor antagonists based on the 4-phenylquinoline structure.
J Med Chem 47: 2574-86 (2004)
Università
Rational design and synthesis of novel dimeric diketoacid-containing inhibitors of HIV-1 integrase: implication for binding to two metal ions on the active site of integrase.
J Med Chem 47: 2561-73 (2004)
Institute Of Materia Medica
General model for estimation of the inhibition of protein kinases using Monte Carlo simulations.
J Med Chem 47: 2534-49 (2004)
Yale University
Non-peptidic small-molecule inhibitors of the single-chain hepatitis C virus NS3 protease/NS4A cofactor complex discovered by structure-based NMR screening.
J Med Chem 47: 2486-98 (2004)
Schering-Plough Research Institute
Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase.
J Med Chem 47: 2475-85 (2004)
Harvard Medical School
Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis.
J Med Chem 47: 2466-74 (2004)
Merck Research Laboratories
5-substituted derivatives of 6-halogeno-3-((2-(S)-azetidinyl)methoxy)pyridine and 6-halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridine with low picomolar affinity for alpha4beta2 nicotinic acetylcholine receptor and wide range of lipophilicity: potential probes for imaging with positron emission tomog
J Med Chem 47: 2453-65 (2004)
National Institute On Drug Abuse
Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.
J Med Chem 47: 2441-52 (2004)
Merck Research Laboratories
Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database.
J Med Chem 47: 2430-40 (2004)
University Of Michigan Comprehensive Cancer Center
N-phenylphenylglycines as novel corticotropin releasing factor receptor antagonists.
J Med Chem 47: 2426-9 (2004)
Bristol-Myers Squibb Pharma Research Laboratories
Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists.
J Med Chem 47: 2422-5 (2004)
Eli Lilly
Discovery of diarylacrylonitriles as a novel series of small molecule sortase A inhibitors.
J Med Chem 47: 2418-21 (2004)
Seoul National University
Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.
J Med Chem 47: 2411-3 (2004)
University Of Antwerp
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagoni
J Med Chem 47: 2405-8 (2004)
Schering-Plough Research Institute
Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.
Bioorg Med Chem Lett 14: 2685-91 (2004)
Idun Pharmaceuticals
Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 4.
Bioorg Med Chem Lett 14: 2653-6 (2004)
Eli Lilly
Three new cyclostellettamines, which inhibit histone deacetylase, from a marine sponge of the genus Xestospongia.
Bioorg Med Chem Lett 14: 2617-20 (2004)
The University Of Tokyo
A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.
Bioorg Med Chem Lett 14: 2613-6 (2004)
Abbott Bioresearch Center
Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor.
Bioorg Med Chem Lett 14: 2603-7 (2004)
Wyeth Research
S-(2-(acylamino)phenyl) 2,2-dimethylpropanethioates as CETP inhibitors.
Bioorg Med Chem Lett 14: 2589-91 (2004)
Central Pharmaceutical Research Institute
Synthesis of 1alpha,25-dihydroxyvitamin D3-26,23-lactams (DLAMs), a novel series of 1 alpha,25-dihydroxyvitamin D3 antagonist.
Bioorg Med Chem Lett 14: 2579-83 (2004)
University Of Tokyo
Discovery of a potent and selective alpha v beta 3 integrin antagonist with strong inhibitory activity against neointima formation in rat balloon injury model.
Bioorg Med Chem Lett 14: 2567-70 (2004)
Dainippon Pharmaceutical
Simple aromatic compounds containing propenone moiety show considerable dual COX/5-LOX inhibitory activities.
Bioorg Med Chem Lett 14: 2559-62 (2004)
Yeungnam University
Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.
Bioorg Med Chem Lett 14: 2551-4 (2004)
Merck Research Laboratories
Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K.
Bioorg Med Chem Lett 14: 2543-6 (2004)
Glaxosmithkline
Rational design and synthesis of novel heparan sulfate mimetic compounds as antiadhesive agents.
Bioorg Med Chem Lett 14: 2505-9 (2004)
Riken Discovery Research Institute
Design and synthesis of bridged gamma-lactams as analogues of beta-lactam antibiotics.
Bioorg Med Chem Lett 14: 2489-92 (2004)
Aventis Pharma
Statin-derived 1,3-oxazinan-2-ones as submicromolar inhibitors of LFA-1/ICAM-1 interaction: stabilization of the metabolically labile vanillyl side chain.
Bioorg Med Chem Lett 14: 2483-7 (2004)
Novartis Institutes For Biomedical Research
Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides.
Bioorg Med Chem Lett 14: 2477-81 (2004)
University College London
Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity.
Bioorg Med Chem Lett 14: 2473-6 (2004)
Cnrs Umr 8076
SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.
Bioorg Med Chem Lett 14: 2469-72 (2004)
Eli Lilly
Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the alpha 2 delta-1 subunit of voltage gated calcium channel.
Bioorg Med Chem Lett 14: 2463-7 (2004)
Merck Research Laboratories
Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists.
Bioorg Med Chem Lett 14: 2451-7 (2004)
Novartis Pharma
Facile synthesis of fused 1,2,4-triazolo[1,5-c]pyrimidine derivatives as human adenosine A3 receptor ligands.
Bioorg Med Chem Lett 14: 2443-6 (2004)
Otsuka Pharmaceutical Factory
Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors.
Bioorg Med Chem Lett 14: 2433-7 (2004)
University Of Newcastle
Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand.
Bioorg Med Chem Lett 14: 2427-31 (2004)
Institute Of Technology
Different regulation of human delta-opioid receptors by SNC-80 [(+)-4-[(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide] and endogenous enkephalins.
J Pharmacol Exp Ther 310: 666-77 (2004)
Laboratoire De Biochimie A
Development of bombesin analogs with conformationally restricted amino acid substitutions with enhanced selectivity for the orphan receptor human bombesin receptor subtype 3.
J Pharmacol Exp Ther 310: 1161-70 (2004)
National Institutes Of Health
Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist.
J Pharmacol Exp Ther 310: 943-51 (2004)
Acadia Pharmaceuticals
Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4.
J Med Chem 47: 2375-88 (2004)
Medical College Of Ohio
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
J Med Chem 47: 2348-55 (2004)
Abbott Laboratories
Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX.
J Med Chem 47: 2337-47 (2004)
Canadian Institutes Of Health Research
Khellinone derivatives as blockers of the voltage-gated potassium channel Kv1.3: synthesis and immunosuppressive activity.
J Med Chem 47: 2326-36 (2004)
Institute Of Medical Research Biotechnology Centre
4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity.
J Med Chem 47: 2308-17 (2004)
Università
Structure-activity relationship of purine ribonucleosides for inhibition of hepatitis C virus RNA-dependent RNA polymerase.
J Med Chem 47: 2283-95 (2004)
Isis Pharmaceuticals
Heterocyclic bis-cations as starting hits for design of inhibitors of the bifunctional enzyme histidine-containing protein kinase/phosphatase from Bacillus subtilis.
J Med Chem 47: 2264-75 (2004)
University Of Strasburg
Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique adenosine derivative.
J Med Chem 47: 2243-55 (2004)
University Of Bonn
Development of a new radioligand, N-(5-fluoro-2-phenoxyphenyl)-N-(2-[18F]fluoroethyl-5-methoxybenzyl)acetamide, for pet imaging of peripheral benzodiazepine receptor in primate brain.
J Med Chem 47: 2228-35 (2004)
National Institute Of Radiological Sciences
Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
J Med Chem 47: 2194-207 (2004)
University Of Florida
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.
J Med Chem 47: 2180-93 (2004)
Nitromed
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
J Med Chem 47: 2176-9 (2004)
Merck Sharp And Dohme Research Laboratories
Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators.
J Med Chem 47: 2171-5 (2004)
Merck Research Laboratories
Inhibition of fucosyltransferase VII by gallic acid and its derivatives.
Arch Biochem Biophys 425: 51-7 (2004)
Schering-Plough Research Institute
Indoline derivatives as 5-HT(2C) receptor agonists.
Bioorg Med Chem Lett 14: 2367-70 (2004)
Vernalis Research
Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with a topically acting antiglaucoma sulfonamide.
Bioorg Med Chem Lett 14: 2357-61 (2004)
Bruker-Axs
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered.
Bioorg Med Chem Lett 14: 2351-6 (2004)
Universit£
3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.
Bioorg Med Chem Lett 14: 2345-9 (2004)
Universita Degli Studi Di Firenze
Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4.
Bioorg Med Chem Lett 14: 2331-4 (2004)
Merck Research Laboratories
Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.
Bioorg Med Chem Lett 14: 2327-30 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Amidines as amide bond replacements in VLA-4 antagonists.
Bioorg Med Chem Lett 14: 2323-6 (2004)
Merck Research Laboratories
Synthesis, SAR, and antitumor properties of diamino-C,N-diarylpyrimidine positional isomers: inhibitors of lysophosphatidic acid acyltransferase-beta.
Bioorg Med Chem Lett 14: 2303-8 (2004)
Cell Therapeutics
Analysis of structure-activity relationships for the 'B-region' of N-(3-acyloxy-2-benzylpropyl)-N(')-[4-(methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: discovery of an N-hydroxythiourea analogue with potent analgesic activity.
Bioorg Med Chem Lett 14: 2291-7 (2004)
Seoul National University
Tight binding ligand approach to oligosaccharide-grafted protein.
Bioorg Med Chem Lett 14: 2285-9 (2004)
Jst
Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA).
Bioorg Med Chem Lett 14: 2279-83 (2004)
Virginia Commonwealth University
Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists.
Bioorg Med Chem Lett 14: 2269-74 (2004)
Neurocrine Biosciences
5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.
Bioorg Med Chem Lett 14: 2265-8 (2004)
Ucb Pharma
Novel halogenated nitrobenzylthioinosine analogs as es nucleoside transporter inhibitors.
Bioorg Med Chem Lett 14: 2257-60 (2004)
University Of Tennessee Health Sciences Center
Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors.
Bioorg Med Chem Lett 14: 2249-52 (2004)
Astrazeneca
Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors.
Bioorg Med Chem Lett 14: 2245-8 (2004)
Astrazeneca
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
Bioorg Med Chem Lett 14: 2233-9 (2004)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.
Bioorg Med Chem Lett 14: 2227-31 (2004)
The Bristol-Myers Squibb Pharmaceutical Research Institute
Application of the four-component Ugi condensation for the preparation of sulfated glycoconjugate libraries.
Bioorg Med Chem Lett 14: 2221-6 (2004)
Progen Industries
Thioxanthene-derived analogs as sigma(1) receptor ligands.
Bioorg Med Chem Lett 14: 2217-20 (2004)
Virginia Commonwealth University
Discovery of novel nonsteroidal glucocorticoid receptor modulators.
Bioorg Med Chem Lett 14: 2209-12 (2004)
Abbott Laboratories
Structure-activity relationships of novel inhibitors of glyceraldehyde-3-phosphate dehydrogenase.
Bioorg Med Chem Lett 14: 2199-204 (2004)
Universidade Federal De Minas Gerais
2,3-diarylpyran-4-ones: a new series of selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett 14: 2195-8 (2004)
Pharmaceutical & Health Research Institute
Novel pyrrole-containing progesterone receptor modulators.
Bioorg Med Chem Lett 14: 2185-9 (2004)
Wyeth Research
Novel CCR1 antagonists with improved metabolic stability.
Bioorg Med Chem Lett 14: 2175-9 (2004)
Pfizer
Potent small molecule CCR1 antagonists.
Bioorg Med Chem Lett 14: 2169-73 (2004)
Pfizer
The discovery of structurally novel CCR1 antagonists derived from a hydroxyethylene peptide isostere template.
Bioorg Med Chem Lett 14: 2163-7 (2004)
Pfizer
Synthesis and inhibition of Src kinase activity by 7-ethenyl and 7-ethynyl-4-anilino-3-quinolinecarbonitriles.
Bioorg Med Chem Lett 14: 2155-8 (2004)
Wyeth Research
Capped dipeptide phenethylamide inhibitors of the HCV NS3 protease.
Bioorg Med Chem Lett 14: 2151-4 (2004)
Irbm, Mrl Rome
Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group.
Bioorg Med Chem Lett 14: 2141-5 (2004)
Merck Research Laboratories
Didehydrofarnesyl diphosphate: an intrinsically fluorescent inhibitor of protein farnesyltransferase.
Bioorg Med Chem Lett 14: 2137-40 (2004)
The University Of Utah
Novel GSK-3 inhibitors with improved cellular activity.
Bioorg Med Chem Lett 14: 2127-30 (2004)
Glaxosmithkline
Novel pyrazolopyrimidine derivatives as GSK-3 inhibitors.
Bioorg Med Chem Lett 14: 2121-5 (2004)
Glaxosmithkline
Synthesis and monoamine transporter affinity of 3'-analogs of 2-beta-carbomethoxy-3-beta-(4'-iodophenyl)tropane (beta-CIT).
Bioorg Med Chem Lett 14: 2117-20 (2004)
Yale School Of Medicine
N-alkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, micro and delta opioid agonists: a micro address.
Bioorg Med Chem Lett 14: 2113-6 (2004)
Johnson And Johnson Pharmaceutical Research And Development
N,N-dialkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, potent, selective delta opioid agonists.
Bioorg Med Chem Lett 14: 2109-12 (2004)
Johnson And Johnson Pharmaceutical Research And Development
Synthesis and phosphodiesterase 5 inhibitory activity of new sildenafil analogues containing a phosphonate group in the 5(')-sulfonamide moiety of phenyl ring.
Bioorg Med Chem Lett 14: 2099-103 (2004)
Ewha Womans University
Synthesis of fluorinated cyclopentenyladenine as potent inhibitor of S-adenosylhomocysteine hydrolase.
Bioorg Med Chem Lett 14: 2091-3 (2004)
Ewha Womans University
Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists.
Bioorg Med Chem Lett 14: 2083-6 (2004)
Neurocrine Biosciences
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
Bioorg Med Chem Lett 14: 2079-82 (2004)
Abbott Laboratories
N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.
Bioorg Med Chem Lett 14: 2073-8 (2004)
Millennium Pharmaceuticals
N-Benzoyl amino acids as ICAM/LFA-1 inhibitors. Part 2: structure-activity relationship of the benzoyl moiety.
Bioorg Med Chem Lett 14: 2055-9 (2004)
Genentech
Biaryl amide glucagon receptor antagonists.
Bioorg Med Chem Lett 14: 2047-50 (2004)
Abbott Laboratories
The design, preparation and SAR of novel small molecule sodium (Na(+)) channel blockers.
Bioorg Med Chem Lett 14: 2025-30 (2004)
Arqule
Characterization of two novel N-methyl-D-aspartate antagonists: EAA-090 (2-[8,9-dioxo-2,6-diazabicyclo [5.2.0]non-1(7)-en2-yl]ethylphosphonic acid) and EAB-318 (R-alpha-amino-5-chloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid hydrochloride).
J Pharmacol Exp Ther 310: 563-70 (2004)
Wyeth Research
Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitro.
Cancer Res 64: 2333-7 (2004)
St. Jude Children'S Research Hospital
Macrocyclization in the design of non-phosphorus-containing Grb2 SH2 domain-binding ligands.
J Med Chem 47: 2166-9 (2004)
National Cancer Institute-Frederick
Design, synthesis, and biological activity of 1,3-disubstituted ureas as potent inhibitors of the soluble epoxide hydrolase of increased water solubility.
J Med Chem 47: 2110-22 (2004)
University Of California Davis
NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
J Med Chem 47: 2089-96 (2004)
Merck Research Laboratories
Synthesis and selective inhibitory activity of 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives against monoamine oxidase.
J Med Chem 47: 2071-4 (2004)
Sapienza University Of Rome
Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists.
J Med Chem 47: 2037-61 (2004)
Millennium Pharmaceuticals
A phenylnorstatine inhibitor binding to HIV-1 protease: geometry, protonation, and subsite-pocket interactions analyzed at atomic resolution.
J Med Chem 47: 2030-6 (2004)
Academy Of Sciences Of The Czech Republic
Structure-based design of potent retinoid X receptor alpha agonists.
J Med Chem 47: 2010-29 (2004)
Glaxosmithkline
Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.
J Med Chem 47: 1969-86 (2004)
Encysive Pharmaceuticals
Identification of compounds with nanomolar binding affinity for checkpoint kinase-1 using knowledge-based virtual screening.
J Med Chem 47: 1962-8 (2004)
Astrazeneca
Crystal structures of the vitamin D nuclear receptor liganded with the vitamin D side chain analogues calcipotriol and seocalcitol, receptor agonists of clinical importance. Insights into a structural basis for the switching of calcipotriol to a receptor antagonist by further side chain modificatio
J Med Chem 47: 1956-61 (2004)
Institute Of Genetics And Molecular And Cellular Biology (Igbmc)
Orally bioavailable competitive CCR5 antagonists.
J Med Chem 47: 1939-55 (2004)
Novartis Institutes For Biomedical Research
Azasugar-based MMP/ADAM inhibitors as antipsoriatic agents.
J Med Chem 47: 1930-8 (2004)
Hokkaido Collaboration Center N-21
Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives.
J Med Chem 47: 1919-29 (2004)
Biocryst Pharmaceuticals
Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor.
J Med Chem 47: 1900-18 (2004)
Recordati
Design and syntheses of 1,6-naphthalene derivatives as selective HCMV protease inhibitors.
J Med Chem 47: 1893-9 (2004)
Wyeth Research
Aza-peptide Michael acceptors: a new class of inhibitors specific for caspases and other clan CD cysteine proteases.
J Med Chem 47: 1889-92 (2004)
School Of Chemistry And Biochemistry And The Parker H. Petit Institute For Bioengineering And Bioscience
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
J Med Chem 47: 1886-8 (2004)
Harvard Medical School
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?
J Med Chem 47: 1869-78 (2004)
Merck Research Laboratories
DiPOA ([8-(3,3-diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic acid), a novel, systemically available, and peripherally restricted mu opioid agonist with antihyperalgesic activity: I. In vitro pharmacological characterization and pharmacokinetic properties.
J Pharmacol Exp Ther 310: 783-92 (2004)
Purdue Pharma Discovery Research
Discovery and optimization of 2-aryl oxazolo-pyrimidines as adenosine kinase inhibitors using liquid phase parallel synthesis.
Bioorg Med Chem Lett 14: 1997-2000 (2004)
Bayer
(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.
Bioorg Med Chem Lett 14: 1991-5 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Parallel synthesis of DAPT derivatives and their gamma-secretase-inhibitory activity.
Bioorg Med Chem Lett 14: 1983-5 (2004)
University Of Tokyo
Structure-activity relationships of untenone A and its derivatives for inhibition of DNA polymerases.
Bioorg Med Chem Lett 14: 1975-7 (2004)
Tokyo University Of Science
Modified norcantharidins; synthesis, protein phosphatases 1 and 2A inhibition, and anticancer activity.
Bioorg Med Chem Lett 14: 1969-73 (2004)
University Of California Irvine
1,2,3,4-tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands.
Bioorg Med Chem Lett 14: 1961-4 (2004)
Virginia Commonwealth University
Sulfonamido, azidosulfonyl and N-acetylsulfonamido analogues of rofecoxib: 4-[4-(N-acetylsulfonamido)phenyl]-3-(4-methanesulfonylphenyl)-2(5H)furanone is a potent and selective cyclooxygenase-2 inhibitor.
Bioorg Med Chem Lett 14: 1957-60 (2004)
University Of Alberta
Design of acyclic triaryl olefins: a new class of potent and selective cyclooxygenase-2 (COX-2) inhibitors.
Bioorg Med Chem Lett 14: 1953-6 (2004)
University Of Alberta
Inhibitors of hepatitis C virus NS3.4A protease. Part 3: P2 proline variants.
Bioorg Med Chem Lett 14: 1939-42 (2004)
Vertex Pharmaceuticals
Probing pockets S2-S4' of the gamma-secretase active site with (hydroxyethyl)urea peptidomimetics.
Bioorg Med Chem Lett 14: 1935-8 (2004)
Harvard Medical School
Farnesyloxycoumarins, a new class of squalene-hopene cyclase inhibitors.
Bioorg Med Chem Lett 14: 1931-4 (2004)
Università
Evans Blue and other dyes as protein tyrosine phosphatase inhibitors.
Bioorg Med Chem Lett 14: 1923-6 (2004)
Inha University
Hydroxytriamides as potent gamma-secretase inhibitors.
Bioorg Med Chem Lett 14: 1917-21 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the alpha2delta subunit of voltage gated calcium channels.
Bioorg Med Chem Lett 14: 1913-6 (2004)
Merck Research Laboratories
Potent and selective inhibitors of bacterial methionyl tRNA synthetase derived from an oxazolone-dipeptide scaffold.
Bioorg Med Chem Lett 14: 1909-11 (2004)
Arqule
Epibatidine structure-activity relationships.
Bioorg Med Chem Lett 14: 1889-96 (2004)
Research Triangle Institute
Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
Bioorg Med Chem Lett 14: 1879-87 (2004)
University Of Maryland
Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.
Bioorg Med Chem Lett 14: 1869-74 (2004)
University Of Kentucky
Subtype-selective nicotinic receptor antagonists: potential as tobacco use cessation agents.
Bioorg Med Chem Lett 14: 1863-7 (2004)
University Of Kentucky
Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.
Bioorg Med Chem Lett 14: 1855-8 (2004)
University Of Illinois At Chicago
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
Bioorg Med Chem Lett 14: 1849-53 (2004)
University Of Florida
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
Bioorg Med Chem Lett 14: 1845-8 (2004)
Georgetown University School Of Medicine
alpha4beta2 nACh receptor pharmacophore models.
Bioorg Med Chem Lett 14: 1841-4 (2004)
Virginia Commonwealth University
Inhibitor binding in a class 2 dihydroorotate dehydrogenase causes variations in the membrane-associated N-terminal domain.
Protein Sci 13: 1031-42 (2004)
University Of Copenhagen
Antityrosinase principles and constituents of the petals of Crocus sativus.
J Nat Prod 67: 437-40 (2004)
National Cheng Kung University
Effects of natural flavones and flavonols on the kinase activity of Cdk5.
J Nat Prod 67: 416-20 (2004)
University Of Chile
Iridoids as allelochemicals and DNA polymerase inhibitors.
J Nat Prod 67: 357-61 (2004)
Universidad Nacional De San Luis
Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist.
Eur J Pharmacol 487: 183-97 (2004)
Abbott Laboratories
Structure-activity study of the ORL1 antagonist Ac-Arg-D-Cha-Qaa-D-Arg-D-p-ClPhe-NH2.
J Med Chem 47: 1864-7 (2004)
Vrije Universiteit Brussel
N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.
J Med Chem 47: 1852-5 (2004)
Universit£
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
J Med Chem 47: 1807-22 (2004)
Merck Sharp And Dohme Research Laboratories
Fluorinated phenylcyclopropylamines. 1. Synthesis and effect of fluorine substitution at the cyclopropane ring on inhibition of microbial tyramine oxidase.
J Med Chem 47: 1796-806 (2004)
National Institute Of Diabetes And Digestive And Kidney Diseases
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
J Med Chem 47: 1760-6 (2004)
Emory University
Synthesis of urea-based inhibitors as active site probes of glutamate carboxypeptidase II: efficacy as analgesic agents.
J Med Chem 47: 1729-38 (2004)
University Of Illinois At Chicago
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.
J Med Chem 47: 1719-28 (2004)
Bristol-Myers Squibb
Discovery of a potent and novel motilin agonist.
J Med Chem 47: 1704-8 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Validation of molecular docking calculations involving FGF-1 and FGF-2.
J Med Chem 47: 1683-93 (2004)
Progen Industries
Synthesis and monoamine transporter binding of 2-(diarylmethoxymethyl)-3 beta-aryltropane derivatives.
J Med Chem 47: 1676-82 (2004)
University Of New Orleans
2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity.
J Med Chem 47: 1662-75 (2004)
Cyclacel
Unraveling the active conformation of urotensin II.
J Med Chem 47: 1652-61 (2004)
University Of Salerno
Countering cooperative effects in protease inhibitors using constrained beta-strand-mimicking templates in focused combinatorial libraries.
J Med Chem 47: 1641-51 (2004)
The University Of Queensland
A new series of highly potent non-peptide bradykinin B2 receptor antagonists incorporating the 4-heteroarylquinoline framework. Improvement of aqueous solubility and new insights into species difference.
J Med Chem 47: 1617-30 (2004)
Fujisawa Pharmaceutical
Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model.
J Med Chem 47: 1602-4 (2004)
Millennium Pharmaceuticals
7-Alkoxy-4-phenylamino-3-quinolinecar-bonitriles as dual inhibitors of Src and Abl kinases.
J Med Chem 47: 1599-601 (2004)
Wyeth Research
Preliminary in vitro studies on two potent, water-soluble trimethoprim analogues with exceptional species selectivity against dihydrofolate reductase from Pneumocystis carinii and Mycobacterium avium.
Bioorg Med Chem Lett 14: 1811-5 (2004)
Harvard Medical School
Synthesis of potent sigma-1 receptor ligands via fragmentation of dextromethorphan.
Bioorg Med Chem Lett 14: 1807-9 (2004)
Ucb Pharma
Synthesis of methylphenidate analogues and their binding affinities at dopamine and serotonin transport sites.
Bioorg Med Chem Lett 14: 1799-802 (2004)
State University Of New York
Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists.
Bioorg Med Chem Lett 14: 1795-8 (2004)
Merck
Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists.
Bioorg Med Chem Lett 14: 1791-4 (2004)
Schering-Plough Research Institute
Synthesis and evaluation of substituted 4-alkoxy-2-aminopyridines as novel neuropeptide Y1 receptor antagonists.
Bioorg Med Chem Lett 14: 1761-4 (2004)
Tsukuba Research Institute
A prodrug approach to COX-2 inhibitors with methylsulfone.
Bioorg Med Chem Lett 14: 1757-60 (2004)
Amorepacific
6-aryl-2,4-dioxo-5-hexenoic acids, novel integrase inhibitors active against HIV-1 multiplication in cell-based assays.
Bioorg Med Chem Lett 14: 1745-9 (2004)
Sapienza University Of Rome
Carbazates as potent inhibitors of hormone-sensitive lipase.
Bioorg Med Chem Lett 14: 1741-4 (2004)
Novo Nordisk
The inhibition of metallo-beta-lactamase by thioxo-cephalosporin derivatives.
Bioorg Med Chem Lett 14: 1737-9 (2004)
University Of Huddersfield
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.
Bioorg Med Chem Lett 14: 1721-7 (2004)
Abbott Laboratories
Small molecule biaryl FSH receptor agonists. Part 2: Lead optimization via parallel synthesis.
Bioorg Med Chem Lett 14: 1717-20 (2004)
Pharmacopeia
Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis.
Bioorg Med Chem Lett 14: 1713-6 (2004)
Pharmacopeia
The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands.
Bioorg Med Chem Lett 14: 1709-12 (2004)
Arqule
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.
Bioorg Med Chem Lett 14: 1703-7 (2004)
Cnrs
N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.
Bioorg Med Chem Lett 14: 1693-6 (2004)
Seoul National University
Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors.
Bioorg Med Chem Lett 14: 1683-8 (2004)
Discovery Research-Dr. Reddy'S Laboratories
Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands.
Bioorg Med Chem Lett 14: 1679-82 (2004)
The Neuroscience Research Centre
Design and synthesis of macrocyclic inhibitors of phosphatase cdc25B.
Bioorg Med Chem Lett 14: 1673-7 (2004)
Schering
Inhibitory activities against topoisomerase I and II by polyhydroxybenzoyl amide derivatives and their structure-activity relationship.
Bioorg Med Chem Lett 14: 1669-72 (2004)
Kumamoto University
Synthesis and evaluation of analogues of S-adenosyl-L-methionine, as inhibitors of the E. coli cyclopropane fatty acid synthase.
Bioorg Med Chem Lett 14: 1661-4 (2004)
Universit£
Lactams as EP4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization.
Bioorg Med Chem Lett 14: 1655-9 (2004)
Roche Palo Alto
Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.
Bioorg Med Chem Lett 14: 1645-9 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery and SAR of trisubstituted thiazolidinones as CCR4 antagonists.
Bioorg Med Chem Lett 14: 1619-24 (2004)
Array Biopharma
The synthesis and structure-activity relationships of 3-amino-4-benzylquinolin-2-ones; discovery of novel KCNQ2 channel openers.
Bioorg Med Chem Lett 14: 1615-8 (2004)
The Bristol-Myers Squibb Pharmaceutical Research Institute
[3H]A-317491, a novel high-affinity non-nucleotide antagonist that specifically labels human P2X2/3 and P2X3 receptors.
J Pharmacol Exp Ther 310: 407-16 (2004)
Abbott Laboratories
The comparative pharmacology and up-regulation of rat neuronal nicotinic receptor subtype binding sites stably expressed in transfected mammalian cells.
J Pharmacol Exp Ther 310: 98-107 (2004)
Georgetown University
Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists [corrected].
Bioorg Med Chem Lett 14: 1053-6 (2004)
Roche Palo Alto
Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.
Bioorg Med Chem Lett 14: 1049-52 (2004)
Merck Research Laboratories
Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.
Bioorg Med Chem Lett 14: 1043-8 (2004)
Merck Frosst Centre For Therapeutic Research
The development of potent non-peptidic PTP-1B inhibitors.
Bioorg Med Chem Lett 14: 1039-42 (2004)
Merck Frosst Centre For Therapeutic Research
1,2-Benzothiazine 1,1-dioxide alpha-ketoamide analogues as potent calpain I inhibitors.
Bioorg Med Chem Lett 14: 1035-8 (2004)
Cephalon
Benzodiazepine-based selective inhibitors of mitochondrial F1F0 ATP hydrolase.
Bioorg Med Chem Lett 14: 1031-4 (2004)
Pharmaceutical Research Institute
N-[1-Aryl-2-(1-imidazolo)ethyl]-guanidine derivatives as potent inhibitors of the bovine mitochondrial F1F0 ATP hydrolase.
Bioorg Med Chem Lett 14: 1027-30 (2004)
Pharmaceutical Research Institute
4-Substituted anilides as selective melatonin MT2 receptor agonists.
Bioorg Med Chem Lett 14: 1023-6 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Anti-inflammatory flavonoids and pterocarpanoid from Crotalaria pallida and C. assamica.
Bioorg Med Chem Lett 14: 1011-4 (2004)
Kaohsiung Medical University
Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.
Bioorg Med Chem Lett 14: 1003-5 (2004)
Virginia Commonwealth University
Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.
Bioorg Med Chem Lett 14: 999-1002 (2004)
Virginia Commonwealth University
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.
Bioorg Med Chem Lett 14: 989-93 (2004)
Millennium Pharmaceuticals
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs.
Bioorg Med Chem Lett 14: 983-7 (2004)
Millennium Pharmaceuticals
Synthesis and evaluation of S-4-(3-thienyl)phenyl-alpha-methylacetic acid.
Bioorg Med Chem Lett 14: 979-82 (2004)
National Institute Of Pharmaceutical Education And Research
Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery of benzimidazole 5-carboxylic amide derivatives with low-nanomolar potency.
Bioorg Med Chem Lett 14: 967-71 (2004)
Boehringer Ingelheim (Canada)
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.
Bioorg Med Chem Lett 14: 959-63 (2004)
Glaxosmithkline
Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.
Bioorg Med Chem Lett 14: 953-7 (2004)
Glaxosmithkline
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.
Bioorg Med Chem Lett 14: 947-52 (2004)
Merck Research Laboratories
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.
Bioorg Med Chem Lett 14: 941-5 (2004)
Merck Research Laboratories
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains.
Bioorg Med Chem Lett 14: 935-9 (2004)
Merck Research Laboratories
A new series of potent oxindole inhibitors of CDK2.
Bioorg Med Chem Lett 14: 913-7 (2004)
Hoffmann-La Roche
Design and synthesis of 3,7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR.
Bioorg Med Chem Lett 14: 909-12 (2004)
Merck Research Laboratories
Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.
Bioorg Med Chem Lett 14: 875-9 (2004)
Kirin Brewery
Carbonic anhydrase inhibitors: the first selective, membrane-impermeant inhibitors targeting the tumor-associated isozyme IX.
Bioorg Med Chem Lett 14: 869-73 (2004)
Slovak Academy Of Sciences
3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2.
Bioorg Med Chem Lett 14: 865-8 (2004)
Abbott Laboratories
Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 14: 859-63 (2004)
Merck Research Laboratories
Miraziridine A: natures blueprint towards protease class-spanning inhibitors.
Bioorg Med Chem Lett 14: 855-7 (2004)
Institut FüR Biochemie
Inhibitory effects on mushroom tyrosinase by some alkylbenzaldehydes.
J Enzyme Inhib Med Chem 18: 491-6 (2003)
Xiamen University
Evaluation of indole esters as inhibitors of p60(c-Src) receptor tyrosine kinase and investigation of the inhibition using receptor docking studies.
J Enzyme Inhib Med Chem 18: 485-90 (2003)
Kobe Gakuin University
HIV protease inhibitors are inhibitors but not substrates of the human breast cancer resistance protein (BCRP/ABCG2).
J Pharmacol Exp Ther 310: 334-41 (2004)
University Of Washington
Elimination of antibacterial activities of non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists derived from erythromycin A.
Bioorg Med Chem Lett 14: 1599-602 (2004)
Abbott Laboratories
Design, synthesis and structure-activity relationship of novel RXR-selective modulators.
Bioorg Med Chem Lett 14: 1593-8 (2004)
Ligand Pharmaceuticals
Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.
Bioorg Med Chem Lett 14: 1577-80 (2004)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological activity of selective azasugar-based TACE inhibitors.
Bioorg Med Chem Lett 14: 1569-72 (2004)
Organon K.K.
Thrombin inhibitors built on an azaphenylalanine scaffold.
Bioorg Med Chem Lett 14: 1563-7 (2004)
University Of Ljubljana
KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.
Bioorg Med Chem Lett 14: 1527-31 (2004)
Kyoto Pharmaceutical University
Discovery of novel heteroaryl-substituted chalcones as inhibitors of TNF-alpha-induced VCAM-1 expression.
Bioorg Med Chem Lett 14: 1513-7 (2004)
Atherogenics
Structure-activity relationships of a novel class of endothelin receptor selective antagonists; 6-carboxy-2-isopropylamino-5,7-diarylcyclopenteno[1,2-b]pyridines.
Bioorg Med Chem Lett 14: 1503-7 (2004)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
2-(N-acyl) and 2-N-acyl-N(6)-substituted analogues of adenosine and their affinity at the human adenosine receptors.
Bioorg Med Chem Lett 14: 1495-8 (2004)
Inotek Pharmaceuticals
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.
Bioorg Med Chem Lett 14: 1491-3 (2004)
Hoffmann-La Roche
New PDMP analogues inhibit process outgrowth in an insect cell line.
Bioorg Med Chem Lett 14: 1487-90 (2004)
University Of Arizona
Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors.
Bioorg Med Chem Lett 14: 1483-6 (2004)
Bristol-Myers Squibb Pharmaceuticals Research Institute
Identification of novel potent bicyclic peptide deformylase inhibitors.
Bioorg Med Chem Lett 14: 1477-81 (2004)
Genomics Institute Of The Novartis Research Foundation
Synthesis of cinnamic acids and related isosteres as potent and selective alpha v beta 3 receptor antagonists.
Bioorg Med Chem Lett 14: 1471-6 (2004)
Pfizer
Determination of the stable conformation of GABA(A)-benzodiazepine receptor bivalent ligands by low temperature NMR and X-ray analysis.
Bioorg Med Chem Lett 14: 1465-9 (2004)
University Of Wisconsin-Milwaukee
Synthesis and SAR of 2-arylbenzoxazoles, benzothiazoles and benzimidazoles as inhibitors of lysophosphatidic acid acyltransferase-beta.
Bioorg Med Chem Lett 14: 1455-9 (2004)
Cell Therapeutics
HIV-1 integrase pharmacophore model derived from diverse classes of inhibitors.
Bioorg Med Chem Lett 14: 1447-54 (2004)
University Of Houston
Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization.
Bioorg Med Chem Lett 14: 1441-6 (2004)
Vertex Pharmaceuticals
Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.
Bioorg Med Chem Lett 14: 1417-21 (2004)
Merck Research Laboratories
Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles.
Bioorg Med Chem Lett 14: 1411-6 (2004)
Wyeth Research
Crucial amides for dimerization inhibitors of HIV-1 protease.
Bioorg Med Chem Lett 14: 1395-8 (2004)
Purdue University
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