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A metabolically stable tight-binding transition-state inhibitor of glyoxalase-I.
Bioorg Med Chem Lett 16: 6039-42 (2006)
University Of Minnesota
5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase.
Bioorg Med Chem Lett 16: 6236-40 (2006)
Gsk
Polyoxometalates--a new class of potent ecto-nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitors.
Bioorg Med Chem Lett 16: 5943-7 (2006)
University Of Bonn
The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck).
Bioorg Med Chem Lett 16: 5973-7 (2006)
Procter And Gamble Pharmaceuticals
Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction.
Bioorg Med Chem Lett 16: 5958-62 (2006)
Abbott Laboratories
Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands.
Bioorg Med Chem Lett 16: 6043-8 (2006)
Johnson & Johnson Pharmaceutical
Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors.
Bioorg Med Chem Lett 16: 5907-12 (2006)
Merck Research Laboratories
Synthesis and biological evaluation of 5-arylamino-6-chloro-1H-indazole-4,7-diones as inhibitors of protein kinase B/Akt.
Bioorg Med Chem Lett 16: 6001-5 (2006)
Ildong Pharmaceutical
Taspine: bioactivity-guided isolation and molecular ligand-target insight of a potent acetylcholinesterase inhibitor from Magnolia x soulangiana.
J Nat Prod 69: 1341-6 (2006)
Leopold-Franzens-Universit£T
Oculatol, oculatolide, and A-nor sterols from the sponge Haliclona oculata.
J Nat Prod 69: 1330-4 (2006)
Peking University
Antidepressant principles of the roots of Polygala tenuifolia.
J Nat Prod 69: 1305-9 (2006)
Medical And Pharmaceutical Industry Technology And Development Center
Grandisines C-G, indolizidine alkaloids from the Australian rainforest tree Elaeocarpus grandis.
J Nat Prod 69: 1295-9 (2006)
Griffith University
Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides.
Bioorg Med Chem Lett 16: 5968-72 (2006)
Merck And
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
Bioorg Med Chem Lett 16: 6086-90 (2006)
Abbott Laboratories
A series of novel, potent, and selective histone deacetylase inhibitors.
Bioorg Med Chem Lett 16: 5948-52 (2006)
Irbm/Merck Research Laboratories
Discovery of small molecule inhibitors of integrin alphavbeta3 through structure-based virtual screening.
Bioorg Med Chem Lett 16: 5878-82 (2006)
Chinese Academy Of Medical Sciences And Peking Union Medical College
Arylsulfonamides: a study of the relationship between activity and conformational preferences for a series of factor Xa inhibitors.
Bioorg Med Chem Lett 16: 5731-5 (2006)
Glaxosmithkline
Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.
Bioorg Med Chem Lett 16: 5953-7 (2006)
Glaxosmithkline
Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
Bioorg Med Chem Lett 16: 6116-9 (2006)
Pfizer
Enzyme inhibition potency enhancement by active site metal chelating and hydrogen bonding induced conformation-restricted cyclopropanecarbonyl derivatives.
Bioorg Med Chem Lett 16: 6024-7 (2006)
Tunghai University
Synthesis and biological study of 4-aminopyrimidine-5-carboxaldehyde oximes as antiproliferative VEGFR-2 inhibitors.
Bioorg Med Chem Lett 16: 6063-6 (2006)
Johnson & Johnson Pharmaceutical
3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.
Bioorg Med Chem Lett 16: 6049-53 (2006)
Merck Research Laboratories
Structure-activity relationships for a novel series of thiazolyl phenyl ether derivatives exhibiting potent and selective acetyl-CoA carboxylase 2 inhibitory activity.
Bioorg Med Chem Lett 16: 6078-81 (2006)
Abbott Laboratories
Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis.
Bioorg Med Chem Lett 16: 6067-72 (2006)
Wyeth Research
Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
Bioorg Med Chem Lett 16: 6120-3 (2006)
Pfizer
Inhibitors of unactivated p38 MAP kinase.
Bioorg Med Chem Lett 16: 6102-6 (2006)
Johnson And Johnson Pharmaceutical Research And Development
Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.
Bioorg Med Chem Lett 16: 5723-30 (2006)
Abbott Laboratories
Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands.
Bioorg Med Chem Lett 16: 6058-62 (2006)
Merck Sharp And Dohme Research Laboratories
Identification of non-furan containing A2A antagonists using database mining and molecular similarity approaches.
Bioorg Med Chem Lett 16: 5993-7 (2006)
Vernalis (R&D)
1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists.
J Med Chem 49: 5794-803 (2006)
Purdue University
Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.
J Med Chem 49: 5785-93 (2006)
University Of Antwerp
HIV-1 protease mutations and inhibitor modifications monitored on a series of complexes. Structural basis for the effect of the A71V mutation on the active site.
J Med Chem 49: 5777-84 (2006)
Academy Of Sciences Of The Czech Republic
[4-(imidazol-1-yl)thiazol-2-yl]phenylamines. A novel class of highly potent colchicine site binding tubulin inhibitors: synthesis and cytotoxic activity on selected human cancer cell lines.
J Med Chem 49: 5769-76 (2006)
University Of Regensburg
Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling.
J Med Chem 49: 5759-68 (2006)
University Of Milano-Bicocca
Synthesis of adenophostin A analogues conjugating an aromatic group at the 5'-position as potent IP3 receptor ligands.
J Med Chem 49: 5750-8 (2006)
Hokkaido University
Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites.
J Med Chem 49: 5710-27 (2006)
Yale University
Iminosugars as potential inhibitors of glycogenolysis: structural insights into the molecular basis of glycogen phosphorylase inhibition.
J Med Chem 49: 5687-701 (2006)
The National Hellenic Research Foundation
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
J Med Chem 49: 5671-86 (2006)
Amgen
Identification of a novel 4-aminomethylpiperidine class of M3 muscarinic receptor antagonists and structural insight into their M3 selectivity.
J Med Chem 49: 5653-63 (2006)
Tsukuba Research Institute
Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
J Med Chem 49: 5649-52 (2006)
Eli Lilly
Fumarranol, a rearranged fumagillin analogue that inhibits angiogenesis in vivo.
J Med Chem 49: 5645-8 (2006)
The Johns Hopkins University School Of Medicine
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
Bioorg Med Chem Lett 16: 5584-9 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
Bioorg Med Chem Lett 16: 5805-8 (2006)
University Of Michigan
A novel series of imidazo[1,2-a]pyridine derivatives as HIF-1alpha prolyl hydroxylase inhibitors.
Bioorg Med Chem Lett 16: 5598-601 (2006)
Procter And Gamble Pharmaceuticals
Identification of novel inhibitors of UDP-Glc 4'-epimerase, a validated drug target for african sleeping sickness.
Bioorg Med Chem Lett 16: 5744-7 (2006)
University Of Dundee
Evaluation of the activities of pyrimethamine analogs against Plasmodium vivax and Plasmodium falciparum dihydrofolate reductase-thymidylate synthase using in vitro enzyme inhibition and bacterial complementation assays.
Antimicrob Agents Chemother 50: 3631-7 (2006)
National Center For Genetic Engineering And Biotechnology At Thailand
AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.
Cancer Res 66: 8715-21 (2006)
Amgen
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.
Bioorg Med Chem Lett 16: 5748-51 (2006)
Merck Sharp & Dohme Research Laboratories
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.
Bioorg Med Chem Lett 16: 5752-6 (2006)
Merck Sharp & Dohme Research Laboratories
Quantitative evaluation of each catalytic subsite of cathepsin B for inhibitory activity based on inhibitory activity-binding mode relationship of epoxysuccinyl inhibitors by X-ray crystal structure analyses of complexes.
J Mol Biol 362: 979-93 (2006)
Osaka University Of Pharmaceutical Sciences
Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.
Bioorg Med Chem Lett 16: 5897-901 (2006)
Merck Research Laboratories
Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors.
Bioorg Med Chem Lett 16: 5773-7 (2006)
University Of California
The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors.
Bioorg Med Chem Lett 16: 5778-83 (2006)
Johnson & Johnson Pharmaceutical
Naphtho[2,3-b][1,4]-thiazine-5,10-diones and 3-substituted-1,4-dioxo-1,4-dihydronaphthalen-2-yl-thioalkanoate derivatives: synthesis and biological evaluation as potential antibacterial and antifungal agents.
Bioorg Med Chem Lett 16: 5883-7 (2006)
Lucknow University
Synthesis of 3,6-bis[H-Tyr/H-Dmt-NH(CH2)m,n]-2(1H)pyrazinone derivatives: function of alkyl chain length on opioid activity.
Bioorg Med Chem Lett 16: 5793-6 (2006)
Kobe Gakuin University
p38 MAP kinase inhibitors. Part 5: discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffold.
Bioorg Med Chem Lett 16: 5468-71 (2006)
Merck Research Laboratories
p38 MAP kinase inhibitors. Part 6: 2-arylpyridazin-3-ones as templates for inhibitor design.
Bioorg Med Chem Lett 16: 5809-13 (2006)
Merck Research Laboratories
Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors.
Bioorg Med Chem Lett 16: 5832-5 (2006)
Virginia Commonwealth University
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
Bioorg Med Chem Lett 16: 5840-3 (2006)
Friedrich-Schiller-UniversitäT Jena
Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA.
Bioorg Med Chem Lett 16: 5605-9 (2006)
Saarland University
Novel thienopyrrole glycogen phosphorylase inhibitors: synthesis, in vitro SAR and crystallographic studies.
Bioorg Med Chem Lett 16: 5567-71 (2006)
Astrazeneca
Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues.
Bioorg Med Chem Lett 16: 5498-502 (2006)
Harvard Medical School
Synthesis and structure-activity relationships of 3-phenyl-2-propenamides as inhibitors of glycogen phosphorylase a.
Bioorg Med Chem Lett 16: 5892-6 (2006)
Glaxosmithkline
Discovery and synthesis of tetrahydroindolone-derived carbamates as Kv1.5 blockers.
Bioorg Med Chem Lett 16: 5855-8 (2006)
Procter And Gamble Pharmaceuticals
A bioisosteric approach to the discovery of indole carbinol androgen receptor ligands.
Bioorg Med Chem Lett 16: 5646-9 (2006)
Johnson And Johnson Pharmaceutical Research And Development
Discovery and synthesis of tetrahydroindolone derived semicarbazones as selective Kv1.5 blockers.
Bioorg Med Chem Lett 16: 5859-63 (2006)
Procter & Gamble Pharmaceuticals
Synthesis and alpha4beta2 nicotinic affinity of unichiral 5-(2-pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes.
Bioorg Med Chem Lett 16: 5610-5 (2006)
Universit£
Potent, selective pyrimidinetrione-based inhibitors of MMP-13.
Bioorg Med Chem Lett 16: 5822-6 (2006)
Pfizer
New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.
J Med Chem 49: 5640-3 (2006)
Harvard Medical School
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine.
J Med Chem 49: 5635-9 (2006)
Rensselaer Polytechnic Institute
Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
J Med Chem 49: 5610-7 (2006)
University Of Cagliari
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
J Med Chem 49: 5597-609 (2006)
Research Triangle Institute
Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.
J Med Chem 49: 5587-96 (2006)
Hokkaido University
3-[5-(4,5-dihydro-1H-imidazol-2-yl)-furan-2-yl]phenylamine (Amifuraline), a promising reversible and selective peripheral MAO-A inhibitor.
J Med Chem 49: 5578-86 (2006)
Università
5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase.
J Med Chem 49: 5562-70 (2006)
Instituto De QuíMica MéDica (Csic)
Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX.
J Med Chem 49: 5544-51 (2006)
Istituto Di Biostrutture E Bioimmagini-Cnr
Structure-activity relationships of uridine 5'-diphosphate analogues at the human P2Y6 receptor.
J Med Chem 49: 5532-43 (2006)
National Institute Of Diabetes And Digestive And Kidney Diseases
Complexes of alkylene-linked tacrine dimers with Torpedo californica acetylcholinesterase: Binding of Bis5-tacrine produces a dramatic rearrangement in the active-site gorge.
J Med Chem 49: 5491-500 (2006)
Institute Of Science
Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity.
J Med Chem 49: 5470-7 (2006)
University Of Oxford
Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.
J Med Chem 49: 5424-33 (2006)
University Of Kansas
Uncompetitive antagonism of AMPA receptors: Mechanistic insights from studies of polyamine toxin derivatives.
J Med Chem 49: 5414-23 (2006)
The Danish University Of Pharmaceutical Sciences
Homobivalent quinazolinimines as novel nanomolar inhibitors of cholinesterases with dirigible selectivity toward butyrylcholinesterase.
J Med Chem 49: 5411-3 (2006)
Friedrich-Schiller-UniversitäT Jena
A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies.
J Med Chem 49: 5404-7 (2006)
Irbm (Merck Research Laboratories Rome)
Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy.
Nat Chem Biol 2: 543-50 (2006)
University Of Illinois
Thermodynamic penalty arising from burial of a ligand polar group within a hydrophobic pocket of a protein receptor.
J Mol Biol 362: 994-1003 (2006)
University Of Leeds
Epibatidine isomers and analogues: structure-activity relationships.
Bioorg Med Chem Lett 16: 5493-7 (2006)
University Of Leicester
Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors.
Bioorg Med Chem Lett 16: 5561-6 (2006)
Valeant Pharmaceuticals Research & Development
Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3.
Bioorg Med Chem Lett 16: 5633-8 (2006)
Procter And Gamble Pharmaceuticals
N,N'-Diarylcyanoguanidines as antagonists of the CXCR2 and CXCR1 chemokine receptors.
Bioorg Med Chem Lett 16: 5513-6 (2006)
Glaxosmithkline
Biological activities and 3D QSAR studies of a series of Delisea pulchra (cf. fimbriata) derived natural products.
J Nat Prod 69: 1180-7 (2006)
Australian Institute Of Marine Science
Chemical probes of UDP-galactopyranose mutase.
Chem Biol 13: 825-37 (2006)
University Of Wisconsin-Madison
Comparison between two classes of selective EP(3) antagonists and their biological activities.
Bioorg Med Chem Lett 16: 5639-42 (2006)
Merck Frosst Centre For Therapeutic Research
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.
Bioorg Med Chem Lett 16: 5546-50 (2006)
Targegen
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.
Bioorg Med Chem Lett 16: 5488-92 (2006)
Gnf
Inhibitory effect of carboxylic acid group on hERG binding.
Bioorg Med Chem Lett 16: 5507-12 (2006)
Portola Pharmaceuticals
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
Bioorg Med Chem Lett 16: 5462-7 (2006)
University Of Arizona
Structure-based design, synthesis, and SAR evaluation of a new series of 8-hydroxyquinolines as HIF-1alpha prolyl hydroxylase inhibitors.
Bioorg Med Chem Lett 16: 5517-22 (2006)
Procter And Gamble Pharmaceuticals
Potent benzimidazolone based human beta(3)-adrenergic receptor agonists.
Bioorg Med Chem Lett 16: 5691-4 (2006)
Eli Lilly
Pyridone derivatives as potent, orally bioavailable VLA-4 integrin antagonists.
Bioorg Med Chem Lett 16: 5538-41 (2006)
Glaxosmithkline
Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
Bioorg Med Chem Lett 16: 5555-60 (2006)
Abbott Laboratories
2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: synthesis and selectivity.
Bioorg Med Chem Lett 16: 5695-9 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
Nat Chem Biol 2: 551-8 (2006)
The Scripps Research Institute
Design of inhibitors against guanase: synthesis and biochemical evaluation of analogues of azepinomycin.
Bioorg Med Chem Lett 16: 5551-4 (2006)
University Of Maryland
Alpha-1-C-octyl-1-deoxynojirimycin as a pharmacological chaperone for Gaucher disease.
Bioorg Med Chem 14: 7736-44 (2006)
Hokuriku University
Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-gamma binding agents with potential application to the treatment of osteoporosis.
Bioorg Med Chem Lett 16: 5659-63 (2006)
Procter And Gamble Pharmaceuticals
Anti-atherosclerotic and anti-inflammatory activities of catecholic xanthones and flavonoids isolated from Cudrania tricuspidata.
Bioorg Med Chem Lett 16: 5580-3 (2006)
National Research Laboratory Of Lipid Metabolism And Atherosclerosis
Potent inhibitors of lipoprotein-associated phospholipase A(2): benzaldehyde O-heterocycle-4-carbonyloxime.
Bioorg Med Chem Lett 16: 5576-9 (2006)
National Research Laboratory Of Lipid Metabolism And Atherosclerosis
Derivatives of 7-amino-1,2,3,4-tetrahydroisoquinoline and isophthalic acids as novel fibrinogen receptor antagonists.
Bioorg Med Chem Lett 16: 5294-7 (2006)
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 16: 5373-7 (2006)
Merck Research Laboratories
2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.
Bioorg Med Chem Lett 16: 5270-4 (2006)
Merck Research Laboratories
Chemical transformations of oxyresveratrol (trans-2,4,3',5'-tetrahydroxystilbene) into a potent tyrosinase inhibitor and a strong cytotoxic agent.
Bioorg Med Chem Lett 16: 5650-3 (2006)
Chulalongkorn University
4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists.
Bioorg Med Chem Lett 16: 5275-9 (2006)
Merck Research Laboratories
Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics.
J Biol Chem 281: 32784-95 (2006)
Incyte
WAY-100635 is a potent dopamine D4 receptor agonist.
Psychopharmacology (Berl) 188: 244-51 (2006)
Purdue University
Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
J Med Chem 49: 5382-5 (2006)
National University Of Singapore
Novel pyrazolopyrimidopyridazinones with potent and selective phosphodiesterase 5 (PDE5) inhibitory activity as potential agents for treatment of erectile dysfunction.
J Med Chem 49: 5363-71 (2006)
Università
7'-substituted benzothiazolothio- and pyridinothiazolothio-purines as potent heat shock protein 90 inhibitors.
J Med Chem 49: 5352-62 (2006)
Conforma Therapeutics
Design and discovery of a novel dipeptidyl-peptidase IV (CD26)-based prodrug approach.
J Med Chem 49: 5339-51 (2006)
Instituto De QuíMica MéDica (Csic)
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
J Med Chem 49: 5333-8 (2006)
University Of Bristol
Replacement of the metabolically labile methyl esters in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors with isoxazolone, isoxazole, oxazolone, or cyano substituents.
J Med Chem 49: 5316-23 (2006)
Purdue University
Phosphonothioate and fluoromethylene phosphonate analogues of cyclic phosphatidic acid: Novel antagonists of lysophosphatidic acid receptors.
J Med Chem 49: 5309-15 (2006)
The University Of Utah
Synthesis, calpain inhibitory activity, and cytotoxicity of P2-substituted proline and thiaproline peptidyl aldehydes and peptidyl alpha-ketoamides.
J Med Chem 49: 5282-90 (2006)
The University Of Tennessee Health Science Center
Synthesis and structure-activity relationships of truncated bisubstrate inhibitors of aminoglycoside 6'-N-acetyltransferases.
J Med Chem 49: 5273-81 (2006)
Mcgill University
Structure-Based Design of Novel HIV-1 Protease Inhibitors To Combat Drug Resistance.
J Med Chem 49: 5252-61 (2006)
Purdue University
Novel small-molecule inhibitors of anthrax lethal factor identified by high-throughput screening.
J Med Chem 49: 5232-44 (2006)
Montana State University
Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors.
J Med Chem 49: 5217-25 (2006)
Virginia Commonwealth University
Calcium channel antagonists discovered by a multidisciplinary approach.
J Med Chem 49: 5206-16 (2006)
Universit£
Structure-based drug design and structural biology study of novel nonpeptide inhibitors of severe acute respiratory syndrome coronavirus main protease.
J Med Chem 49: 5154-61 (2006)
National Defense Medical Center
Novel structural features of CDK inhibition revealed by an ab initio computational method combined with dynamic simulations.
J Med Chem 49: 5141-53 (2006)
University Of Cambridge
N1-Benzoyl-N2-[1-(1-naphthyl)ethyl]-trans-1,2-diaminocyclohexanes: Development of 4-chlorophenylcarboxamide (calhex 231) as a new calcium sensing receptor ligand demonstrating potent calcilytic activity.
J Med Chem 49: 5119-28 (2006)
Cnrs
1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction.
J Med Chem 49: 5093-109 (2006)
Abbott Laboratories
Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).
J Med Chem 49: 5051-8 (2006)
Istituto Di Cristallografia
Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders.
J Med Chem 49: 5047-50 (2006)
Institut De Recherches Servier
Synthesis and monoamine transporter affinity of 2beta-carbomethoxy-3beta-(4'-p-substituted phenyl)-piperidine analogs of cocaine.
Bioorg Med Chem Lett 16: 5222-5 (2006)
Yale University
Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.
Bioorg Med Chem Lett 16: 5303-8 (2006)
Novo Nordisk
Design and synthesis of substituted pyridine derivatives as HIF-1alpha prolyl hydroxylase inhibitors.
Bioorg Med Chem Lett 16: 5616-20 (2006)
Procter And Gamble Pharmaceuticals
Application of azide-alkyne cycloaddition 'click chemistry' for the synthesis of Grb2 SH2 domain-binding macrocycles.
Bioorg Med Chem Lett 16: 5265-9 (2006)
Nih
Design and synthesis of a series of novel pyrazolopyridines as HIF-1alpha prolyl hydroxylase inhibitors.
Bioorg Med Chem Lett 16: 5687-90 (2006)
Procter And Gamble Pharmaceuticals
Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: from benzimidazole to indole scaffolds.
Bioorg Med Chem Lett 16: 4987-93 (2006)
Boehringer Ingelheim Pharmaceuticals
Peptidyl-urea based inhibitors of soluble epoxide hydrolases.
Bioorg Med Chem Lett 16: 5439-44 (2006)
University Of California
Farnesoid X-activated receptor antagonists from a marine sponge Spongia sp.
Bioorg Med Chem Lett 16: 5398-402 (2006)
Seoul National University
Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters.
Bioorg Med Chem Lett 16: 5018-21 (2006)
University Of Kentucky
Novel benzimidazole-based MCH R1 antagonists.
Bioorg Med Chem Lett 16: 4994-5000 (2006)
Glaxosmithkline
New, potent P1/P2-morpholinone-based HIV-protease inhibitors.
Bioorg Med Chem Lett 16: 5226-30 (2006)
Glaxosmithkline
Synthesis of bicyclic molecular scaffolds (BTAa): an investigation towards new selective MMP-12 inhibitors.
Bioorg Med Chem 14: 7392-403 (2006)
University Of Florence
Synthesis and biological evaluation of heterocycle containing adamantane 11beta-HSD1 inhibitors.
Bioorg Med Chem Lett 16: 5414-9 (2006)
Abbott Laboratories
Synthesis and biological evaluation of benzamides and benzamidines as selective inhibitors of VEGFR tyrosine kinases.
Bioorg Med Chem Lett 16: 5127-31 (2006)
Gakushuin University
Synthesis and structure-activity relationships of FAAH inhibitors: cyclohexylcarbamic acid biphenyl esters with chemical modulation at the proximal phenyl ring.
ChemMedChem 1: 130-9 (2006)
Universit?? Degli Studi Di Parma
Unexpected novel binding mode of pyrrolidine-based aspartyl protease inhibitors: design, synthesis and crystal structure in complex with HIV protease.
ChemMedChem 1: 106-17 (2006)
Philipps-Universität Marburg
Selective indole-based ECE inhibitors: synthesis and pharmacological evaluation.
ChemMedChem 1: 96-105 (2006)
Bayer Healthcare
Synthesis, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis.
Bioorg Med Chem Lett 16: 5041-6 (2006)
Washington University
Aza-stilbenes as potent and selective c-RAF inhibitors.
Bioorg Med Chem Lett 16: 5378-83 (2006)
Glaxosmithkline
Novel C-3 N-urea, amide, and carbamate dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs as potent TIE-2 and VEGF-R2 dual inhibitors.
Bioorg Med Chem Lett 16: 5368-72 (2006)
Cephalon
Synthesis of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones as potent antimalarial agents active against CQ-resistant P. falciparum strains.
Bioorg Med Chem Lett 16: 5384-8 (2006)
Universit£
Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors.
Bioorg Med Chem Lett 16: 5360-3 (2006)
St. Jude Children'S Research Hospital
Synthesis and structural activity relationship of 11beta-HSD1 inhibitors with novel adamantane replacements.
Bioorg Med Chem Lett 16: 5408-13 (2006)
Abbott Laboratories
The molecular basis for the selection of captopril cis and trans conformations by angiotensin I converting enzyme.
Bioorg Med Chem Lett 16: 5084-7 (2006)
Mrc Laboratory Of Molecular Biology, Hills Road, Cambridge, Cb2 2Qh
Novel aminobenzimidazoles as selective MCH-R1 antagonists for the treatment of metabolic diseases.
Bioorg Med Chem Lett 16: 5427-31 (2006)
Schering-Plough Research Institute
1-Alkyl-2-aryl-4-(1-naphthoyl)pyrroles: new high affinity ligands for the cannabinoid CB1 and CB2 receptors.
Bioorg Med Chem Lett 16: 5432-5 (2006)
Clemson University
Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine.
Bioorg Med Chem Lett 16: 5052-6 (2006)
Merck Research Laboratories
Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists.
Bioorg Med Chem Lett 16: 5066-72 (2006)
Amgen
Novel tricyclic azepine derivatives: Biological evaluation of pyrimido[4,5-b]-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase.
Bioorg Med Chem Lett 16: 5102-6 (2006)
Imclone Systems
Novel methylenephosphophosphonate analogues of mycophenolic adenine dinucleotide. Inhibition of inosine monophosphate dehydrogenase.
J Med Chem 49: 5018-22 (2006)
University Of Minnesota
NMR structure of a potent small molecule inhibitor bound to human keratinocyte fatty acid-binding protein.
J Med Chem 49: 5013-7 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis of anthranylaldoxime derivatives as estrogen receptor ligands and computational prediction of binding modes.
J Med Chem 49: 5001-12 (2006)
Università
Probing hot spots at protein-ligand binding sites: a fragment-based approach using biophysical methods.
J Med Chem 49: 4992-5000 (2006)
University Chemical Laboratory
Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.
J Med Chem 49: 4981-91 (2006)
Amgen
Synthesis, crystal structure, structure-activity relationships, and antiviral activity of a potent SARS coronavirus 3CL protease inhibitor.
J Med Chem 49: 4971-80 (2006)
Taigen Biotechnology
Design of inhibitors of orotidine monophosphate decarboxylase using bioisosteric replacement and determination of inhibition kinetics.
J Med Chem 49: 4937-45 (2006)
University Of Toronto
Structural insights into monoamine oxidase inhibitory potency and selectivity of 7-substituted coumarins from ligand- and target-based approaches.
J Med Chem 49: 4912-25 (2006)
Universit£
4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution.
J Med Chem 49: 4896-911 (2006)
University Of Auckland
Brunsvicamides A-C: sponge-related cyanobacterial peptides with Mycobacterium tuberculosis protein tyrosine phosphatase inhibitory activity.
J Med Chem 49: 4871-8 (2006)
University Of Bonn
Inhibition of kinesin motor proteins by adociasulfate-2.
J Med Chem 49: 4857-60 (2006)
University Of Georgia
Structure-activity relationships of [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5' '-(4' '-amino-1' ',2' '-oxathiole-2' ',2' '-dioxide)thymine derivatives as inhibitors of HIV-1 reverse transcriptase dimerization.
J Med Chem 49: 4834-41 (2006)
University Of Pittsburgh
Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate.
J Med Chem 49: 4809-12 (2006)
Nagoya City University
Accurate prediction of the relative potencies of members of a series of kinase inhibitors using molecular docking and MM-GBSA scoring.
J Med Chem 49: 4805-8 (2006)
Astrazeneca R&D Boston
Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists.
J Med Chem 49: 4801-4 (2006)
Merck Research Laboratories
Inhibition of HIV-1 integrase activity by synthetic peptides derived from the HIV-1 HXB2 Pol region of the viral genome.
Bioorg Med Chem Lett 16: 5199-202 (2006)
University Of Southern California
A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives.
Bioorg Med Chem Lett 16: 5057-61 (2006)
Eli Lilly
Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand.
Bioorg Med Chem Lett 16: 5001-4 (2006)
Merck
Identification of substituted 4-aminopiperidines and 3-aminopyrrolidines as potent MCH-R1 antagonists for the treatment of obesity.
Bioorg Med Chem Lett 16: 5445-50 (2006)
Procter And Gamble Pharmaceuticals
Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRalpha and beta.
Bioorg Med Chem Lett 16: 5231-7 (2006)
F. Hoffmann-La Roche
Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.
Bioorg Med Chem Lett 16: 5022-7 (2006)
Daiichi Asubio Medical Research Laboratories
Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors.
Bioorg Med Chem Lett 16: 5107-11 (2006)
Gnf
Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers.
Bioorg Med Chem Lett 16: 5244-8 (2006)
Institute Of Science And Technology
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.
Bioorg Med Chem Lett 16: 5122-6 (2006)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers.
Bioorg Med Chem Lett 16: 5112-7 (2006)
Gnf
Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity.
Bioorg Med Chem Lett 16: 5088-92 (2006)
Jerini
Homo-cysteinyl peptide inhibitors of the L1 metallo-beta-lactamase, and SAR as determined by combinatorial library synthesis.
Bioorg Med Chem Lett 16: 5169-75 (2006)
University Of Virginia
A general strategy for creating "inactive-conformation" abl inhibitors.
Chem Biol 13: 779-86 (2006)
The Scripps Research Institute
MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells.
Chem Biol 13: 711-22 (2006)
Gpc Biotech
A novel class of positive allosteric modulators of AMPA receptors: design, synthesis, and structure-activity relationships of 3-biphenyl-4-yl-4-cyano-5-ethyl-1-methyl-1H-pyrrole-2-carboxylic acid, LY2059346.
Bioorg Med Chem Lett 16: 5203-6 (2006)
Eli Lilly
Phenanthroquinolizidine alkaloids from the roots of Boehmeria pannosa potently inhibit hypoxia-inducible factor-1 in AGS human gastric cancer cells.
J Nat Prod 69: 1095-7 (2006)
Korea Research Institute Of Bioscience And Biotechnology
An apigenin-derived xanthine oxidase inhibitor from Palhinhaea cernua.
J Nat Prod 69: 1089-91 (2006)
Nanjing University
Antibiotic bisanthraquinones produced by a streptomycete isolated from a cyanobacterium associated with Ecteinascidia turbinata.
J Nat Prod 69: 1070-3 (2006)
University Of Rhode Island
Chemokine receptor CCR-5 inhibitors produced by Chaetomium globosum.
J Nat Prod 69: 1025-8 (2006)
Schering-Plough Research Institute
Biphenyl glycosides from the fruit of Pyracantha fortuneana.
J Nat Prod 69: 1022-4 (2006)
Shenyang Pharmaceutical University
Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors.
Bioorg Med Chem Lett 16: 4818-21 (2006)
Johnson & Johnson Pharmaceutical Research & Development
Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease.
Bioorg Med Chem Lett 16: 5183-9 (2006)
Hawaii Biotech
Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors.
Bioorg Med Chem Lett 16: 4728-32 (2006)
Procter And Gamble Pharmaceuticals
Synthesis and SAR of conformationally restricted inhibitors of soluble epoxide hydrolase.
Bioorg Med Chem Lett 16: 5212-6 (2006)
University Of California
Synthesis and biological activity of 5-aryl-4-(4-(5-methyl-1H-imidazol-4-yl)piperidin-1-yl)pyrimidine analogs as potent, highly selective, and orally bioavailable NHE-1 inhibitors.
Bioorg Med Chem Lett 16: 4796-9 (2006)
Pharmaceutical Research Institute
Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa.
Bioorg Med Chem Lett 16: 5176-82 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Tubulin polymerization inhibitors with a fluorinated phthalimide skeleton derived from thalidomide.
Bioorg Med Chem Lett 16: 4748-51 (2006)
The University Of Tokyo
The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.
Bioorg Med Chem Lett 16: 4723-7 (2006)
Glaxosmithkline
4-Amino-2-alkyl-butyramides as small molecule CCR2 antagonists with favorable pharmacokinetic properties.
Bioorg Med Chem Lett 16: 4715-22 (2006)
Merck Research Laboratories
Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-substituted phenyl alkyl imidazole-based inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha)).
Bioorg Med Chem Lett 16: 4752-6 (2006)
Kingston University
Design and synthesis of substituted quinolines as novel and selective melanin concentrating hormone antagonists as anti-obesity agents.
Bioorg Med Chem Lett 16: 5207-11 (2006)
Procter And Gamble Pharmaceuticals
From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
Bioorg Med Chem Lett 16: 5217-21 (2006)
Neurogen
Fatty acid synthase inhibitory activity of acylphloroglucinols isolated from Dryopteris crassirhizoma.
Bioorg Med Chem Lett 16: 4738-42 (2006)
Korea Research Institute Of Bioscience And Biotechnology
The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases.
J Am Chem Soc 128: 9699-704 (2006)
The Scripps Research Institute
Synthesis and biological evaluation of novel compounds within a class of 3-aminochroman derivatives with dual 5-HT1A receptor and serotonin transporter affinity.
J Med Chem 49: 4785-9 (2006)
Wyeth Research
Indenone derivatives: a novel template for peroxisome proliferator-activated receptor gamma (PPARgamma) agonists.
J Med Chem 49: 4781-4 (2006)
Korea Research Institute Of Chemical Technology
Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
J Med Chem 49: 4777-80 (2006)
University Of Bologna
Toward stable N4-modified neurotensins for NTS1-receptor-targeted tumor imaging with 99mTc.
J Med Chem 49: 4767-76 (2006)
National Center For Scientific Research Demokritos
Potent inhibitors of the Qi site of the mitochondrial respiration complex III.
J Med Chem 49: 4762-6 (2006)
Fmc Stine Research Center
Design, synthesis, and evaluation of proline and pyrrolidine based melanocortin receptor agonists. A conformationally restricted dipeptide mimic approach.
J Med Chem 49: 4745-61 (2006)
Procter & Gamble Pharmaceuticals
Benzimidazole derivatives bearing substituted biphenyls as hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors: structure-activity relationship studies and identification of a potent and highly selective inhibitor JTK-109.
J Med Chem 49: 4721-36 (2006)
Central Pharmaceutical Research Institute
Probing the role of the covalent linkage of ferrocene into a chloroquine template.
J Med Chem 49: 4707-14 (2006)
Unit£
Molecular tongs containing amino acid mimetic fragments: new inhibitors of wild-type and mutated HIV-1 protease dimerization.
J Med Chem 49: 4657-64 (2006)
Paris-Sud University
Fatty acid amide hydrolase inhibitors from virtual screening of the endocannabinoid system.
J Med Chem 49: 4650-6 (2006)
University Of Kuopio
3'-Substituted 7-halogenoindirubins, a new class of cell death inducing agents.
J Med Chem 49: 4638-49 (2006)
Cnrs
Structure-activity relationship of 6-methylidene penems bearing 6,5 bicyclic heterocycles as broad-spectrum beta-lactamase inhibitors: evidence for 1,4-thiazepine intermediates with C7 R stereochemistry by computational methods.
J Med Chem 49: 4623-37 (2006)
Wyeth Research
Hydrophobic effect and hydrogen bonds account for the improved activity of a complement inhibitor, compstatin.
J Med Chem 49: 4616-22 (2006)
University Of Pennsylvania
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
J Med Chem 49: 4606-15 (2006)
Infinity Pharmaceuticals
Synthesis and monoamine transporter binding properties of 2,3-cyclo analogues of 3beta-(4'-aminophenyl)-2beta-tropanemethanol.
J Med Chem 49: 4589-94 (2006)
Research Triangle Institute
Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease beta-site amyloid precursor protein cleaving enzyme (BACE).
J Med Chem 49: 4544-67 (2006)
Universite De Montreal At Succursale Centre-Ville
Discovery of small molecule integrin alphavbeta3 antagonists as novel anticancer agents.
J Med Chem 49: 4526-34 (2006)
University Of Southern California
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.
J Med Chem 49: 4512-6 (2006)
Vrije Universiteit Amsterdam
Simplified cyclic analogues of bastadin-5. Structure-activity relationships for modulation of the RyR1/FKBP12 Ca2+ channel complex.
J Med Chem 49: 4497-511 (2006)
University Of California
Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
J Med Chem 49: 4487-96 (2006)
Salk Institute
Sequence-based design and discovery of peptide inhibitors of HIV-1 integrase: insight into the binding mode of the enzyme.
J Med Chem 49: 4477-86 (2006)
Graduate School Of The Chinese Academy Of Sciences
Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists.
J Med Chem 49: 4459-69 (2006)
Abbott Laboratories
Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors.
J Med Chem 49: 4455-8 (2006)
Abbott Laboratories
Complexation of adamantyl compounds by beta-cyclodextrin and monoaminoderivatives.
J Phys Chem B 109: 9719-26 (2005)
Universidade De Santiago De Compostela
Synthesis and structure activity relationships of novel non-peptidic metallo-aminopeptidase inhibitors.
Bioorg Med Chem 14: 7241-57 (2006)
Enscmu
New spiro-piperidines as 5-HT2B receptor antagonists.
Bioorg Med Chem Lett 16: 4830-3 (2006)
Hopital Saint-Louis
Binding mode of new (thio)hydantoin inhibitors of fatty acid amide hydrolase: comparison with two original compounds, OL-92 and JP104.
Bioorg Med Chem Lett 16: 4772-6 (2006)
Fundp
Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines.
Bioorg Med Chem Lett 16: 4777-9 (2006)
Laboratory Of Medicinal Chemistry University Of Antwerp
Identification of novel pyrazole acid antagonists for the EP1 receptor.
Bioorg Med Chem Lett 16: 4767-71 (2006)
Glaxosmithkline
A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5).
Bioorg Med Chem Lett 16: 4792-5 (2006)
Astrazeneca R & D M£Lndal
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849.
Bioorg Med Chem Lett 16: 4872-8 (2006)
Glaxosmithkline
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849.
Bioorg Med Chem Lett 16: 4865-71 (2006)
Glaxosmithkline
Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6.
Bioorg Med Chem Lett 16: 4861-4 (2006)
Fujisawa Pharmaceutical
Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5).
Bioorg Med Chem Lett 16: 4788-91 (2006)
Astrazeneca R&D MöLndal
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
Bioorg Med Chem Lett 16: 4504-11 (2006)
Merck Research Laboratories
Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo.
Nat Chem Biol 2: 434-41 (2006)
The Scripps Research Institute
Arylisothiocyanato selective androgen receptor modulators (SARMs) for prostate cancer.
Bioorg Med Chem 14: 6525-38 (2006)
University Of Tennessee Health Science Center
Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity.
Bioorg Med Chem Lett 16: 4946-50 (2006)
University Of Arizona
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist.
Bioorg Med Chem Lett 16: 4856-60 (2006)
Faust Pharmaceuticals
Synthesis of tetramic and tetronic acids as beta-secretase inhibitors.
J Comb Chem 8: 480-90 (2006)
Darmstadt Technical University
Himbacine derived thrombin receptor (PAR-1) antagonists: structure-activity relationship of the lactone ring.
Bioorg Med Chem Lett 16: 4969-72 (2006)
Schering-Plough Research Institute
Pharmacophore-based virtual screening: the discovery of novel methionyl-tRNA synthetase inhibitors.
Bioorg Med Chem Lett 16: 4898-907 (2006)
Seoul National University
Propionylpiperazines as human melanocortin-4 receptor ligands.
Bioorg Med Chem Lett 16: 4800-3 (2006)
Neurocrine Biosciences
Identification and structure-based optimization of novel dihydropyrones as potent HCV RNA polymerase inhibitors.
Bioorg Med Chem Lett 16: 4834-8 (2006)
Pfizer
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2.
Bioorg Med Chem Lett 16: 4922-30 (2006)
Neurocrine Biosciences
Tetrahydroisoquinolines as MCH-R1 antagonists.
Bioorg Med Chem Lett 16: 4917-21 (2006)
Schering-Plough Research Institute
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
Bioorg Med Chem Lett 16: 4497-503 (2006)
Merck Research Laboratories
Imidazole-dioxolane compounds as isozyme-selective heme oxygenase inhibitors.
J Med Chem 49: 4437-41 (2006)
Queen'S University
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship.
J Med Chem 49: 4425-36 (2006)
Pfizer
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder. Synthesis and activity of functionalized glutaramides.
J Med Chem 49: 4409-24 (2006)
Pfizer
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
J Med Chem 49: 4384-91 (2006)
University Of Bonn
(R)-3'-(3-methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo[2,2,2]octane-3,5'-oxazolidin]-2'-one, a novel and potent alpha7 nicotinic acetylcholine receptor partial agonist displays cognitive enhancing properties.
J Med Chem 49: 4374-83 (2006)
Mitsubishi Pharma
Design and synthesis of novel 2-amino-5-hydroxyindole derivatives that inhibit human 5-lipoxygenase.
J Med Chem 49: 4327-32 (2006)
Friedrich Alexander University Erlangen
Structural requirements for the substrates of the H+/peptide cotransporter PEPT2 determined by three-dimensional quantitative structure-activity relationship analysis.
J Med Chem 49: 4286-96 (2006)
Martin-Luther-University Halle-Wittenberg
Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human beta-secretase inhibitors. Design, synthesis, and enzymatic BACE-1 and cell assays.
J Med Chem 49: 4275-85 (2006)
Universite De La Mediterranee
C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptor.
J Med Chem 49: 4269-74 (2006)
Purdue University
Docking and three-dimensional quantitative structure-activity relationship (3D QSAR) analyses of nonsteroidal progesterone receptor ligands.
J Med Chem 49: 4261-8 (2006)
Scientific Computing
From ligand to complexes: inhibition of human immunodeficiency virus type 1 integrase by beta-diketo acid metal complexes.
J Med Chem 49: 4248-60 (2006)
Università
Further structural exploration of trisubstituted asymmetric pyran derivatives (2S,4R,5R)-2-benzhydryl-5-benzylamino-tetrahydropyran-4-ol and their corresponding disubstituted (3S,6S) pyran derivatives: a proposed pharmacophore model for high-affinity interaction with the dopamine, serotonin, and no
J Med Chem 49: 4239-47 (2006)
Wayne State University
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.
J Med Chem 49: 4216-31 (2006)
Glaxosmithkline
Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.
J Med Chem 49: 4208-15 (2006)
Universit£
Acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase.
J Med Chem 49: 4183-95 (2006)
Cardiff University
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 3. Synthesis, pharmacokinetics, and in vivo potency.
J Med Chem 49: 4159-70 (2006)
Cardiovascular And Urogenital Centre Of Excellence For Drug Discovery
Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.
J Med Chem 49: 4140-52 (2006)
Ono Pharmaceutical
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
J Med Chem 49: 4127-39 (2006)
Novo Nordisk Research And Development
Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase.
J Med Chem 49: 4116-26 (2006)
Curacyte Chemistry
Design, synthesis, and structure-activity relationships of novel 2-substituted pyrazinoylguanidine epithelial sodium channel blockers: drugs for cystic fibrosis and chronic bronchitis.
J Med Chem 49: 4098-115 (2006)
Parion Sciences
Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models.
J Med Chem 49: 4085-97 (2006)
Università
Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists.
J Med Chem 49: 4072-84 (2006)
University Of Mississippi
Discovery of potent and orally available malonyl-CoA decarboxylase inhibitors as cardioprotective agents.
J Med Chem 49: 4055-8 (2006)
Chugai Pharma Usa
Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction.
J Med Chem 49: 4048-51 (2006)
Chinese Academy Of Sciences
Discovery of novel triazole-based opioid receptor antagonists.
J Med Chem 49: 4044-7 (2006)
University Of Medicine And Dentistry Of New Jersey And Umdnj Informatics Institute
Tetrahydrofluorenones with conformationally restricted side chains as selective estrogen receptor beta ligands.
Bioorg Med Chem Lett 16: 4462-6 (2006)
Merck Research Laboratories
Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides.
Bioorg Med Chem Lett 16: 4440-3 (2006)
National Research Institute Of Chinese Medicine
Synthesis and receptor binding properties of chimeric peptides containing a mu-opioid receptor ligand and nociceptin/orphanin FQ receptor ligand Ac-RYYRIK-amide.
Bioorg Med Chem Lett 16: 4839-41 (2006)
Tohoku Pharmaceutical University
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1.
Bioorg Med Chem Lett 16: 4450-7 (2006)
Neurocrine Biosciences
Macrolactin N, a new peptide deformylase inhibitor produced by Bacillus subtilis.
Bioorg Med Chem Lett 16: 4889-92 (2006)
Korea Research Institute Of Bioscience And Biotechnology
Carbonic anhydrase inhibitors. Inhibition of the cytosolic human isozymes I and II, and the transmembrane, tumor-associated isozymes IX and XII with substituted aromatic sulfonamides activatable in hypoxic tumors.
Bioorg Med Chem Lett 16: 4846-51 (2006)
Medical University Of Gdansk
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
Bioorg Med Chem Lett 16: 4936-40 (2006)
Abbott Laboratories
Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists.
Bioorg Med Chem Lett 16: 4543-7 (2006)
Schering-Plough Research Institute
Inhibition of the enzymatic activity of heme oxygenases by azole-based antifungal drugs.
J Pharmacol Exp Ther 319: 277-84 (2006)
Queen'S University
Modification of the clozapine structure by parallel synthesis.
Bioorg Med Chem Lett 16: 4548-53 (2006)
Schering-Plough Research Institute
Monocyclic thiophenes as protein tyrosine phosphatase 1B inhibitors: capturing interactions with Asp48.
Bioorg Med Chem Lett 16: 4941-5 (2006)
Wyeth Research
4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 3. Identification of lead candidate.
Bioorg Med Chem Lett 16: 4965-8 (2006)
Bayer Research Center
Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.
Bioorg Med Chem Lett 16: 4908-12 (2006)
Astrazeneca
Design and synthesis of new water-soluble tetrazolide derivatives of celecoxib and rofecoxib as selective cyclooxygenase-2 (COX-2) inhibitors.
Bioorg Med Chem Lett 16: 4483-7 (2006)
Tehran University Of Medical Sciences
N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1.
Bioorg Med Chem Lett 16: 4533-6 (2006)
Glaxosmithkline
Synthesis of a red-shifted fluorescence polarization probe for Hsp90.
Bioorg Med Chem Lett 16: 4515-8 (2006)
Memorial Sloan-Kettering Cancer Center
Synthesis of gallic acid based naphthophenone fatty acid amides as cathepsin D inhibitors.
Bioorg Med Chem Lett 16: 4603-8 (2006)
Institute Of Medicinal And Aromatic Plants
Studies towards the conception of new selective PPARbeta/delta ligands.
Bioorg Med Chem Lett 16: 4528-32 (2006)
Université
Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a series of 4-hydroxyphenyl ketones as potential inhibitors of 17beta-hydroxysteroid dehydrogenase type 3 (17beta-HSD3).
Bioorg Med Chem Lett 16: 4519-22 (2006)
Kingston University
Synthesis and evaluation of (2-phenethyl-2H-1,2,3-triazol-4-yl)(phenyl)methanones as Kv1.5 channel blockers for the treatment of atrial fibrillation.
Bioorg Med Chem Lett 16: 4629-32 (2006)
Procter & Gamble Pharmaceuticals
Potent 4-amino-5-azaindole factor VIIa inhibitors.
Bioorg Med Chem Lett 16: 4567-70 (2006)
Celera Genomics
Biotransformation of (-)-ambrox by cell suspension cultures of Actinidia deliciosa.
J Nat Prod 69: 957-9 (2006)
University Of Karachi
Quercetin as the active principle of Hypericum hircinum exerts a selective inhibitory activity against MAO-A: extraction, biological analysis, and computational study.
J Nat Prod 69: 945-9 (2006)
Sapienza University Of Rome
Synthesis of salvinorin A analogues as opioid receptor probes.
J Nat Prod 69: 914-8 (2006)
The University Of Iowa
Nitrogen-containing phorbol esters from Croton ciliatoglandulifer and their effects on cyclooxygenases-1 and -2.
J Nat Prod 69: 887-90 (2006)
Centro De Investigaciones QuíMicas De La Universidad AutóNoma Del Estado De Morelos
New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.
J Med Chem 49: 3990-3 (2006)
Vrije Universiteit Brussels
S-alkylated homocysteine derivatives: new inhibitors of human betaine-homocysteine S-methyltransferase.
J Med Chem 49: 3982-9 (2006)
Academy Of Sciences Of The Czech Republic
Structural studies on bioactive compounds. 40.(1) Synthesis and biological properties of fluoro-, methoxyl-, and amino-substituted 3-phenyl-4H-1-benzopyran-4-ones and a comparison of their antitumor activities with the activities of related 2-phenylbenzothiazoles.
J Med Chem 49: 3973-81 (2006)
University Of Nottingham
Activation of murine RNase L by isopolar 2'-phosphonate analogues of 2',5' oligoadenylates.
J Med Chem 49: 3955-62 (2006)
Academy Of Sciences Of The Czech Republic
2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.
J Med Chem 49: 3938-47 (2006)
Laboratoire De Chimie Th�Rapeutique
Exploration of orally available calpain inhibitors 2: peptidyl hemiacetal derivatives.
J Med Chem 49: 3926-32 (2006)
Senju Pharmaceutical
4-amido-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-ones as new potent and selective human A3 adenosine receptor antagonists. synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
J Med Chem 49: 3916-25 (2006)
Università
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-5-aryl thiophenes as a new class of potent antitubulin agents.
J Med Chem 49: 3906-15 (2006)
Universit£
Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns.
J Med Chem 49: 3888-96 (2006)
National Institute Of Diabetes And Digestive And Kidney Diseases
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.
J Med Chem 49: 3857-71 (2006)
Serono Pharmaceutical Research Institute
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
J Med Chem 49: 3832-49 (2006)
Abbott Laboratories
Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists.
J Med Chem 49: 3809-25 (2006)
Takeda Pharmaceutical
Synthesis, molecular characterization, and biological activity of novel synthetic derivatives of chromen-4-one in human cancer cells.
J Med Chem 49: 3800-8 (2006)
University Of Pune
Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic.
J Med Chem 49: 3774-89 (2006)
Incyte
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors.
J Med Chem 49: 3770-3 (2006)
Abbott Laboratories
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.
J Med Chem 49: 3766-9 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy.
J Med Chem 49: 3759-62 (2006)
University Of Michigan
3-arylimino-2-indolones are potent and selective galanin GAL3 receptor antagonists.
J Med Chem 49: 3757-8 (2006)
Lundbeck Research Usa
A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties.
J Med Chem 49: 3753-6 (2006)
Neurocrine Biosciences
Synthesis and monoamine transporter affinity of front bridged tricyclic 3beta-(4'-halo or 4'-methyl)phenyltropanes bearing methylene or carbomethoxymethylene on the bridge to the 2beta-position.
Bioorg Med Chem Lett 16: 4661-3 (2006)
Emory University
High affinity inhibitors of the dopamine transporter (DAT): novel biotinylated ligands for conjugation to quantum dots.
Bioorg Med Chem Lett 16: 4664-7 (2006)
Vanderbilt University
Synthesis of novel keto-ACE analogues as domain-selective angiotensin I-converting enzyme inhibitors.
Bioorg Med Chem Lett 16: 4612-5 (2006)
University Of Cape Town
3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors.
Bioorg Med Chem Lett 16: 4620-3 (2006)
Merck Research Laboratories
Synthesis and molecular modeling of a lisinopril-tryptophan analogue inhibitor of angiotensin I-converting enzyme.
Bioorg Med Chem Lett 16: 4616-9 (2006)
University Of Cape Town
Rational design of inhibitors that bind to inactive kinase conformations.
Nat Chem Biol 2: 358-64 (2006)
Novartis Research Foundation
Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc.
Bioorg Med Chem Lett 16: 4633-7 (2006)
Pfizer
Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
Bioorg Med Chem Lett 16: 4638-40 (2006)
Gedeon Richter
Synthesis and evaluation of novel 1-(2-acylhydrazinocarbonyl)-cycloalkyl carboxamides as interleukin-1beta converting enzyme (ICE) inhibitors.
Bioorg Med Chem Lett 16: 4233-6 (2006)
Procter & Gamble Pharmaceuticals
Design, synthesis, and biochemical evaluation of novel cruzain inhibitors with potential application in the treatment of Chagas' disease.
Bioorg Med Chem Lett 16: 4405-9 (2006)
Baylor University
Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners.
Bioorg Med Chem Lett 16: 4291-5 (2006)
University Of Kentucky
Amide-substituted farnesylcysteine analogs as inhibitors of human isoprenylcysteine carboxyl methyltransferase.
Bioorg Med Chem Lett 16: 4420-3 (2006)
Purdue University
Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 16: 4674-8 (2006)
Neurocrine Biosciences
Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18).
Bioorg Med Chem Lett 16: 4679-85 (2006)
Mclean Hospital
Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
Bioorg Med Chem Lett 16: 4686-91 (2006)
Glaxosmithkline
Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists.
Bioorg Med Chem Lett 16: 4652-6 (2006)
Merck Research Laboratories
Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors.
Biochemistry 45: 7474-82 (2006)
Abbott Laboratories
Combinatorial chemistry identifies high-affinity peptidomimetics against alpha4beta1 integrin for in vivo tumor imaging.
Nat Chem Biol 2: 381-9 (2006)
University Of California
Small molecule-based reversible reprogramming of cellular lifespan.
Nat Chem Biol 2: 369-74 (2006)
Korea Advanced Institute Of Science And Technology
Synthesis of biotinylated photoaffinity probes based on arylsulfonamide gamma-secretase inhibitors.
Bioorg Med Chem Lett 16: 4184-9 (2006)
University Of Tokyo
Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists.
Bioorg Med Chem Lett 16: 4668-73 (2006)
Procter & Gamble Pharmaceuticals
Discovery of protein-protein binding disruptors using multi-component condensations small molecules.
Bioorg Med Chem Lett 16: 3998-4001 (2006)
Pierre Fabre Urologie
Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors.
Bioorg Med Chem Lett 16: 4283-6 (2006)
Virginia Commonwealth University
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.
Bioorg Med Chem Lett 16: 4163-8 (2006)
Chiron
4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters.
Bioorg Med Chem Lett 16: 4321-5 (2006)
F. Hoffmann-La Roche
Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists.
Bioorg Med Chem Lett 16: 4237-42 (2006)
Neurocrine Biosciences
Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: achieving selectivity against the mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors.
Bioorg Med Chem Lett 16: 4305-10 (2006)
F. Hoffmann-La Roche
Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.
Bioorg Med Chem Lett 16: 4339-44 (2006)
Pfizer
Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of N,N'-bis[2-oxo-2H-benzopyran]-3-carboxamides.
Bioorg Med Chem Lett 16: 4135-40 (2006)
Universit£
Design and synthesis of potent, non-peptidic inhibitors of HPTPbeta.
Bioorg Med Chem Lett 16: 4252-6 (2006)
Procter & Gamble Pharmaceuticals
N-hydroxyurea--a versatile zinc binding function in the design of metalloenzyme inhibitors.
Bioorg Med Chem Lett 16: 4316-20 (2006)
Università
1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors.
Bioorg Med Chem Lett 16: 4266-71 (2006)
Abbott Laboratories
Synthesis, structural reassignment, and biological activity of type B MAO inhibitors based on the 5H-indeno[1,2-c]pyridazin-5-one core.
J Med Chem 49: 3743-7 (2006)
FacultéS Universitaires N.D. De La Paix
Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.
J Med Chem 49: 3719-42 (2006)
Amgen
Synthesis and pharmacological evaluation of novel nitrobenzenic thromboxane modulators as antiplatelet agents acting on both the alpha and beta isoforms of the human thromboxane receptor.
J Med Chem 49: 3701-9 (2006)
University Of LièGe
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.
J Med Chem 49: 3682-92 (2006)
Cv Therapeutics
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
J Med Chem 49: 3659-66 (2006)
Abbott Laboratories
6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.
J Med Chem 49: 3653-8 (2006)
Universidad De Santiago De Compostela
Human PEPT1 pharmacophore distinguishes between dipeptide transport and binding.
J Med Chem 49: 3636-44 (2006)
Pharmaceutical Research Institute
Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists.
J Med Chem 49: 3628-35 (2006)
Friedrich-Alexander University
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
J Med Chem 49: 3614-27 (2006)
Merck Research Laboratories
A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability.
J Med Chem 49: 3581-94 (2006)
Pfizer
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.
J Med Chem 49: 3563-80 (2006)
Abbott Laboratories
The combi-targeting concept: synthesis of stable nitrosoureas designed to inhibit the epidermal growth factor receptor (EGFR).
J Med Chem 49: 3544-52 (2006)
Mcgill University Health Center/Royal Victoria Hospital
Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III.
J Med Chem 49: 3536-43 (2006)
Salk Institute
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.
J Med Chem 49: 3520-35 (2006)
Abbott Laboratories
Mapping the melatonin receptor. 7. Subtype selective ligands based on beta-substituted N-acyl-5-methoxytryptamines and beta-substituted N-acyl-5-methoxy-1-methyltryptamines.
J Med Chem 49: 3509-19 (2006)
University Of Athens
Inhibition of carbonic anhydrase-II by sulfamate and sulfamide groups: an investigation involving direct thermodynamic binding measurements.
J Med Chem 49: 3496-500 (2006)
Johnson & Johnson Pharmaceutical Research & Development
Discovery of a novel family of SARS-CoV protease inhibitors by virtual screening and 3D-QSAR studies.
J Med Chem 49: 3485-95 (2006)
National Tsing Hua University
Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor.
J Med Chem 49: 3467-77 (2006)
The University Of Melbourne
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.
J Med Chem 49: 3454-66 (2006)
University Of Innsbruck
Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.
J Med Chem 49: 3440-3 (2006)
Peking University
Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.
J Med Chem 49: 3432-5 (2006)
University Of Michigan
Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability.
Bioorg Med Chem Lett 16: 4311-5 (2006)
F. Hoffmann-La Roche
The development of novel 1,2-dihydro-pyrimido[4,5-c]pyridazine based inhibitors of lymphocyte specific kinase (Lck).
Bioorg Med Chem Lett 16: 4257-61 (2006)
Procter And Gamble Pharmaceuticals
beta-Secretase inhibitors: modification at the P4 position and improvement of inhibitory activity in cultured cells.
Bioorg Med Chem Lett 16: 4354-9 (2006)
Kyoto Pharmaceutical University
Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: impacting hERG liability via aryl modifications.
Bioorg Med Chem Lett 16: 4262-5 (2006)
Schering-Plough Research Institute
Discovery of potent CRTh2 (DP2) receptor antagonists.
Bioorg Med Chem Lett 16: 4287-90 (2006)
Astrazeneca R&D Charnwood
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.
Bioorg Med Chem Lett 16: 4296-9 (2006)
Celera Genomics
p38 MAP kinase inhibitors. Part 3: SAR on 3,4-dihydropyrimido[4,5-d]pyrimidin-2-ones and 3,4-dihydropyrido[4,3-d]pyrimidin-2-ones.
Bioorg Med Chem Lett 16: 4400-4 (2006)
Merck Research Laboratories
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.
Bioorg Med Chem Lett 16: 4371-5 (2006)
Abbott Laboratories
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1.
Bioorg Med Chem Lett 16: 4376-80 (2006)
The Genomics Institute Of The Novartis Research Foundation
The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production.
Bioorg Med Chem Lett 16: 4360-5 (2006)
Procter And Gamble Pharmaceuticals
Identification of potent and highly selective chiral tri-amine and tetra-amine mu opioid receptors ligands: an example of lead optimization using mixture-based libraries.
Bioorg Med Chem Lett 16: 4331-8 (2006)
Institute For Molecular Studies
The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT2C receptor agonist.
Bioorg Med Chem Lett 16: 4130-4 (2006)
Athersys
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.
Bioorg Med Chem Lett 16: 4349-53 (2006)
Pfizer
Synthesis and biochemical evaluation of a range of potent benzyl imidazole-based compounds as potential inhibitors of the enzyme complex 17alpha-hydroxylase/17,20-lyase (P450(17alpha)).
Bioorg Med Chem Lett 16: 4011-5 (2006)
Kingston University
Analysis of complexes of inhibitors with Cryptosporidium hominis DHFR leads to a new trimethoprim derivative.
Bioorg Med Chem Lett 16: 4366-70 (2006)
Dartmouth College
CA224, a non-planar analogue of fascaplysin, inhibits Cdk4 but not Cdk2 and arrests cells at G0/G1 inhibiting pRB phosphorylation.
Bioorg Med Chem Lett 16: 4272-8 (2006)
De Montfort University
N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.
Bioorg Med Chem Lett 16: 4345-8 (2006)
Pfizer
Structure-based design of indole propionic acids as novel PPARalpha/gamma co-agonists.
Bioorg Med Chem Lett 16: 4016-20 (2006)
F. Hoffmann-La Roche
Multiple conformations of phosphodiesterase-5: implications for enzyme function and drug development.
J Biol Chem 281: 21469-79 (2006)
University Of North Carolina At Chapel Hill
Synthesis and efficacy of 1-[bis(4-fluorophenyl)-methyl]piperazine derivatives for acetylcholinesterase inhibition, as a stimulant of central cholinergic neurotransmission in Alzheimer's disease.
Bioorg Med Chem Lett 16: 3932-6 (2006)
University Of Mysore
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.
Bioorg Med Chem Lett 16: 4326-30 (2006)
Abbott Laboratories
7-(aryl/heteroaryl-2-ylethynyl)-4-phenylamino-3-quinolinecarbonitriles as new Src kinase inhibitors: addition of water solubilizing groups.
Bioorg Med Chem Lett 16: 3993-7 (2006)
Wyeth Research
CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo.
Mol Cancer Ther 5: 1309-17 (2006)
Celera Genomics
Estrogen receptor beta-subtype selective tetrahydrofluorenones: use of a fused pyrazole as a phenol bioisostere.
Bioorg Med Chem Lett 16: 3896-901 (2006)
Merck Research Laboratories
P2-P4 macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease.
Bioorg Med Chem Lett 16: 3960-5 (2006)
Schering-Plough Research Institute
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Bioorg Med Chem Lett 16: 4141-7 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.
Bioorg Med Chem Lett 16: 3906-12 (2006)
Glaxosmithkline
Amino substituted analogs of 1-phenyl-3-phenylimino-2-indolones with potent galanin Gal3 receptor binding affinity and improved solubility.
Bioorg Med Chem Lett 16: 3950-4 (2006)
Lundbeck Research Usa
Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors.
Bioorg Med Chem Lett 16: 3937-42 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and pharmacological characterization of novel fluorescent histamine H2-receptor ligands derived from aminopotentidine.
Bioorg Med Chem Lett 16: 3886-90 (2006)
The University Of Kansas
The synthesis and SAR of 2-arylsulfanylphenyl-1-oxyalkylamino acids as GlyT-1 inhibitors.
Bioorg Med Chem Lett 16: 3981-4 (2006)
H. Lundbeck
Discovery of 3-hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles as potent MEK1 inhibitors.
Bioorg Med Chem Lett 16: 3975-80 (2006)
Valeant Pharmaceutical Research And Development
Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.
Bioorg Med Chem Lett 16: 4085-9 (2006)
Celera Genomics
Design and synthesis of butynyloxyphenyl beta-sulfone piperidine hydroxamates as TACE inhibitors.
Bioorg Med Chem Lett 16: 3927-31 (2006)
Wyeth Research
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.
Bioorg Med Chem Lett 16: 4068-70 (2006)
Korea Research Institute Of Bioscience And Biotechnology
Design, synthesis, and biological evaluation of novel tricyclic HIV-1 integrase inhibitors by modification of its pyridine ring.
Bioorg Med Chem Lett 16: 3985-8 (2006)
Gilead Sciences
Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors.
Bioorg Med Chem Lett 16: 3989-92 (2006)
Gilead Sciences
Design and synthesis of selective alpha1B adrenoceptor antagonists.
Bioorg Med Chem Lett 16: 4045-7 (2006)
Toray Industries
Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.
J Med Chem 49: 3421-5 (2006)
Universita Di Siena
Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior.
J Med Chem 49: 3416-20 (2006)
University Of Naples Federico Ii
Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists.
J Med Chem 49: 3402-11 (2006)
Johnson & Johnson Pharmaceutical
Synthesis and structure-activity relationships of linear and conformationally constrained peptide analogues of CIYKYY as Src tyrosine kinase inhibitors.
J Med Chem 49: 3395-401 (2006)
University Of Rhode Island
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.
J Med Chem 49: 3362-7 (2006)
Pfizer
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
J Med Chem 49: 3354-61 (2006)
Leiden University
Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids.
J Med Chem 49: 3345-53 (2006)
University Of Zurich
Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
J Med Chem 49: 3332-44 (2006)
Vanderbilt University School Of Medicine
A combination of docking/dynamics simulations and pharmacophoric modeling to discover new dual c-Src/Abl kinase inhibitors.
J Med Chem 49: 3278-86 (2006)
Università
Synthesis and pharmacological characterization of nicotinic acetylcholine receptor properties of (+)- and (-)-pyrido-[3,4-b]homotropanes.
J Med Chem 49: 3244-50 (2006)
Research Triangle Institute
Conformationally constrained analogues of diacylglycerol. 26. Exploring the chemical space surrounding the C1 domain of protein kinase C with DAG-lactones containing aryl groups at the sn-1 and sn-2 positions.
J Med Chem 49: 3185-203 (2006)
National Cancer Institute-Frederick
New ligands with affinity for the alpha4beta2 subtype of nicotinic acetylcholine receptors. Synthesis, receptor binding, and 3D-QSAR modeling.
J Med Chem 49: 3159-71 (2006)
Neurosearch
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
J Med Chem 49: 3116-35 (2006)
Predix Pharmaceuticals
Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
J Med Chem 49: 3101-15 (2006)
University Of Regensburg
Construction of human ghrelin receptor (hGHS-R1a) model using a fragmental prediction approach and validation through docking analysis.
J Med Chem 49: 3077-85 (2006)
Universit£
cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization.
J Med Chem 49: 3068-76 (2006)
Pfizer
Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents.
J Med Chem 49: 3064-7 (2006)
University Of Messina
Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.
J Med Chem 49: 3056-9 (2006)
Johnson & Johnson Pharmaceutical Research & Development
Discovery of proline sulfonamides as potent and selective hepatitis C virus NS5b polymerase inhibitors. Evidence for a new NS5b polymerase binding site.
J Med Chem 49: 3052-5 (2006)
Wyeth Research
New potent P-glycoprotein inhibitors carrying a polycyclic scaffold.
J Med Chem 49: 3049-51 (2006)
University Of Bologna
Effect of substitution on novel tricyclic HIV-1 integrase inhibitors.
Bioorg Med Chem Lett 16: 4031-5 (2006)
Gilead Sciences
A gatekeeper residue for inhibitor sensitization of protein tyrosine phosphatases.
Bioorg Med Chem Lett 16: 4002-6 (2006)
Amherst College
Synthesis and biological activity of nociceptin/orphanin FQ(1-13)NH2 analogues modified in 9 and/or 13 position.
Bioorg Med Chem Lett 16: 4071-4 (2006)
University Of Chemical Technology And Metallurgy
Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.
Bioorg Med Chem Lett 16: 4036-40 (2006)
Celera
Identification of thieno[3,2-b]pyrroles as allosteric inhibitors of hepatitis C virus NS5B polymerase.
Bioorg Med Chem Lett 16: 4026-30 (2006)
Mrl Rome
5-benzylidene-hydantoins as new EGFR inhibitors with antiproliferative activity.
Bioorg Med Chem Lett 16: 4021-5 (2006)
Università
Dibasic non-imidazole histamine H3 receptor antagonists with a rigid biphenyl scaffold.
Bioorg Med Chem Lett 16: 4063-7 (2006)
Universit£
Identification of metabolites of the tryptase inhibitor CRA-9249: observation of a metabolite derived from an unexpected hydroxylation pathway.
Bioorg Med Chem Lett 16: 4053-8 (2006)
Celera Genomics
Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: novel classes of histone deacetylase inhibitors.
Bioorg Med Chem Lett 16: 4048-52 (2006)
Methylgene
Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors.
Bioorg Med Chem Lett 16: 3793-6 (2006)
Virginia Commonwealth University
Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity.
J Biol Chem 281: 24818-30 (2006)
German Cancer Research Center
Putative therapeutic agents for the learning and memory deficits of people with Down syndrome.
Bioorg Med Chem Lett 16: 3772-6 (2006)
Research Center Idrtech
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.
Bioorg Med Chem Lett 16: 3735-9 (2006)
Merck Research Laboratories
Dipeptide vinyl sultams: synthesis via the Wittig-Horner reaction and activity against papain, falcipain-2 and Plasmodium falciparum.
Bioorg Med Chem Lett 16: 4115-9 (2006)
University Of Lisbon
Nepsilon-thioacetyl-lysine: a multi-facet functional probe for enzymatic protein lysine Nepsilon-deacetylation.
Bioorg Med Chem Lett 16: 3651-6 (2006)
University Of Akron
Structure-activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists.
Bioorg Med Chem Lett 16: 3657-62 (2006)
Glaxosmithkline
Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.
Bioorg Med Chem Lett 16: 3784-8 (2006)
Glaxosmithkline
Synthesis and structure-activity relationships of 3,4-diaminocyclobut-3-ene-1,2-dione CXCR2 antagonists.
Bioorg Med Chem Lett 16: 4107-10 (2006)
Pharmacopeia Drug Discovery
New pyrrolopyrimidin-6-yl benzenesulfonamides: potent A2B adenosine receptor antagonists.
Bioorg Med Chem Lett 16: 3642-5 (2006)
RhôNe-Poulenc Rorer
Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents.
Bioorg Med Chem Lett 16: 3713-8 (2006)
Amgen
Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes.
Bioorg Med Chem Lett 16: 3679-83 (2006)
Merck Research Laboratories
Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor.
Bioorg Med Chem Lett 16: 3693-6 (2006)
Neurocrine Biosciences
Privileged structure based ligands for melanocortin receptors--4,4-disubstituted piperidine derivatives.
Bioorg Med Chem Lett 16: 3843-6 (2006)
Eli Lilly
Pharmacological characterization of the competitive GLUK5 receptor antagonist decahydroisoquinoline LY466195 in vitro and in vivo.
J Pharmacol Exp Ther 318: 772-81 (2006)
Eli Lilly
Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists.
Bioorg Med Chem Lett 16: 3674-8 (2006)
Schering-Plough Research Institute
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.
Bioorg Med Chem Lett 16: 3635-8 (2006)
Merck Research Laboratories
Synthesis and structure-activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists.
Bioorg Med Chem Lett 16: 3668-73 (2006)
Schering-Plough Research Institute
Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells.
J Med Chem 49: 3012-8 (2006)
Universit£
Design and synthesis of substrate and intermediate analogue inhibitors of S-ribosylhomocysteinase.
J Med Chem 49: 3003-11 (2006)
The Ohio State University
Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase.
J Med Chem 49: 2998-3002 (2006)
The Scripps Research Institute
Synthesis and biological evaluation of glycosidase inhibitors: gem-difluoromethylenated nojirimycin analogues.
J Med Chem 49: 2989-97 (2006)
Chinese Academy Of Sciences
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
J Med Chem 49: 2953-68 (2006)
Celera
Application of the Goldilocks effect to the design of potent and selective inhibitors of phenylethanolamine N-methyltransferase: balancing pKa and steric effects in the optimization of 3-methyl-1,2,3,4-tetrahydroisoquinoline inhibitors by beta-fluorination.
J Med Chem 49: 2939-52 (2006)
University Of Kansas
New 2-alkylidene 1alpha,25-dihydroxy-19-norvitamin D3 analogues of high intestinal activity: synthesis and biological evaluation of 2-(3'-alkoxypropylidene) and 2-(3'-hydroxypropylidene) derivatives.
J Med Chem 49: 2909-20 (2006)
University Of Wisconsin-Madison
Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.
J Med Chem 49: 2898-908 (2006)
Boehringer Ingelheim Pharmaceuticals
NO-donor phenols: a new class of products endowed with antioxidant and vasodilator properties.
J Med Chem 49: 2886-97 (2006)
Università
Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
J Med Chem 49: 2876-85 (2006)
Mgi Pharma
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
J Med Chem 49: 2868-75 (2006)
University Of Arizona Tucson
2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists.
J Med Chem 49: 2861-7 (2006)
Leiden/Amsterdam Center For Drug Research
The first potent inhibitor of mammalian group X secreted phospholipase A2: elucidation of sites for enhanced binding.
J Med Chem 49: 2858-60 (2006)
University Of Washington
3-Substituted gem-cyclohexane sulfone based gamma-secretase inhibitors for Alzheimer's disease: conformational analysis and biological activity.
Bioorg Med Chem Lett 16: 3839-42 (2006)
Merck Sharp And Dohme Research Laboratories
Development of N-4,6-pyrimidine-N-alkyl-N'-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase.
Bioorg Med Chem Lett 16: 3646-50 (2006)
Procter & Gamble Pharmaceuticals
Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.
Bioorg Med Chem Lett 16: 3755-60 (2006)
Bristol-Myers Squibb
Synthesis of a potential photoactivatable anandamide analog.
Bioorg Med Chem Lett 16: 3765-8 (2006)
University Of Montpellier
Cyclobutane derivatives as potent NK1 selective antagonists.
Bioorg Med Chem Lett 16: 3859-63 (2006)
Schering-Plough Research Institute
Novel gamma-secretase inhibitors discovered by library screening of in-house synthetic natural product intermediates.
Bioorg Med Chem Lett 16: 3813-6 (2006)
University Of Tokyo
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.
Bioorg Med Chem Lett 16: 3706-12 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4.
Bioorg Med Chem Lett 16: 3688-92 (2006)
Lanzhou University
Critical modifications of the ISO-1 scaffold improve its potent inhibition of macrophage migration inhibitory factor (MIF) tautomerase activity.
Bioorg Med Chem Lett 16: 3376-9 (2006)
Institute For Medical Research
Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.
Bioorg Med Chem Lett 16: 3639-41 (2006)
Johnson & Johnson Pharmaceutical Research & Development
Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Bioorg Med Chem Lett 16: 3684-7 (2006)
Merck
Identification of potent 5-pyrimidinyl-2-aminothiazole CDK4, 6 inhibitors with significant selectivity over CDK1, 2, 5, 7, and 9.
Bioorg Med Chem Lett 16: 3751-4 (2006)
Banyu Tsukuba Research Institute
Structure-guided design of peptide-based tryptase inhibitors.
Biochemistry 45: 5964-73 (2006)
Celera
Design of cyclic peptides with agonist activity at melanocortin receptor-4.
Bioorg Med Chem Lett 16: 3723-6 (2006)
Asahi Kasei Pharma
3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors.
Bioorg Med Chem Lett 16: 3789-92 (2006)
Chiron
Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.
Bioorg Med Chem Lett 16: 3740-4 (2006)
Abbott Laboratories
Nanomolar inhibition of the enterobactin biosynthesis enzyme, EntE: synthesis, substituent effects, and additivity.
Bioorg Med Chem Lett 16: 3802-5 (2006)
University Of North Carolina
Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines.
Bioorg Med Chem Lett 16: 3777-9 (2006)
Glaxosmithkline
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Bioorg Med Chem Lett 16: 3371-5 (2006)
National Institute On Drug Abuse
Synthesis and SAR of novel histamine H3 receptor antagonists.
Bioorg Med Chem Lett 16: 3415-8 (2006)
Eli Lilly
Design, synthesis and evaluation of novel uracil amino acid conjugates for the inhibition of Trypanosoma cruzi dUTPase.
Bioorg Med Chem Lett 16: 3809-12 (2006)
Cardiff University
Arylpiperazines with N-acylated amino acids as 5-HT1A receptor ligands.
Bioorg Med Chem Lett 16: 3406-10 (2006)
University Of Montpellier
Strategy for discovering chemical inhibitors of human cyclophilin a: focused library design, virtual screening, chemical synthesis and bioassay.
J Comb Chem 8: 326-37 (2006)
East China Univesity Of Science And Technology
Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor.
J Pharmacol Exp Ther 318: 657-65 (2006)
Wyeth Research
Bivalent inhibitors of glutathione S-transferase: the effect of spacer length on isozyme selectivity.
Bioorg Med Chem Lett 16: 3780-3 (2006)
Syntrix Biosytems
Inhibition of chloroplast electron transport reactions by trifluralin and diallate.
Plant Physiol 60: 840-4 (1977)
The University Of Michigan
Efforts toward oral bioavailability in factor VIIa inhibitors.
Bioorg Med Chem Lett 16: 3829-32 (2006)
Celera
A highly selective kappa-opioid receptor agonist with low addictive potential and dependence liability.
Bioorg Med Chem Lett 16: 3609-13 (2006)
Kaist
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-benzyl and N-1-[3-methylbutyl]-4-hydroxy-1,8-naphthyridon-3-yl benzothiadiazine analogs containing substituents on the aromatic ring.
Bioorg Med Chem Lett 16: 3833-8 (2006)
Abbott Laboratories
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides.
Bioorg Med Chem Lett 16: 3367-70 (2006)
Abbott Laboratories
Privileged structure based ligands for melanocortin-4 receptors--aliphatic piperazine derivatives.
Bioorg Med Chem Lett 16: 3449-53 (2006)
Eli Lilly
Synthesis and SAR of 1,3-disubstituted cyclohexylmethyl urea and amide derivatives as non-peptidic motilin receptor antagonists.
Bioorg Med Chem Lett 16: 3362-6 (2006)
Johnson & Johnson Pharmaceutical Research & Development
Racemic and chiral sulfoxides as potential prodrugs of 4-pyrone COX-2 inhibitors.
Bioorg Med Chem Lett 16: 3605-8 (2006)
RhôNe-Poulenc Rorer
Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity.
Bioorg Med Chem Lett 16: 3463-8 (2006)
Johnson & Johnson Pharmaceutical
Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors.
Bioorg Med Chem Lett 16: 3614-7 (2006)
Arpida
Discovery and SAR of oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers.
Bioorg Med Chem Lett 16: 3424-9 (2006)
Abbott Laboratories
Thiazolo[5,4-f]quinazolin-9-ones, inhibitors of glycogen synthase kinase-3.
Bioorg Med Chem Lett 16: 3419-23 (2006)
Université
Heteroaryl substituted bis-trifluoromethyl carbinols as malonyl-CoA decarboxylase inhibitors.
Bioorg Med Chem Lett 16: 3484-8 (2006)
Chugai Pharma
Identification and characterization of 4-aryl-3,4-dihydropyrimidin-2(1H)-ones as inhibitors of the fatty acid transporter FATP4.
Bioorg Med Chem Lett 16: 3504-9 (2006)
Millennium Pharmaceuticals
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.
Bioorg Med Chem Lett 16: 3434-9 (2006)
Celera Genomics
Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-acyl aromatic alpha-amino acids.
Bioorg Med Chem Lett 16: 3459-62 (2006)
Ambrilia Biopharma
Sundaicumones A and B, polyprenylated acylphloroglucinol derivatives from Calophyllumsundaicum with weak activity against the glucocorticoid receptor.
J Nat Prod 69: 707-9 (2006)
Merlion Pharmaceuticals
Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay.
J Nat Prod 69: 700-3 (2006)
University Of Illinois At Chicago
Vanillic acid glycoside and quinic acid derivatives from Gardeniae Fructus.
J Nat Prod 69: 600-3 (2006)
Korea Institute Of Science And Technology
Bioassay for the identification of natural product-based activators of peroxisome proliferator-activated receptor-gamma (PPARgamma): the marine sponge metabolite psammaplin A activates PPARgamma and induces apoptosis in human breast tumor cells.
J Nat Prod 69: 547-52 (2006)
University Of Mississippi
Serotonergic activity-guided phytochemical investigation of the roots of Angelica sinensis.
J Nat Prod 69: 536-41 (2006)
University Of Illinois At Chicago
Synthesis of biphenyltrienes as probes for beta-amyloid plaques.
J Med Chem 49: 2841-4 (2006)
University Of Pennsylvania
Biological evaluation of bishydroxymethyl-substituted cage dimeric 1,4-dihydropyridines as a novel class of p-glycoprotein modulating agents in cancer cells.
J Med Chem 49: 2838-40 (2006)
Martin-Luther-University Halle-Wittenberg
Discovery of a piperidine-4-carboxamide CCR5 antagonist (TAK-220) with highly potent Anti-HIV-1 activity.
J Med Chem 49: 2784-93 (2006)
Takeda Pharmaceutical
Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
J Med Chem 49: 2758-71 (2006)
Glaxosmithkline
Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication.
J Med Chem 49: 2750-7 (2006)
Schering-Plough Research Institute
Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX.
J Med Chem 49: 2743-9 (2006)
University Of Namur
[2-11C]isopropyl-, [1-11C]ethyl-, and [11C]methyl-labeled phenoxyphenyl acetamide derivatives as positron emission tomography ligands for the peripheral benzodiazepine receptor: radiosynthesis, uptake, and in vivo binding in brain.
J Med Chem 49: 2735-42 (2006)
National Institute Of Radiological Sciences
Novel benzofuran derivatives for PET imaging of beta-amyloid plaques in Alzheimer's disease brains.
J Med Chem 49: 2725-30 (2006)
Nagasaki University
Structure-based drug design of a novel family of PPARgamma partial agonists: virtual screening, X-ray crystallography, and in vitro/in vivo biological activities.
J Med Chem 49: 2703-12 (2006)
National Health Research Institutes
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.
J Med Chem 49: 2689-702 (2006)
National Institute Of Diabetes And Digestive And Kidney Diseases
Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta.
J Med Chem 49: 2681-8 (2006)
Kyoto University
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
J Med Chem 49: 2673-6 (2006)
University Of Illinois At Chicago
Design, synthesis, and progress toward optimization of potent small molecule antagonists of CC chemokine receptor 8 (CCR8).
J Med Chem 49: 2669-72 (2006)
Millennium Pharmaceuticals
Stable benzotriazole esters as mechanism-based inactivators of the severe acute respiratory syndrome 3CL protease.
Chem Biol 13: 261-8 (2006)
Academia Sinica
Analysis of HIV-1 CRF_01 A/E protease inhibitor resistance: structural determinants for maintaining sensitivity and developing resistance to atazanavir.
Biochemistry 45: 5468-77 (2006)
Johnson & Johnson Pharmaceutical
Discovery of novel isothiazole inhibitors of the TrkA kinase: structure-activity relationship, computer modeling, optimization, and identification of highly potent antagonists.
Bioorg Med Chem Lett 16: 3444-8 (2006)
Pfizer
Synthesis and SAR of alpha-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors.
Bioorg Med Chem Lett 16: 3096-100 (2006)
Johnson & Johnson Pharmaceutical Research And Development
The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.
Bioorg Med Chem Lett 16: 3489-94 (2006)
Merck Research Laboratories
Development of N-2,4-pyrimidine-N-phenyl-N'-phenyl ureas as inhibitors of tumor necrosis factor alpha (TNF-alpha) synthesis. Part 1.
Bioorg Med Chem Lett 16: 3510-3 (2006)
Procter And Gamble Pharmaceuticals
3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.
Bioorg Med Chem Lett 16: 3524-8 (2006)
Johnson & Johnson Pharmaceutical Research And Development
A new class of selective, non-basic 5-HT2A receptor antagonists.
Bioorg Med Chem Lett 16: 3201-4 (2006)
Merck Sharp & Dohme
Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Bioorg Med Chem Lett 16: 3574-7 (2006)
Abbott Laboratories
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
Bioorg Med Chem Lett 16: 3430-3 (2006)
Genomics Institute Of The Novartis Research Foundation
Modulators of the human CCR5 receptor. Part 3: SAR of substituted 1-[3-(4-methanesulfonylphenyl)-3-phenylpropyl]-piperidinyl phenylacetamides.
Bioorg Med Chem Lett 16: 3533-6 (2006)
Astrazeneca
Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.
Bioorg Med Chem Lett 16: 3115-20 (2006)
Johnson & Johnson Pharmaceutical
Development of lipopeptides for inhibiting 20S proteasomes.
Bioorg Med Chem Lett 16: 3277-81 (2006)
Cnrs-Université
The discovery of tropane-derived CCR5 receptor antagonists.
Chem Biol Drug Des 67: 305-8 (2006)
TBA
Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.
Bioorg Med Chem 14: 5357-69 (2006)
F. Hoffmann-La Roche
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.
Bioorg Med Chem 14: 4740-9 (2006)
Abbott Laboratories
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: selective modification of the furan ring.
Bioorg Med Chem Lett 16: 3170-4 (2006)
The University Of Iowa
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
Bioorg Med Chem Lett 16: 3541-4 (2006)
Universit£
Phosphonic acid-containing analogues of mycophenolic acid as inhibitors of IMPDH.
Bioorg Med Chem Lett 16: 3479-83 (2006)
Gilead Sciences
Novel 5-azaindole factor VIIa inhibitors.
Bioorg Med Chem Lett 16: 3197-200 (2006)
Celera
Design, synthesis, and biological evaluation of indole derivatives as novel nociceptin/orphanin FQ (N/OFQ) receptor antagonists.
Bioorg Med Chem Lett 16: 3569-73 (2006)
Banyu Tsukuba Research Institute
Synthesis of Hsp90 dimerization modulators.
Bioorg Med Chem Lett 16: 3529-32 (2006)
Memorial Sloan-Kettering Cancer Center
2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors.
Bioorg Med Chem Lett 16: 3564-8 (2006)
Merck Research Laboratories
2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.
Bioorg Med Chem Lett 16: 3550-4 (2006)
Merck Sharp And Dohme Research Laboratories
Function of the alkyl side chains of Deltalac-acetogenins in the inhibitory effect on mitochondrial complex I (NADH-ubiquinone oxidoreductase).
Bioorg Med Chem Lett 16: 3555-8 (2006)
Kyoto University
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.
Bioorg Med Chem Lett 16: 3219-23 (2006)
Florida A&M University
Carbonic anhydrase inhibitors: inhibition of the cytosolic human isozyme VII with anions.
Bioorg Med Chem Lett 16: 3139-43 (2006)
Universit£
Synthesis of pyrazoles and isoxazoles as potent alpha(v)beta3 receptor antagonists.
Bioorg Med Chem Lett 16: 3156-61 (2006)
Pfizer
Inhibitory activity of cyclohexenyl chalcone derivatives and flavonoids of fingerroot, Boesenbergia rotunda (L.), towards dengue-2 virus NS3 protease.
Bioorg Med Chem Lett 16: 3337-40 (2006)
Sunway University College
Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors.
J Am Chem Soc 128: 5310-1 (2006)
Purdue University
Diphenylmethane skeleton as a multi-template for nuclear receptor ligands: preparation of FXR and PPAR ligands.
Bioorg Med Chem Lett 16: 3213-8 (2006)
University Of Tokyo
3,4-Fused cyclohexyl sulfones as gamma-secretase inhibitors.
Bioorg Med Chem Lett 16: 3073-7 (2006)
Neuroscience Research Centre
Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity.
Bioorg Med Chem Lett 16: 3229-32 (2006)
Wayne State University
Racemic and chiral sulfoxides as potential prodrugs of the COX-2 inhibitors Vioxx and Arcoxia.
Bioorg Med Chem Lett 16: 3209-12 (2006)
RhôNe-Poulenc Rorer
Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides are potent antagonists of the human H3-receptor.
Bioorg Med Chem Lett 16: 3162-5 (2006)
Novo Nordisk
A practical synthesis of the major 3-hydroxy-2-pyrrolidinone metabolite of a potent CDK2/cyclin A inhibitor.
Bioorg Med Chem Lett 16: 3205-8 (2006)
Nerviano Medical Sciences
Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors.
Bioorg Med Chem Lett 16: 3144-6 (2006)
Institut Curie
Synthesis and molecular modelling of novel substituted-4,5-dihydro-(1H)-pyrazole derivatives as potent and highly selective monoamine oxidase-A inhibitors.
Chem Biol Drug Des 67: 206-14 (2006)
UniversitÀ
Substituted 1,4-benzodiazepine-2,5-diones as alpha-helix mimetic antagonists of the HDM2-p53 protein-protein interaction.
Chem Biol Drug Des 67: 201-5 (2006)
Johnson & Johnson Pharmaceutical Research & Development
Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity.
J Med Chem 49: 2661-5 (2006)
University Of Cincinnati
Synthesis and biological evaluation of cyclopropyl analogues of fosmidomycin as potent Plasmodium falciparum growth inhibitors.
J Med Chem 49: 2656-60 (2006)
Ghent University
Design and synthesis of 1-indol-1-yl-propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha.
J Med Chem 49: 2611-20 (2006)
University Of MüNster
A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
J Med Chem 49: 2600-10 (2006)
Merck Sharp & Dohme Research Laboratories
Investigating the role of stereochemistry in the activity of anticancer acylfulvenes: synthesis, reductase-mediated bioactivation, and cellular toxicity.
J Med Chem 49: 2593-9 (2006)
University Of Minnesota
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.
J Med Chem 49: 2579-92 (2006)
University Walk
2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists.
J Med Chem 49: 2568-78 (2006)
Abbott Laboratories
A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: effect of various substitutions at the primary amino function.
J Med Chem 49: 2549-57 (2006)
Vrije Universiteit Amsterdam
4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
J Med Chem 49: 2526-33 (2006)
Lund University
Refinement of the benzodiazepine receptor site topology by structure-activity relationships of new N-(heteroarylmethyl)indol-3-ylglyoxylamides.
J Med Chem 49: 2489-95 (2006)
Universit£
Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their"receptor desmodynamic processes".
J Med Chem 49: 2456-62 (2006)
University Of Naples Federico Ii
Synthesis and characterization of 3-arylquinazolinone and 3-arylquinazolinethione derivatives as selective estrogen receptor beta modulators.
J Med Chem 49: 2440-55 (2006)
Bristol-Myers Squibb
Catalytic site prediction and virtual screening of cytochrome P450 2D6 substrates by consideration of water and rescoring in automated docking.
J Med Chem 49: 2417-30 (2006)
Vrije Universiteit
Practical synthesis and evaluation of the biological activities of 1alpha,25-dihydroxyvitamin D3 antagonists, 1alpha,25-dihydroxyvitamin D3-26,23-lactams. Designed on the basis of the helix 12-folding inhibition hypothesis.
J Med Chem 49: 2398-406 (2006)
University Of Tokyo
Slow-binding human serine racemase inhibitors from high-throughput screening of combinatorial libraries.
J Med Chem 49: 2388-97 (2006)
University Of California
Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application.
J Med Chem 49: 2363-6 (2006)
Università
Flexible synthesis and biological evaluation of novel 5-deoxyadenophorine analogues.
Bioorg Med Chem Lett 16: 3262-7 (2006)
Université
Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP.
Bioorg Med Chem Lett 16: 3175-9 (2006)
Merck Research Laboratories
Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity.
Bioorg Med Chem Lett 16: 3150-5 (2006)
Abbott Laboratories
4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors.
Bioorg Med Chem Lett 16: 3121-4 (2006)
Chiron
Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands.
Bioorg Med Chem Lett 16: 3233-7 (2006)
Johnson & Johnson Pharmaceutical Research And Development
Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases.
Bioorg Med Chem Lett 16: 3595-9 (2006)
Chiron
P3 and P4 position analysis of vinyl ester pseudopeptide proteasome inhibitors.
Bioorg Med Chem Lett 16: 3125-30 (2006)
University Of Ferrara
Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design.
Bioorg Med Chem Lett 16: 3310-4 (2006)
Johnson & Johnson Pharmaceutical
Identification of a potent botulinum neurotoxin a protease inhibitor using in situ lead identification chemistry.
Org Lett 8: 1729-32 (2006)
The Scripps Research Institute
Selectivity and potency of cyclin-dependent kinase inhibitors.
AAPS J 8: 204-21 (2006)
Georgetown University
Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 16: 3268-72 (2006)
National Health Research Institutes
2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists.
Bioorg Med Chem Lett 16: 2905-8 (2006)
Merck Research Laboratories
Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development.
Bioorg Med Chem Lett 16: 3287-91 (2006)
Gsk
Diarylacetylene piperidinyl amides as novel anxiolytics.
Bioorg Med Chem Lett 16: 3065-7 (2006)
Johnson & Johnson Pharmaceutical Research And Development
Protein tyrosine phosphatase 1B inhibitory activity of triterpenes isolated from Astilbe koreana.
Bioorg Med Chem Lett 16: 3273-6 (2006)
Korea Research Institute Of Bioscience And Biotechnology
Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.
Bioorg Med Chem Lett 16: 3282-6 (2006)
Johnson & Johnson Pharmaceutical Research And Development
Identification of chemically diverse Chk1 inhibitors by receptor-based virtual screening.
Bioorg Med Chem 14: 4792-802 (2006)
Vernalis (R&D)
NK1 antagonists based on seven membered lactam scaffolds.
Bioorg Med Chem Lett 16: 2929-32 (2006)
Merck Sharp And Dohme Research Laboratories
Synthesis and evaluation of two 18F-labeled imidazo[1,2-a]pyridine analogues as potential agents for imaging beta-amyloid in Alzheimer's disease.
Bioorg Med Chem Lett 16: 3015-8 (2006)
Emory University
Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.
J Med Chem 49: 2339-52 (2006)
Abbott Laboratories
Oxyhomologues of anandamide and related endolipids: chemoselective synthesis and biological activity.
J Med Chem 49: 2333-8 (2006)
University Of Piemonte Orientale
Development of the first potential covalent inhibitors of anandamide cellular uptake.
J Med Chem 49: 2320-32 (2006)
Institute Of Biomolecular Chemistry
Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas.
J Med Chem 49: 2294-310 (2006)
Schering-Plough Research Institute
Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
J Med Chem 49: 2268-75 (2006)
Washington University
Novel potent and efficacious nonpeptidic urotensin II receptor agonists.
J Med Chem 49: 2232-40 (2006)
G£Teborg University
Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.
Pharmacol Rev 49: 2222-31 (2006)
Saarland University
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
J Med Chem 49: 2210-21 (2006)
Glaxosmithkline
Identification of potent and selective inhibitors of PDGF receptor autophosphorylation.
J Med Chem 49: 2186-92 (2006)
Kirin Brewery
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
J Med Chem 49: 2174-85 (2006)
National Institutes Of Health
Design, synthesis, and biological evaluation of semicarbazide-sensitive amine oxidase (SSAO) inhibitors with anti-inflammatory activity.
J Med Chem 49: 2166-73 (2006)
La Jolla Pharmaceutical
Nanomolar inhibitors of the peptidyl prolyl cis/trans isomerase Pin1 from combinatorial peptide libraries.
J Med Chem 49: 2147-50 (2006)
Max Planck Research Unit For Enzymology Of Protein Folding
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
J Med Chem 49: 2143-6 (2006)
Pharmaceutical Research Institute
Chemical modulation of receptor signaling inhibits regenerative angiogenesis in adult zebrafish.
Nat Chem Biol 2: 265-73 (2006)
Dana-Farber Cancer Institute
Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype.
Bioorg Med Chem Lett 16: 2955-9 (2006)
Friedrich-Alexander University
Synthetic analogues of the manzamenones and plakoridines which inhibit DNA polymerase.
Bioorg Med Chem Lett 16: 2877-81 (2006)
The University Of Manchester
The search for novel TRPV1-antagonists: from carboxamides to benzimidazoles and indazolones.
Bioorg Med Chem Lett 16: 2872-6 (2006)
Merck Sharp & Dohme
A new non-azole inhibitor of ABA 8'-hydroxylase: effect of the hydroxyl group substituted for geminal methyl groups in the six-membered ring.
Bioorg Med Chem Lett 16: 3302-5 (2006)
Shizuoka University
Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4.
Bioorg Med Chem Lett 16: 2842-5 (2006)
Amgen
Two novel aromatic valerenane-type sesquiterpenes from the Chinese green alga Caulerpa taxifolia.
Bioorg Med Chem Lett 16: 2947-50 (2006)
Chinese Academy Of Sciences
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
J Nat Prod 69: 432-5 (2006)
Tom'S Of Maine
Bioactive dammarane triterpenes from the mangrove plant Bruguiera gymnorrhiza.
J Nat Prod 69: 421-4 (2006)
Mahidol University
N1-(3-cyclohexylbutanoyl)-N2-[3-(1H-imidazol-4-yl)propyl]guanidine (UR-AK57), a potent partial agonist for the human histamine H1- and H2-receptors.
J Pharmacol Exp Ther 317: 1262-8 (2006)
University Of Kansas
Development of activity-based probes for trypsin-family serine proteases.
Bioorg Med Chem Lett 16: 2882-5 (2006)
Celera Genomics
A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.
Bioorg Med Chem Lett 16: 2900-4 (2006)
Merck Research Laboratories
1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists.
Bioorg Med Chem Lett 16: 2969-73 (2006)
The Genomics Institute Of The Novartis Research Foundation
Inhibition of trypsin and urokinase by Cbz-amino(4-guanidinophenyl)methanephosphonate aromatic ester derivatives: the influence of the ester group on their biological activity.
Bioorg Med Chem Lett 16: 2886-90 (2006)
Wroc£?Aw University Of Technology
Triketoacid inhibitors of HIV-integrase: a new chemotype useful for probing the integrase pharmacophore.
Bioorg Med Chem Lett 16: 2920-4 (2006)
Bristol-Myers Squibb
Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.
Bioorg Med Chem Lett 16: 2909-14 (2006)
Celera Genomics
Pentacyclic triterpenes. Part 3: Synthesis and biological evaluation of oleanolic acid derivatives as novel inhibitors of glycogen phosphorylase.
Bioorg Med Chem Lett 16: 2915-9 (2006)
China Pharmaceutical University
The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT2C receptor agonists.
Bioorg Med Chem Lett 16: 2891-4 (2006)
Athersys
New 4-(4-methyl-phenyl)phthalazin-1(2H)-one derivatives and their effects on alpha1-receptors.
Bioorg Med Chem Lett 16: 2575-9 (2006)
Università
1,2,4-Oxadiazolidin-3,5-diones and 1,3,5-triazin-2,4,6-triones as cytosolic phospholipase A2alpha inhibitors.
Bioorg Med Chem Lett 16: 2978-81 (2006)
Wyeth Research
Inhibition of protein tyrosine phosphatase 1B by diterpenoids isolated from Acanthopanax koreanum.
Bioorg Med Chem Lett 16: 3061-4 (2006)
Korea Research Institute Of Bioscience And Biotechnology
Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists.
Bioorg Med Chem Lett 16: 2724-8 (2006)
Pharmacopeia Drug Discovery
Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.
Bioorg Med Chem Lett 16: 2986-90 (2006)
Mochida Pharmaceutical
Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
J Med Chem 49: 2138-42 (2006)
Eli Lilly
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
J Med Chem 49: 2117-26 (2006)
Kochi Medical School
Dopamine/serotonin receptor ligands. 12(1): SAR studies on hexahydro-dibenz[d,g]azecines lead to 4-chloro-7-methyl-5,6,7,8,9,14-hexahydrodibenz[d,g]azecin-3-ol, the first picomolar D5-selective dopamine-receptor antagonist.
J Med Chem 49: 2110-6 (2006)
Friedrich-Schiller-UniversitäT Jena
Synthesis and biological evaluation of purealin and analogues as cytoplasmic dynein heavy chain inhibitors.
J Med Chem 49: 2063-76 (2006)
University Of Pittsburgh
Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety.
J Med Chem 49: 2037-48 (2006)
Takeda Pharmaceutical
Branched diacylglycerol-lactones as potent protein kinase C ligands and alpha-secretase activators.
J Med Chem 49: 2028-36 (2006)
Research Institute Of Pharmaceutical Sciences
Synthesis and SAR studies of 2-oxoquinoline derivatives as CB2 receptor inverse agonists.
J Med Chem 49: 2022-7 (2006)
University Of Kuopio
Diadenosine and diuridine poly(borano)phosphate analogues: synthesis, chemical and enzymatic stability, and activity at P2Y1 and P2Y2 receptors.
J Med Chem 49: 1980-90 (2006)
Bar-Ilan University
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
J Med Chem 49: 1946-52 (2006)
University Of Arizona
Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, biological activities, and mechanism of action.
J Med Chem 49: 1939-45 (2006)
Sapienza University Of Rome
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
J Med Chem 49: 1925-31 (2006)
Universit£
A systematic study of C-glucoside trisphosphates as myo-inositol trisphosphate receptor ligands. Synthesis of beta-C-glucoside trisphosphates based on the conformational restriction strategy.
J Med Chem 49: 1900-9 (2006)
Hokkaido University
Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors.
J Med Chem 49: 1882-90 (2006)
Universita Di Napoli Federico Ii
Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase.
J Med Chem 49: 1867-73 (2006)
University Of North Carolina At Chapel Hill
Enthalpy versus entropy-driven binding of bisphosphonates to farnesyl diphosphate synthase.
J Am Chem Soc 128: 3524-5 (2006)
University Of Illinois At Urbana-Champaign
Functional characterization of IRESes by an inhibitor of the RNA helicase eIF4A.
Nat Chem Biol 2: 213-20 (2006)
Mcgill University
3-Amidoquinuclidine derivatives: synthesis of compounds and inhibition of butyrylcholinesterase.
Bioorg Chem 34: 90-8 (2006)
University Of Zagreb
Synthesis and biological evaluation of rhodanine derivatives as PRL-3 inhibitors.
Bioorg Med Chem Lett 16: 2996-9 (2006)
Korea Research Institute Of Chemical Technology
High-throughput screening for Hsp90 ATPase inhibitors.
Bioorg Med Chem Lett 16: 3005-8 (2006)
The University Of Kansas
SAR studies: designing potent and selective LXR agonists.
Bioorg Med Chem Lett 16: 3055-60 (2006)
Merck Research Laboratories
Identification of an indole series of prostaglandin D2 receptor antagonists.
Bioorg Med Chem Lett 16: 3043-8 (2006)
Merck Frosst Canada
5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists.
Bioorg Med Chem Lett 16: 2791-5 (2006)
Merck Research Laboratories
Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents.
Bioorg Med Chem Lett 16: 3039-42 (2006)
Pfizer
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.
Bioorg Med Chem Lett 16: 3034-8 (2006)
Nih
Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead.
Bioorg Med Chem Lett 16: 2595-8 (2006)
Department Of Medicinal Chemistry Merck
Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors.
Bioorg Med Chem Lett 16: 2590-4 (2006)
Abbott Laboratories
Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2.
Bioorg Med Chem Lett 16: 2689-92 (2006)
Genomics Institute Of The Novartis Research Foundation
Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.
Bioorg Med Chem Lett 16: 2621-7 (2006)
Millennium Pharmaceuticals
Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an alpha-ketothiazole arginine.
Bioorg Med Chem Lett 16: 3049-54 (2006)
Daiichi Asubio Medical Research Laboratories
Virtual and biomolecular screening converge on a selective agonist for GPR30.
Nat Chem Biol 2: 207-12 (2006)
University Of New Mexico Health Sciences Center
A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity.
J Biol Chem 281: 12445-50 (2006)
Duke University Medical Center
Synthesis and SAR studies of diarylpyrrole anticoccidial agents.
Bioorg Med Chem Lett 16: 2817-21 (2006)
Merck Research Laboratories
Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.
Bioorg Med Chem Lett 16: 2641-7 (2006)
Abbott
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.
Bioorg Med Chem Lett 16: 2672-6 (2006)
Astrazeneca
Synthesis and in vitro evaluation of N-substituted aza-trozamicol analogs as vesicular acetylcholine transporter ligands.
Bioorg Med Chem Lett 16: 2654-7 (2006)
Université
Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors.
Bioorg Med Chem Lett 16: 2608-12 (2006)
Merck Frosst Center For Therapeutic Research
A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors.
Bioorg Med Chem Lett 16: 2632-6 (2006)
Novartis Institutes For Biomedical Research
Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents.
Bioorg Med Chem Lett 16: 2753-7 (2006)
University Of Wuerzburg
Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors.
Bioorg Med Chem Lett 16: 2699-704 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
N-Benzylbenzamides: a new class of potent tyrosinase inhibitors.
Bioorg Med Chem Lett 16: 2682-4 (2006)
Seoul National University
Vasorelaxant activity of phthalazinones and related compounds.
Bioorg Med Chem Lett 16: 2786-90 (2006)
Universidad De Salamanca
(R)-sila-venlafaxine: a selective noradrenaline reuptake inhibitor for the treatment of emesis.
Bioorg Med Chem Lett 16: 2555-8 (2006)
Paradigm Therapeutics
Microwave-accelerated synthesis of P1'-extended HIV-1 protease inhibitors encompassing a tertiary alcohol in the transition-state mimicking scaffold.
J Med Chem 49: 1828-32 (2006)
Uppsala University
Stereochemical sensitivity of the human UDP-glucuronosyltransferases 2B7 and 2B17.
J Med Chem 49: 1818-27 (2006)
University Of Helsinki
Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
J Med Chem 49: 1808-17 (2006)
Istituto Di Ricerche Chimiche E Biochimiche G. Ronzoni
Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
J Med Chem 49: 1773-80 (2006)
University Of Arizona
Design and synthesis of promiscuous high-affinity monoamine transporter ligands: unraveling transporter selectivity.
J Med Chem 49: 1766-72 (2006)
Niddk
Lipolanthionine peptides act as inhibitors of TLR2-mediated IL-8 secretion. Synthesis and structure-activity relationships.
J Med Chem 49: 1754-65 (2006)
University Of T£Bingen
Synthesis and biological studies of a new series of 5-heteroarylcarbamoylaminopyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidines as human A3 adenosine receptor antagonists. Influence of the heteroaryl substituent on binding affinity and molecular modeling investigations.
J Med Chem 49: 1720-9 (2006)
Universit£
2-(2-Thienyl)-5,6-dihydroxy-4-carboxypyrimidines as inhibitors of the hepatitis C virus NS5B polymerase: discovery, SAR, modeling, and mutagenesis.
J Med Chem 49: 1693-705 (2006)
P. Angeletti S.P.A. (Merck Research Laboratories)
Dynamic pharmacophore model optimization: identification of novel HIV-1 integrase inhibitors.
J Med Chem 49: 1684-92 (2006)
University Of Houston
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.
J Med Chem 49: 1668-83 (2006)
University Of Alberta
Discovery of protein phosphatase 2C inhibitors by virtual screening.
J Med Chem 49: 1658-67 (2006)
The Rockefeller University
Design, synthesis, and biological evaluation of isoquinoline-1,3,4-trione derivatives as potent caspase-3 inhibitors.
J Med Chem 49: 1613-23 (2006)
Shanghai Institutes For Biological Sciences
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.
J Med Chem 49: 1597-612 (2006)
Gsk
Discovery of a novel nonphosphorylated pentapeptide motif displaying high affinity for Grb2-SH2 domain by the utilization of 3'-substituted tyrosine derivatives.
J Med Chem 49: 1585-96 (2006)
Graduate School Of The Chinese Academy Of Sciences
Identification of novel parasitic cysteine protease inhibitors by use of virtual screening. 2. The available chemical directory.
J Med Chem 49: 1576-84 (2006)
University Of Mississippi
Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase.
J Med Chem 49: 1562-75 (2006)
Roche Palo Alto
Pyrazolo[3,4-d]pyrimidines as potent antiproliferative and proapoptotic agents toward A431 and 8701-BC cells in culture via inhibition of c-Src phosphorylation.
J Med Chem 49: 1549-61 (2006)
Università
Synthesis and structure-activity relationship of small-molecule malonyl coenzyme A decarboxylase inhibitors.
J Med Chem 49: 1517-25 (2006)
Chugai Pharma Usa
Novel HIV-1 integrase inhibitors derived from quinolone antibiotics.
J Med Chem 49: 1506-8 (2006)
Central Pharmaceutical Research Institute
Selective irreversible inhibition of fructose 1,6-bisphosphate aldolase from Trypanosoma brucei.
J Med Chem 49: 1499-502 (2006)
Université
Ultrahigh resolution crystal structures of human carbonic anhydrases I and II complexed with "two-prong" inhibitors reveal the molecular basis of high affinity.
J Am Chem Soc 128: 3011-8 (2006)
University Of Pennsylvania
Synthesis of a potent 5'-methylthioadenosine/S-adenosylhomocysteine (MTAN) inhibitor.
Bioorg Med Chem Lett 16: 2662-5 (2006)
Biocryst Pharmaceuticals
Studies on the novel alpha-glucosidase inhibitory activity and structure-activity relationships for andrographolide analogues.
Bioorg Med Chem Lett 16: 2710-3 (2006)
Zhengzhou University
Synthesis of phospholipase A2 inhibitory biflavonoids.
Bioorg Med Chem Lett 16: 2373-5 (2006)
Kangwon National University
3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid as a highly potent and selective retinoic acid metabolic blocking agent.
Bioorg Med Chem Lett 16: 2729-33 (2006)
Osi Pharmaceuticals
Design of a potent, soluble glucokinase activator with excellent in vivo efficacy.
Bioorg Med Chem Lett 16: 2705-9 (2006)
Astrazeneca R&D
Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant.
Bioorg Med Chem Lett 16: 2748-52 (2006)
Mrl Rome
Discovery of novel biaryl heterocyclic EP1 receptor antagonists.
Bioorg Med Chem Lett 16: 2666-71 (2006)
Glaxosmithkline
Novel substituted naphthalen-1-yl-methanone derivatives as anti-hyperglycemic agents.
Bioorg Med Chem Lett 16: 2719-23 (2006)
Central Drug Research Institute
Bioactive compounds from Peperomia pellucida.
J Nat Prod 69: 247-50 (2006)
Chinese Academy Of Sciences
N-Alkyl-N-arylmethylpiperidin-4-amines: novel dual inhibitors of serotonin and norepinephrine reuptake.
Bioorg Med Chem Lett 16: 2714-8 (2006)
Eli Lilly
Optimization of 2-aminothiazole derivatives as CCR4 antagonists.
Bioorg Med Chem Lett 16: 2800-3 (2006)
Amgen
Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent.
Bioorg Med Chem 14: 4208-16 (2006)
Johnson & Johnson Pharmaceutical
Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2.
Bioorg Med Chem Lett 16: 2777-80 (2006)
Universite Paris 5 René
An efficient rapid system for profiling the cellular activities of molecular libraries.
Proc Natl Acad Sci U S A 103: 3153-8 (2006)
Genomics Institute Of The Novartis Research Foundation
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.
Chem Biol 13: 201-11 (2006)
Cyclacel
Structure-based optimization of MurF inhibitors.
Chem Biol Drug Des 67: 58-65 (2006)
Abbott Laboratories
Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds.
Chem Biol Drug Des 67: 46-57 (2006)
Ariad Pharmaceuticals
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.
Bioorg Med Chem Lett 16: 2416-8 (2006)
University Of Virginia
Discovery of novel hydroxy pyrazole based factor IXa inhibitor.
Bioorg Med Chem Lett 16: 2796-9 (2006)
Celera Genomics
Identification of potent phenyl imidazoles as opioid receptor agonists.
Bioorg Med Chem Lett 16: 2505-8 (2006)
Johnson & Johnson Pharmaceutical Research & Development
Novel indole inhibitors of IMPDH from fragments: synthesis and initial structure-activity relationships.
Bioorg Med Chem Lett 16: 2539-42 (2006)
Ucb Pharma
Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.
Bioorg Med Chem Lett 16: 2419-22 (2006)
Glaxosmithkline
Isoquinoline derivatives as potential acetylcholinesterase inhibitors.
Bioorg Med Chem Lett 16: 2170-2 (2006)
Naresuan University
Low molecular weight indole fragments as IMPDH inhibitors.
Bioorg Med Chem Lett 16: 2535-8 (2006)
Ucb Pharma
Design and synthesis of potent beta-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres.
Bioorg Med Chem Lett 16: 2380-6 (2006)
Kyoto Pharmaceutical University
Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.
Bioorg Med Chem Lett 16: 2411-5 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationship of thiopyrimidines as mGluR5 antagonists.
Bioorg Med Chem Lett 16: 2467-9 (2006)
Nps Pharmaceuticals
Fluorescent glycosidase inhibiting 1,5-dideoxy-1,5-iminoalditols.
Bioorg Med Chem Lett 16: 2067-70 (2006)
Technische UniversitäT Graz
Ketopiperazine-based renin inhibitors: optimization of the "C" ring.
Bioorg Med Chem Lett 16: 2500-4 (2006)
Pfizer
Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P2'-ligands.
Bioorg Med Chem Lett 16: 1869-73 (2006)
Purdue University
Design and synthesis of 2,3,4,9-tetrahydro-1H-carbazole and 1,2,3,4-tetrahydro-cyclopenta[b]indole derivatives as non-nucleoside inhibitors of hepatitis C virus NS5B RNA-dependent RNA polymerase.
Bioorg Med Chem Lett 16: 2532-4 (2006)
Wyeth Research
Dipeptide nitrile inhibitors of cathepsin K.
Bioorg Med Chem Lett 16: 2549-54 (2006)
Novartis Pharmaceuticals
4-Amino derivatives of the Hsp90 inhibitor CCT018159.
Bioorg Med Chem Lett 16: 2543-8 (2006)
Vernalis
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
J Med Chem 49: 1475-85 (2006)
Pfizer
Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.
J Med Chem 49: 1455-65 (2006)
Glsynthesis
A new class of blockers of the voltage-gated potassium channel Kv1.3 via modification of the 4- or 7-position of khellinone.
J Med Chem 49: 1433-41 (2006)
Institute Of Medical Research Biotechnology Centre
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.
J Med Chem 49: 1420-32 (2006)
Organix
Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition.
J Med Chem 49: 1413-9 (2006)
The Ohio State University
Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
J Med Chem 49: 1388-96 (2006)
The Danish University Of Pharmaceutical Sciences
Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M.
J Med Chem 49: 1379-87 (2006)
Georgia State University
Novel human lipoxygenase inhibitors discovered using virtual screening with homology models.
J Med Chem 49: 1356-63 (2006)
University Of California
Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors.
J Med Chem 49: 1346-55 (2006)
Astex
Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.
J Med Chem 49: 1325-45 (2006)
University Of Bath
Vitamin D receptor: ligand recognition and allosteric network.
J Med Chem 49: 1313-24 (2006)
Tokyo Medical And Dental University
Crystal structures of Helicobacter pylori type II dehydroquinase inhibitor complexes: new directions for inhibitor design.
J Med Chem 49: 1282-90 (2006)
University Of Glasgow
Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors.
J Med Chem 49: 1271-81 (2006)
Johannes Gutenberg University
Dual binding mode of a novel series of DHODH inhibitors.
J Med Chem 49: 1239-47 (2006)
4Sc
Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.
J Med Chem 49: 1235-8 (2006)
TBA
Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists.
J Med Chem 49: 1231-4 (2006)
TBA
1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b.
J Med Chem 49: 1227-30 (2006)
TBA
Inactivation of S-adenosyl-L-homocysteine hydrolase by 6'-cyano-5',6'-didehydro-6'-deoxyhomoadenosine and 6'-chloro-6'-cyano-5',6'-didehydro-6'-deoxyhomoadenosine. Antiviral and cytotoxic effects.
J Med Chem 49: 1223-6 (2006)
TBA
Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.
J Biol Chem 281: 9987-95 (2006)
University Of Queensland
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Bioorg Med Chem Lett 16: 2357-63 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist.
J Pharmacol Exp Ther 317: 910-8 (2006)
Acadia Pharmaceuticals
Synthesis and biological activity of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 2: 2'-substituted triclosan derivatives.
Bioorg Med Chem Lett 16: 2163-9 (2006)
Jacobus Pharmaceutical
Alpha-methylated derivatives of 2-arachidonoyl glycerol: synthesis, CB1 receptor activity, and enzymatic stability.
Bioorg Med Chem Lett 16: 2437-40 (2006)
University Of Kuopio
Uncharged isocoumarin-based inhibitors of urokinase-type plasminogen activator.
BMC Chem Biol 6: 1 (2006)
University Of New Mexico
Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents.
Bioorg Med Chem Lett 16: 2479-83 (2006)
Merck Research Laboratories
Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors.
Bioorg Med Chem Lett 16: 2076-80 (2006)
Veterinary Medicine Research And Development Pfizer
Structure-activity relationship study between Ornithyl-Proline and Lysyl-Proline based tripeptidomimics as angiotensin-converting enzyme inhibitors.
Bioorg Med Chem Lett 16: 2117-21 (2006)
Institute Of Genomics And Integrative Biology
The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A3 receptor.
Bioorg Med Chem Lett 16: 2525-7 (2006)
Pfizer
Substituted coumarins as potent 5-lipoxygenase inhibitors.
Bioorg Med Chem Lett 16: 2528-31 (2006)
Merck Frosst Centre For Therapeutic Research
A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core.
Bioorg Med Chem Lett 16: 2071-5 (2006)
Amgen
Synthesis of fluorescent derivatives of wortmannin and demethoxyviridin as probes for phosphatidylinositol 3-kinase.
Bioorg Med Chem Lett 16: 2518-21 (2006)
State University Of New York-Esf
Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.
Bioorg Med Chem Lett 16: 1950-3 (2006)
Hoffmann-La Roche
Orally active thrombin inhibitors. Part 2: optimization of the P2-moiety.
Bioorg Med Chem Lett 16: 2648-53 (2006)
Abbott
Synthesis and evaluation of novel heterocyclic inhibitors of GSK-3.
Bioorg Med Chem Lett 16: 2091-4 (2006)
Glaxosmithkline
Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.
Bioorg Med Chem Lett 16: 1913-9 (2006)
Chemical Diversity
A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.
Bioorg Med Chem Lett 16: 2200-4 (2006)
Johnson & Johnson Pharmaceutical Research And Development
Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis.
Bioorg Med Chem Lett 16: 2158-62 (2006)
Cephalon
Discovery of novel heterocyclic factor VIIa inhibitors.
Bioorg Med Chem Lett 16: 2270-3 (2006)
Celera
Synthesis of novel benzofuran isoxazolines as protein tyrosine phosphatase 1B inhibitors.
Bioorg Med Chem Lett 16: 2139-43 (2006)
Central Drug Research Institute
Transport of glyburide by placental ABC transporters: implications in fetal drug exposure.
Placenta 27: 1096-102 (2006)
Hospital For Sick Children
Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori.
Bioorg Med Chem Lett 16: 2182-8 (2006)
Kochi Medical School
Specific inhibitors of Plasmodium falciparum thioredoxin reductase as potential antimalarial agents.
Bioorg Med Chem Lett 16: 2283-92 (2006)
University Of Michigan
Inhibitors of human mitotic kinesin Eg5: characterization of the 4-phenyl-tetrahydroisoquinoline lead series.
Bioorg Med Chem Lett 16: 2095-100 (2006)
Bristol-Myers Squibb
The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors.
Bioorg Med Chem Lett 16: 2209-12 (2006)
Johnson And Johnson Pharmaceutical Research And Development
Identification and structure-activity relationships of a new series of Melanocortin-4 receptor antagonists.
Bioorg Med Chem Lett 16: 2302-5 (2006)
Millennium Pharmaceuticals
Factor VIIa inhibitors: a prodrug strategy to improve oral bioavailability.
Bioorg Med Chem Lett 16: 2224-8 (2006)
Celera Genomics
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
Bioorg Med Chem Lett 16: 1788-94 (2006)
Glaxosmithkline
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.
Bioorg Med Chem Lett 16: 2101-4 (2006)
Columbia University College Of Physicians And Surgeons
Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1.
Bioorg Med Chem Lett 16: 2173-6 (2006)
Genomics Institute Of The Novartis Research Foundation
QSAR study on topically acting sulfonamides incorporating GABA moieties: a molecular connectivity approach.
Bioorg Med Chem Lett 16: 2044-51 (2006)
A.P.S. University
Potent blockers of the monocarboxylate transporter MCT1: novel immunomodulatory compounds.
Bioorg Med Chem Lett 16: 2260-5 (2006)
Astrazeneca
3D-QSAR studies of farnesyltransferase inhibitors: a comparative molecular field analysis approach.
Bioorg Med Chem Lett 16: 1821-7 (2006)
The M.S. University Of Baroda
An efficient, asymmetric solid-phase synthesis of benzothiadiazine-substituted tetramic acids: potent inhibitors of the hepatitis C virus RNA-dependent RNA polymerase.
Bioorg Med Chem Lett 16: 2205-8 (2006)
Glaxosmithkline
Benzimidazole inhibitors of hepatitis C virus NS5B polymerase: identification of 2-[(4-diarylmethoxy)phenyl]-benzimidazole.
Bioorg Med Chem Lett 16: 1859-63 (2006)
Central Pharmaceutical Research Institute
Factor VIIa inhibitors: improved pharmacokinetic parameters.
Bioorg Med Chem Lett 16: 2243-6 (2006)
Celera Genomics
The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent.
Bioorg Med Chem Lett 16: 2219-23 (2006)
Merck Research Laboratories
Pyridone derivatives as potent and selective VLA-4 integrin antagonists.
Bioorg Med Chem Lett 16: 2256-9 (2006)
Glaxosmithkline
Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: design, synthesis, structural biology, and molecular docking studies.
J Med Chem 49: 1212-6 (2006)
National Health Research Institutes
Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
J Med Chem 49: 1202-6 (2006)
Pfizer
Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.
J Med Chem 49: 1165-81 (2006)
Abbott Laboratories
A QSAR model for in silico screening of MAO-A inhibitors. Prediction, synthesis, and biological assay of novel coumarins.
J Med Chem 49: 1149-56 (2006)
University Of Santiago De Compostela
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.
J Med Chem 49: 1125-39 (2006)
Pfizer
New cannabidiol derivatives: synthesis, binding to cannabinoid receptor, and evaluation of their antiinflammatory activity.
J Med Chem 49: 1113-7 (2006)
Ben-Gurion University Of The Negev
Trace amine-associated receptor agonists: synthesis and evaluation of thyronamines and related analogues.
J Med Chem 49: 1101-12 (2006)
University Of California San Francisco
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
J Med Chem 49: 1080-100 (2006)
University Of Illinois At Chicago
Beta-substituted cyclohexanecarboxamide: a nonpeptidic framework for the design of potent inhibitors of cathepsin K.
J Med Chem 49: 1066-79 (2006)
Merck Frosst Centre For Therapeutic Research
Dual inhibitors of thymidylate synthase and dihydrofolate reductase as antitumor agents: design, synthesis, and biological evaluation of classical and nonclassical pyrrolo[2,3-d]pyrimidine antifolates(1).
J Med Chem 49: 1055-65 (2006)
Duquesne University
SAR and mode of action of novel non-nucleoside inhibitors of hepatitis C NS5b RNA polymerase.
J Med Chem 49: 1034-46 (2006)
Amgen
Potent CYP19 (aromatase) 1-[(benzofuran-2-yl)(phenylmethyl)pyridine, -imidazole, and -triazole inhibitors: synthesis and biological evaluation.
J Med Chem 49: 1016-22 (2006)
Cardiff University
Design and synthesis of 5-aryl-pyridone-carboxamides as inhibitors of anaplastic lymphoma kinase.
J Med Chem 49: 1006-15 (2006)
Chembridge Research Laboratories And Chembridge
Novel potent hepatitis C virus NS3 serine protease inhibitors derived from proline-based macrocycles.
J Med Chem 49: 995-1005 (2006)
Schering-Plough Research Institute
3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase.
J Med Chem 49: 971-83 (2006)
Glaxosmithkline
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
J Med Chem 49: 955-70 (2006)
Astrazeneca
Evaluation of carbon-11-labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-iodoethenyl)phenyl]nortropane as a potential radioligand for imaging the serotonin transporter by PET.
J Med Chem 49: 942-6 (2006)
Emory University
Structural Insight into the Stereoselective Inhibition of MMP-8 by Enantiomeric Sulfonamide Phosphonates.
J Med Chem 49: 923-31 (2006)
Istituto Di Cristallografia
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
J Med Chem 49: 911-22 (2006)
Millennium Pharmaceuticals
Structure-based design, synthesis, and biological evaluation of novel inhibitors of human cyclophilin A.
J Med Chem 49: 900-10 (2006)
University Of Montpellier
Amiodarone has intrinsic anti-Trypanosoma cruzi activity and acts synergistically with posaconazole.
J Med Chem 49: 892-9 (2006)
Instituto Venezolano De Investigaciones CientíFicas
Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists.
J Med Chem 49: 872-82 (2006)
Universit£
Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
J Med Chem 49: 864-71 (2006)
Johann Wolfgang Goethe University
Novel benzodiazepine photoaffinity probe stereoselectively labels a site deep within the membrane-spanning domain of the cholecystokinin receptor.
J Med Chem 49: 850-63 (2006)
Mayo Clinic
Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.
J Med Chem 49: 847-9 (2006)
Banyu Tsukuba Research Institute
A selective estrogen receptor modulator for the treatment of hot flushes.
J Med Chem 49: 843-6 (2006)
Eli Lilly
Aminoethylenes: a tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1.
J Med Chem 49: 839-42 (2006)
Sunesis
Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase.
Bioorg Med Chem Lett 16: 1807-10 (2006)
Abbott Laboratories
Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3.
Bioorg Med Chem Lett 16: 1975-80 (2006)
Gnf
Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors.
Bioorg Med Chem Lett 16: 2293-8 (2006)
Abbott Laboratories
Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases.
Bioorg Med Chem Lett 16: 2247-51 (2006)
Chiron
Global effects of the energetics of coenzyme binding: NADPH controls the protein interaction properties of human cytochrome P450 reductase.
Biochemistry 45: 1421-34 (2006)
Merck Research Laboratories
Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats.
Bioorg Med Chem Lett 16: 1799-802 (2006)
Pfizer
Novel non-benzimidazole chk2 kinase inhibitors.
Bioorg Med Chem Lett 16: 1924-8 (2006)
Johnson And Johnson Pharmaceutical Research And Development
Hydantoin derivatives as non-peptidic inhibitors of Ras farnesyl transferase.
Bioorg Med Chem Lett 16: 1954-6 (2006)
Keimyung University
Optimization of 2,4-diaminopyrimidines as GHS-R antagonists: side chain exploration.
Bioorg Med Chem Lett 16: 1864-8 (2006)
Abbott Laboratories
Isoflavonoids with antiestrogenic activity from Millettia pachycarpa.
J Nat Prod 69: 138-41 (2006)
Meijo University
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: semisynthesis of salvinicins A and B and other chemical transformations of salvinorin A.
J Nat Prod 69: 107-12 (2006)
The University Of Iowa
A common protein fold topology shared by flavonoid biosynthetic enzymes and therapeutic targets.
J Nat Prod 69: 14-7 (2006)
Griffith University
Chlamydocin analogs bearing carbonyl group as possible ligand toward zinc atom in histone deacetylases.
Bioorg Med Chem 14: 3438-46 (2006)
Kyushu Institute Of Technology
Synthesis and SAR of highly potent and selective dopamine D3-receptor antagonists: variations on the 1H-pyrimidin-2-one theme.
Bioorg Med Chem Lett 16: 1934-7 (2006)
Abbott
Synthesis of alpha-substituted fosmidomycin analogues as highly potent Plasmodium falciparum growth inhibitors.
Bioorg Med Chem Lett 16: 1888-91 (2006)
Ghent University
Beta-diketo acids with purine nucleobase scaffolds: novel, selective inhibitors of the strand transfer step of HIV integrase.
Bioorg Med Chem Lett 16: 1920-3 (2006)
University Of Georgia
Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP.
Bioorg Med Chem Lett 16: 1775-9 (2006)
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
Bioorg Med Chem Lett 16: 1780-3 (2006)
Merck Research Laboratories
First dual M3 antagonists-PDE4 inhibitors: synthesis and SAR of 4,6-diaminopyrimidine derivatives.
Bioorg Med Chem Lett 16: 1834-9 (2006)
Ucb Pharma
Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.
Bioorg Med Chem Lett 16: 1892-7 (2006)
F. Hoffmann-La Roche
Synthesis and activity of small molecule GPR40 agonists.
Bioorg Med Chem Lett 16: 1840-5 (2006)
Glaxosmithkline Research And Development
Pharmacological characterization and feeding-suppressive property of FMS586 [3-(5,6,7,8-tetrahydro-9-isopropyl-carbazol-3-yl)-1-methyl-1-(2-pyridin-4-yl-ethyl)-urea hydrochloride], a novel, selective, and orally active antagonist for neuropeptide Y Y5 receptor.
J Pharmacol Exp Ther 317: 562-70 (2006)
Meiji Seika Kaisha
Multidrug resistance protein 1 (MRP1, ABCC1) mediates resistance to mitoxantrone via glutathione-dependent drug efflux.
Mol Pharmacol 69: 1499-505 (2006)
Wake Forest University School Of Medicine
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
Bioorg Med Chem Lett 16: 1795-8 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities.
Bioorg Med Chem Lett 16: 1938-40 (2006)
Johann Wolfgang Goethe-UniversitäT
Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases.
Bioorg Med Chem Lett 16: 1905-8 (2006)
Graduate School Of Chinese Academy Of Sciences
Design and modular parallel synthesis of a MCR derived alpha-helix mimetic protein-protein interaction inhibitor scaffold.
Bioorg Med Chem Lett 16: 1740-3 (2006)
Abc Pharma
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
Bioorg Med Chem Lett 16: 1605-9 (2006)
Wyeth Research
Orally active purine-based inhibitors of the heat shock protein 90.
J Med Chem 49: 817-28 (2006)
Conforma Therapeutics
Correlation of antifungal activity with fungal phospholipase inhibition using a series of bisquaternary ammonium salts.
J Med Chem 49: 811-6 (2006)
The University Of Sydney
Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides.
J Med Chem 49: 800-5 (2006)
University College London
Synthesis and biological evaluation of novel phenylcarbazoles as potential anticancer agents.
J Med Chem 49: 789-99 (2006)
Université
Dopamine/serotonin receptor ligands. 10: SAR Studies on azecine-type dopamine receptor ligands by functional screening at human cloned D1, D2L, and D5 receptors with a microplate reader based calcium assay lead to a novel potent D1/D5 selective antagonist.
J Med Chem 49: 760-9 (2006)
University Of Bonn
Novel 5alpha-reductase inhibitors: synthesis, structure-activity studies, and pharmacokinetic profile of phenoxybenzoylphenyl acetic acids.
J Med Chem 49: 748-59 (2006)
Saarland University
(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
J Med Chem 49: 716-26 (2006)
Astellas Pharma
Structure-activity study of brassinin derivatives as indoleamine 2,3-dioxygenase inhibitors.
J Med Chem 49: 684-92 (2006)
Bryn Mawr College
Discovery of two novel, small-molecule inhibitors of DNA methylation.
J Med Chem 49: 678-83 (2006)
Polish Academy Of Sciences
The first potent inhibitors for human glutaminyl cyclase: synthesis and structure-activity relationship.
J Med Chem 49: 664-77 (2006)
Probiodrug
Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor.
J Med Chem 49: 637-47 (2006)
Neurocrine Biosciences
Identification of the key residue of calcitonin gene related peptide (CGRP) 27-37 to obtain antagonists with picomolar affinity at the CGRP receptor.
J Med Chem 49: 616-24 (2006)
University Of Leipzig
Trisubstituted acridines as G-quadruplex telomere targeting agents. Effects of extensions of the 3,6- and 9-side chains on quadruplex binding, telomerase activity, and cell proliferation.
J Med Chem 49: 582-99 (2006)
University Of London
Potent 7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid-based macrocyclic inhibitors of hepatitis C virus NS3 protease.
J Med Chem 49: 567-74 (2006)
Schering-Plough Research Institute
3D-QSAR studies on cannabinoid CB1 receptor agonists: G-protein activation as biological data.
J Med Chem 49: 554-66 (2006)
University Of Kuopio
Classification of chemical compounds by protein-compound docking for use in designing a focused library.
J Med Chem 49: 523-33 (2006)
National Institute Of Advanced Industrial Science And Technology (Aist)
Metal-mediated inhibition of Escherichia coli methionine aminopeptidase: structure-activity relationships and development of a novel scoring function for metal-ligand interactions.
J Med Chem 49: 511-22 (2006)
Saarland University
Computational study of antagonist/alpha1A adrenoceptor complexes--observations of conformational variations on the formation of ligand/receptor complexes.
J Med Chem 49: 501-10 (2006)
University Of Dublin
Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain.
J Med Chem 49: 471-4 (2006)
Novartis Institutes For Biomedical Research
Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties.
J Med Chem 49: 459-62 (2006)
Instituto De Quimica Medica (Csic)
Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.
J Med Chem 49: 456-8 (2006)
Chinese Academy Of Sciences
HIV integrase inhibitors with nucleobase scaffolds: discovery of a highly potent anti-HIV agent.
J Med Chem 49: 445-7 (2006)
University Of Georgia
Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-ones.
J Med Chem 49: 441-4 (2006)
Array Biopharma
Allosteric inhibitors of Bcr-abl-dependent cell proliferation.
Nat Chem Biol 2: 95-102 (2006)
Genomics Institute Of The Novartis Research Foundation
Microarray-based method for monitoring yeast overexpression strains reveals small-molecule targets in TOR pathway.
Nat Chem Biol 2: 103-9 (2006)
Harvard University
Factor VIIa inhibitors: gaining selectivity within the trypsin family.
Bioorg Med Chem Lett 16: 1596-600 (2006)
Celera
1-Phenyl-8-azabicyclo[3.2.1]octane ethers: a novel series of neurokinin (NK1) antagonists.
Bioorg Med Chem Lett 16: 2008-12 (2006)
Merck Sharp & Dohme Research Laboratories
Investigation of mechanism-based thrombin inhibitors: Implications of a highly conserved water molecule for the binding of coumarins within the S pocket.
Bioorg Med Chem Lett 16: 2017-21 (2006)
University Of Namur
Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.
Bioorg Med Chem Lett 16: 2000-7 (2006)
Abbott Laboratories
Discovery of novel and selective tertiary alcohol containing inhibitors of the norepinephrine transporter.
Bioorg Med Chem Lett 16: 2022-5 (2006)
Eli Lilly
Identification of a potent and selective non-basic cathepsin K inhibitor.
Bioorg Med Chem Lett 16: 1985-9 (2006)
Merck Frosst Centre For Therapeutic Research
In silico identification of novel EGFR inhibitors with antiproliferative activity against cancer cells.
Bioorg Med Chem Lett 16: 1969-74 (2006)
Molsoft
Small molecule inhibitors of plasma kallikrein.
Bioorg Med Chem Lett 16: 2034-6 (2006)
Celera Genomics
Novel inhibitors of hepatitis C NS3-NS4A serine protease derived from 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid.
Bioorg Med Chem Lett 16: 1628-32 (2006)
Schering-Plough Research Institute
6H-Benzo[c]chromen-6-one derivatives as selective ERbeta agonists.
Bioorg Med Chem Lett 16: 1468-72 (2006)
Merck Research Laboratories
Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
Bioorg Med Chem Lett 16: 2013-6 (2006)
Peking University
Tricyclic azepine derivatives: pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors.
Bioorg Med Chem Lett 16: 1643-6 (2006)
Imclone Systems
A novel series of urea-based peptidomimetic calpain inhibitors.
Bioorg Med Chem Lett 16: 1965-8 (2006)
The University Of Tennessee Health Science Center
Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl.
Bioorg Med Chem Lett 16: 1486-90 (2006)
Gnf
Factor VIIa inhibitors: chemical optimization, preclinical pharmacokinetics, pharmacodynamics, and efficacy in an arterial baboon thrombosis model.
Bioorg Med Chem Lett 16: 2037-41 (2006)
Celera Genomics
BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles: chromene, coumarin and quinoline.
Bioorg Med Chem Lett 16: 1995-9 (2006)
University Of The Mediterranean
Allosteric control of an ionotropic glutamate receptor with an optical switch.
Nat Chem Biol 2: 47-52 (2006)
University Of California Berkeley
Secramine inhibits Cdc42-dependent functions in cells and Cdc42 activation in vitro.
Nat Chem Biol 2: 39-46 (2006)
Harvard Medical School
Purmorphamine activates the Hedgehog pathway by targeting Smoothened.
Nat Chem Biol 2: 29-30 (2006)
Stanford University School Of Medicine
Host sphingolipid biosynthesis as a target for hepatitis C virus therapy.
Nat Chem Biol 1: 333-7 (2006)
Chugai Pharmaceutical
Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.
Nat Chem Biol 1: 143-5 (2005)
Ludwig-Maximillians University Of Munich
Assignment of protein function in the postgenomic era.
Nat Chem Biol 1: 130-42 (2006)
The Scripps Research Institute
Linking agonist binding to histamine H1 receptor activation.
Nat Chem Biol 1: 98-103 (2006)
Vrije Universiteit Amsterdam
Diversity-oriented synthesis: exploring the intersections between chemistry and biology.
Nat Chem Biol 1: 74-84 (2006)
Memorial Sloan-Kettering Cancer Center
Activity-based probes that target diverse cysteine protease families.
Nat Chem Biol 1: 33-8 (2005)
Stanford University
Small-molecule inhibition of siderophore biosynthesis in Mycobacterium tuberculosis and Yersinia pestis.
Nat Chem Biol 1: 29-32 (2006)
Weill Medical College Of Cornell University
Conformation-assisted inhibition of protein-tyrosine phosphatase-1B elicits inhibitor selectivity over T-cell protein-tyrosine phosphatase.
J Biol Chem 281: 8010-5 (2006)
Merck Frosst Center For Therapeutic Research
Effector-repressor interactions, binding of a single effector molecule to the operator-bound TtgR homodimer mediates derepression.
J Biol Chem 281: 7102-9 (2006)
Estacion Experimental Del Zaidin
Herbicide-binding sites revealed in the structure of plant acetohydroxyacid synthase.
Proc Natl Acad Sci U S A 103: 569-73 (2006)
University Of Queensland
Brequinar derivatives and species-specific drug design for dihydroorotate dehydrogenase.
Bioorg Med Chem Lett 16: 1610-5 (2006)
Cornell University
Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.
Bioorg Med Chem Lett 16: 1175-9 (2006)
Merck Sharp And Dohme Research Laboratories
Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.
Bioorg Med Chem Lett 16: 1679-85 (2006)
Abbott Laboratories
Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead.
J Med Chem 49: 407-16 (2006)
Institute Of Cancer Research
Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90.
J Med Chem 49: 381-90 (2006)
Memorial Sloan-Kettering Cancer Center
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
J Med Chem 49: 373-80 (2006)
National Health Research Institutes
Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors.
J Med Chem 49: 366-72 (2006)
Universit£
Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands for visualization of brain dopamine D3 receptors.
J Med Chem 49: 358-65 (2006)
Università
Discovery of benzylidenebenzofuran-3(2H)-one (aurones) as inhibitors of tyrosinase derived from human melanocytes.
J Med Chem 49: 329-33 (2006)
Umr-Cnrs 5063
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
J Med Chem 49: 318-28 (2006)
Alcon Research
Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor.
J Med Chem 49: 282-99 (2006)
Universit£
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.
J Med Chem 49: 273-81 (2006)
Ewha Womans University
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
J Med Chem 49: 256-62 (2006)
Harvard Medical School
Effect of polyamine homologation on the transport and biological properties of heterocyclic amidines.
J Med Chem 49: 232-45 (2006)
Universit£
Inhibition of Trypanosoma cruzi hexokinase by bisphosphonates.
J Med Chem 49: 215-23 (2006)
University Of Illinois At Urbana-Champaign
Rational design and enantioselective synthesis of (1R,4S,5R,6S)-3-azabicyclo[3.3.0]octane-4,6-dicarboxylic acid - a novel inhibitor at human glutamate transporter subtypes 1, 2, and 3.
J Med Chem 49: 172-8 (2006)
The Danish University Of Pharmaceutical Sciences
Structure-activity relationships at the 5-position of thiolactomycin: an intact (5R)-isoprene unit is required for activity against the condensing enzymes from Mycobacterium tuberculosis and Escherichia coli.
J Med Chem 49: 159-71 (2006)
National Institute Of Allergy And Infectious Diseases
Inhibition of cytosolic phospholipase A2alpha: hit to lead optimization.
J Med Chem 49: 135-58 (2006)
Wyeth Research
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.
J Med Chem 49: 125-34 (2006)
Columbia University College Of Physicians And Surgeons
Discovery of nonpeptidic small-molecule AP-1 inhibitors: lead hopping based on a three-dimensional pharmacophore model.
J Med Chem 49: 80-91 (2006)
Toyama Chemical
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.
J Med Chem 49: 70-9 (2006)
Universit£
Matrix metalloproteinase target family landscape: a chemometrical approach to ligand selectivity based on protein binding site analysis.
J Med Chem 49: 51-69 (2006)
Aventis Pharma Deutschland
Isothiazolopyridones: synthesis, structure, and biological activity of a new class of antibacterial agents.
J Med Chem 49: 39-42 (2006)
Achillion Pharmaceuticals
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.
J Med Chem 49: 35-8 (2006)
Merck Sharp Laboratory
Anthrax lethal factor protease inhibitors: synthesis, SAR, and structure-based 3D QSAR studies.
J Med Chem 49: 27-30 (2006)
Burnham Institute
6H,13H-Pyrazino[1,2-a;4,5-a']diindole analogs: probing the pharmacophore for allosteric ligands of muscarinic M2 receptors.
Bioorg Med Chem Lett 16: 1481-5 (2006)
University Of W£Rzburg
Depeptidization efforts on P3-P2' alpha-ketoamide inhibitors of HCV NS3-4A serine protease: effect on HCV replicon activity.
Bioorg Med Chem Lett 16: 1621-7 (2006)
Schering-Plough Research Institute
Structural modifications of the cannabinoid side chain towards C3-aryl and 1',1'-cycloalkyl-1'-cyano cannabinoids.
Bioorg Med Chem Lett 16: 1616-20 (2006)
National Hellenic Research Foundation
1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors.
Bioorg Med Chem Lett 16: 1574-8 (2006)
Procter & Gamble Pharmaceuticals
Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17beta-hydroxysteroid dehydrogenase type 3.
Bioorg Med Chem Lett 16: 1532-6 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
8-Fluoroimidazo[1,2-a]pyridine: synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABA A receptor.
Bioorg Med Chem Lett 16: 1518-22 (2006)
Merck Sharp And Dohme Research Laboratories
Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Bioorg Med Chem Lett 16: 1477-80 (2006)
Merck Sharp And Dohme Research Laboratories
Guanidinylated 2,5-dideoxystreptamine derivatives as anthrax lethal factor inhibitors.
Bioorg Med Chem Lett 16: 1527-31 (2006)
Hawaii Biotech
Discovery and SAR study of novel dihydroquinoline containing glucocorticoid receptor ligands.
Bioorg Med Chem Lett 16: 1549-52 (2006)
Boehringer Ingelheim Pharmaceuticals
Synthesis and insecticidal activity of fluorinated 2-(2,6-dichloro-4-trifluoromethylphenyl)-2,4,5,6-tetrahydrocyclopentapyrazoles.
Bioorg Med Chem Lett 16: 1702-6 (2006)
Johnson & Johnson Pharmaceutical Research And Development
Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II.
Bioorg Med Chem Lett 16: 1579-81 (2006)
Imclone Systems
Discovery and optimization of a novel series of liver X receptor-alpha agonists.
Bioorg Med Chem Lett 16: 1638-42 (2006)
Amgen
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Bioorg Med Chem Lett 16: 1582-5 (2006)
Merck Sharp And Dohme Research Laboratories
Design and synthesis of potent and subtype-selective PPARalpha agonists.
Bioorg Med Chem Lett 16: 1673-8 (2006)
Merck Research Laboratories
CDK2/cyclinA inhibitors: targeting the cyclinA recruitment site with small molecules derived from peptide leads.
Bioorg Med Chem Lett 16: 1716-20 (2006)
Genentech
Novel lactam NK1 antagonists with anti-emetic activity.
Bioorg Med Chem Lett 16: 1197-201 (2006)
Merck Sharp & Dohme Research Laboratories
Interaction of ivermectin with multidrug resistance proteins (MRP1, 2 and 3).
Chem Biol Interact 159: 169-79 (2006)
Laboratoire De Pharmacologie-Toxicologie Inra
Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket.
Bioorg Med Chem Lett 16: 1633-7 (2006)
Astrazeneca
Novel dual inhibitors of calpain and lipid peroxidation with enhanced cellular activity.
Bioorg Med Chem Lett 16: 1586-9 (2006)
Institut Henri Beaufour
Structure-activity relationships of alpha-amino acid ligands for the alpha2delta subunit of voltage-gated calcium channels.
Bioorg Med Chem Lett 16: 1138-41 (2006)
Abbott Laboratories
Indole-glucosides as novel sodium glucose co-transporter 2 (SGLT2) inhibitors. Part 2.
Bioorg Med Chem Lett 16: 1696-701 (2006)
Johnson & Johnson Pharmaceutical Research And Development
Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues.
Bioorg Med Chem Lett 16: 1142-5 (2006)
Astrazeneca R&D
Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: potent and selective aromatase inhibitors.
Bioorg Med Chem Lett 16: 1134-7 (2006)
Nantes University
5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers.
Bioorg Med Chem Lett 16: 1202-6 (2006)
Pfizer
Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists.
Bioorg Med Chem Lett 16: 1544-8 (2006)
Schering-Plough Research Institute
4-Aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors.
Bioorg Med Chem Lett 16: 1502-5 (2006)
Sankyo
Nostocarboline: isolation and synthesis of a new cholinesterase inhibitor from Nostoc 78-12A.
J Nat Prod 68: 1793-5 (2005)
University Of ZüRich
Synthesis, biological evaluation, and pharmacokinetic study of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives as VLA-4 antagonists.
Bioorg Med Chem 14: 2725-46 (2006)
Daiichi Pharmaceutical
Novel endotoxin-sequestering compounds with terephthalaldehyde-bis-guanylhydrazone scaffolds.
Bioorg Med Chem Lett 16: 1305-8 (2006)
University Of Kansas
The reversed binding of beta-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors.
Bioorg Med Chem Lett 16: 1744-8 (2006)
Santhera Pharmaceuticals
Asymmetric synthesis of the L-fuco-nojirimycin, a nanomolar alpha-L-fucosidase inhibitor.
Bioorg Med Chem Lett 16: 1172-4 (2006)
Université
New benzimidazoles as thrombopoietin receptor agonists.
Bioorg Med Chem Lett 16: 1212-6 (2006)
Glaxosmithkline
Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1.
Bioorg Med Chem Lett 16: 1731-4 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis of Tic-D-Phe Psi[CH2-CH2] isostere and its use in the development of melanocortin receptor agonists.
Bioorg Med Chem Lett 16: 1721-5 (2006)
Procter & Gamble Pharmaceuticals
Novel, potent P2-P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors.
Bioorg Med Chem Lett 16: 1735-9 (2006)
Glaxosmithkline
Actin is the primary cellular receptor of bistramide A.
Nat Chem Biol 1: 383-8 (2005)
University Of Chicago
C3-symmetric peptide scaffolds are functional mimetics of trimeric CD40L.
Nat Chem Biol 1: 377-82 (2005)
Institut De Biologie MoléCulaire Et Cellulaire
Monocarboxylate transporter MCT1 is a target for immunosuppression.
Nat Chem Biol 1: 371-6 (2005)
Astrazeneca R&D Charnwood
Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.
Bioorg Med Chem Lett 16: 1146-50 (2006)
Merck Research Laboratories
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
J Med Chem 48: 8289-98 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Synthesis of tricyclic 1,3-oxazin-4-ones and kinetic analysis of cholesterol esterase and acetylcholinesterase inhibition.
J Med Chem 48: 8270-88 (2005)
University Of Bonn
2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching.
J Med Chem 48: 8253-60 (2005)
Universit£
Methyl substitution on the piperidine ring of N-[omega-(6-methoxynaphthalen-1-yl)alkyl] derivatives as a probe for selective binding and activity at the sigma(1) receptor.
J Med Chem 48: 8237-44 (2005)
Universit£
Synthesis, biological activity, and preliminary pharmacokinetic evaluation of analogues of a phosphosulfomannan angiogenesis inhibitor (PI-88).
J Med Chem 48: 8229-36 (2005)
Progen Industries
Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities.
J Med Chem 48: 8194-208 (2005)
National Health Research Institutes
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.
J Med Chem 48: 8163-73 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Binding of rasagiline-related inhibitors to human monoamine oxidases: a kinetic and crystallographic analysis.
J Med Chem 48: 8148-54 (2005)
University Of Pavia
Estradiol-adenosine hybrid compounds designed to inhibit type 1 17beta-hydroxysteroid dehydrogenase.
J Med Chem 48: 8134-47 (2005)
Chuq-Pavillon Chul And Université
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
J Med Chem 48: 8112-4 (2005)
University Of Cagliari
Human P2Y(6) receptor: molecular modeling leads to the rational design of a novel agonist based on a unique conformational preference.
J Med Chem 48: 8108-11 (2005)
Niddk
Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.
J Med Chem 48: 8103-7 (2005)
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists.
Bioorg Med Chem Lett 16: 1749-52 (2006)
Glaxosmithkline
2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.
Bioorg Med Chem Lett 16: 1726-30 (2006)
Chemical Diversity
Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands.
Bioorg Med Chem Lett 16: 1130-3 (2006)
Merck Research Laboratories
Aza-retinoids as novel retinoid X receptor-specific agonists.
Bioorg Med Chem Lett 16: 2352-6 (2006)
Ligand Pharmaceuticals
Probing structure/affinity relationships for the Plasmodium falciparum hexose transporter with glucose derivatives.
Bioorg Med Chem Lett 16: 1267-71 (2006)
Université
Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.
Bioorg Med Chem Lett 16: 1207-11 (2006)
F. Hoffmann-La Roche
Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Bioorg Med Chem Lett 16: 1151-5 (2006)
Cephalon
A topological function based on spectral moments for predicting affinity toward A3 adenosine receptors.
Bioorg Med Chem Lett 16: 1291-6 (2006)
Vigo University
Synthesis of 3-benzyl-2-substituted quinoxalines as novel monoamine oxidase A inhibitors.
Bioorg Med Chem Lett 16: 1753-6 (2006)
University Of Alexandria
Protein tyrosine phosphatase 1B inhibitors from Morus root bark.
Bioorg Med Chem Lett 16: 1426-9 (2006)
Korea Research Institute Of Bioscience And Biotechnology (Kribb)
Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis.
Proc Natl Acad Sci U S A 102: 18620-5 (2005)
Mcgill University
Triaminotriazine DNA helicase inhibitors with antibacterial activity.
Bioorg Med Chem Lett 16: 1286-90 (2006)
Targanta Therapeutics
Pharmacological characterization of (E)-N-(4-fluorobut-2-enyl)-2beta-carbomethoxy-3beta-(4'-tolyl)nortropane (LBT-999) as a highly promising fluorinated ligand for the dopamine transporter.
J Pharmacol Exp Ther 317: 147-52 (2006)
University Of Tours
Thyroid receptor ligands. Part 5: novel bicyclic agonist ligands selective for the thyroid hormone receptor beta.
Bioorg Med Chem Lett 16: 1240-4 (2006)
Karo Bio
The discovery of a potent and selective lethal factor inhibitor for adjunct therapy of anthrax infection.
Bioorg Med Chem Lett 16: 964-8 (2006)
Merck Research Laboratories
Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligands.
Bioorg Med Chem Lett 16: 1297-300 (2006)
University Of Tours
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
Bioorg Med Chem Lett 16: 1272-6 (2006)
Achillion Pharmaceuticals
Aminoalkyl phenyl sulfones--a novel series of 5-HT7 receptor ligands.
Bioorg Med Chem Lett 16: 1255-8 (2006)
Merck Sharp And Dohme Research Laboratories
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
Bioorg Med Chem Lett 16: 1277-81 (2006)
Achillion Pharmaceuticals
Identification of phosphodiesterase-1 and 5 dual inhibitors by a ligand-based virtual screening optimized for lead evolution.
Bioorg Med Chem Lett 16: 1371-9 (2006)
Sumitomo Pharmaceuticals
High-resolution crystal structure of aldose reductase complexed with the novel sulfonyl-pyridazinone inhibitor exhibiting an alternative active site anchoring group.
J Mol Biol 356: 45-56 (2006)
Philipps University Marburg
SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors.
Bioorg Med Chem Lett 16: 1320-23 (2006)
Astrazeneca
Synthesis and SAR of 1,2-trans-(1-hydroxy-3-phenylprop-1-yl)cyclopentane carboxamide derivatives, a new class of sodium channel blockers.
Bioorg Med Chem Lett 16: 1358-61 (2006)
Merck Research Laboratories
Design and synthesis of 2'-anilino-4,4'-bipyridines as selective inhibitors of c-Jun N-terminal kinase-3.
Bioorg Med Chem Lett 16: 1397-401 (2006)
Astrazeneca R&D SöDertäLje
Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase.
Bioorg Med Chem Lett 16: 1335-7 (2006)
Academy Of Sciences Of The Czech Republic
From pyrroles to pyrrolo[1,2-a]pyrazinones: a new class of mGluR1 antagonists.
Bioorg Med Chem Lett 16: 1342-5 (2006)
Glaxosmithkline
A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold.
J Med Chem 48: 8098-102 (2005)
Uppsala University
Antitrypanosomal, antileishmanial, and antimalarial activities of quaternary arylalkylammonium 2-amino-4-chlorophenyl phenyl sulfides, a new class of trypanothione reductase inhibitor, and of N-acyl derivatives of 2-amino-4-chlorophenyl phenyl sulfide.
J Med Chem 48: 8087-97 (2005)
University Of Manchester
cycloSal-PMEA and cycloAmb-PMEA: potentially new phosphonate prodrugs based on the cycloSal-pronucleotide approach.
J Med Chem 48: 8079-86 (2005)
University Of Hamburg
Synthesis and biological evaluation of a novel series of"ortho-nitrated" inhibitors of catechol-O-methyltransferase.
J Med Chem 48: 8070-8 (2005)
Department Of Research & Development
Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1.
J Med Chem 48: 8045-54 (2005)
Elixir Pharmaceuticals
Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
J Med Chem 48: 8035-44 (2005)
Kobe Gakuin University
Diketo acid pharmacophore. 2. Discovery of structurally diverse inhibitors of HIV-1 integrase.
J Med Chem 48: 8009-15 (2005)
University Of Southern California
Chemoenzymatic synthesis of a series of 4-substituted glutamate analogues and pharmacological characterization at human glutamate transporters subtypes 1-3.
J Med Chem 48: 7980-92 (2005)
Université
Further structure-activity relationship studies of piperidine-based monoamine transporter inhibitors: effects of piperidine ring stereochemistry on potency. Identification of norepinephrine transporter selective ligands and broad-spectrum transporter inhibitors.
J Med Chem 48: 7970-9 (2005)
University Of Illinois At Chicago
Use of structure-based drug design approaches to obtain novel anthranilic acid acyl carrier protein synthase inhibitors.
J Med Chem 48: 7960-9 (2005)
Wyeth Research
1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.
J Med Chem 48: 7932-45 (2005)
Università
First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.
J Med Chem 48: 7919-22 (2005)
Università
Studies toward the discovery of the next generation of antidepressants. Part 5: 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives with dual 5-HT1A receptor and serotonin transporter affinity.
Bioorg Med Chem Lett 16: 1338-41 (2006)
Wyeth Research
Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors.
Bioorg Med Chem Lett 16: 1346-9 (2006)
Merck Research Laboratories
Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.
Bioorg Med Chem Lett 16: 1362-5 (2006)
F. Hoffmann-La Roche
Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
Bioorg Med Chem Lett 16: 1350-2 (2006)
University Of Pennsylvania
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.
Bioorg Med Chem Lett 16: 1353-7 (2006)
Vernalis (R&D)
Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.
Bioorg Med Chem Lett 16: 1440-4 (2006)
Chemical Diversity
Naphthofuroquinone derivatives: inhibition of receptor tyrosine kinases.
Bioorg Med Chem Lett 16: 737-42 (2005)
Korea Research Institute Of Chemical Technology
Expedited SAR study of high-affinity ligands to the alpha(2)delta subunit of voltage-gated calcium channels: Generation of a focused library using a solution-phase Sn2Ar coupling methodology.
Bioorg Med Chem Lett 16: 746-9 (2005)
Merck Research Laboratories
Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer.
Bioorg Med Chem Lett 16: 1402-4 (2006)
Università
In silico fragment-based discovery of DPP-IV S1 pocket binders.
Bioorg Med Chem Lett 16: 1405-9 (2006)
Santhera Pharmaceuticals
Sarcosine based indandione hGlyT1 inhibitors.
Bioorg Med Chem Lett 16: 1388-91 (2006)
Merck Sharp And Dohme Research Laboratories
Strong solute-solute dispersive interactions in a protein-ligand complex.
J Am Chem Soc 127: 17061-7 (2005)
University Of Leeds
Designing rapid onset selective serotonin re-uptake inhibitors. Part 1: Structure-activity relationships of substituted (1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydro-1-naphthaleneamine.
Bioorg Med Chem Lett 16: 1434-9 (2006)
Pfizer
Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels.
Bioorg Med Chem Lett 16: 798-802 (2006)
Ajinomoto
Androstenediol analogs as ER-beta-selective SERMs.
Bioorg Med Chem Lett 16: 834-8 (2006)
Merck Research Laboratories
Synthesis and pharmacochemical study of novel polyfunctional molecules combining anti-inflammatory, antioxidant, and hypocholesterolemic properties.
Bioorg Med Chem Lett 16: 825-9 (2006)
Aristotelian University Of Thessaloniki
(+)-Myristinins A and D from Knema elegans, which inhibit DNA polymerase beta and cleave DNA.
J Nat Prod 68: 1625-8 (2005)
University Of Virginia
Free-radical-scavenging and xanthine oxidase inhibitory constituents from Stereospermum personatum.
J Nat Prod 68: 1615-21 (2005)
Institute Of Chemical Technology
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
Bioorg Med Chem Lett 16: 821-4 (2006)
Gsk
Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists.
Bioorg Med Chem Lett 16: 811-4 (2006)
Merck Sharp & Dohme Research Laboratories
Bicyclic and tricyclic thiophenes as protein tyrosine phosphatase 1B inhibitors.
Bioorg Med Chem 14: 2162-77 (2006)
Wyeth Research
Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.
Bioorg Med Chem Lett 16: 884-6 (2006)
Karo Bio
Synthesis of 2,5-thiazole butanoic acids as potent and selective alpha(v)beta3 integrin receptor antagonists with improved oral pharmacokinetic properties.
Bioorg Med Chem Lett 16: 845-9 (2006)
Pfizer
Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.
J Med Chem 48: 7882-905 (2005)
Serono Pharmaceutical Research Institute
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
J Med Chem 48: 7867-81 (2005)
University Walk
Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
J Med Chem 48: 7860-6 (2005)
Kochi Medical School
On the use of nonfluorescent dye labeled ligands in FRET-based receptor binding studies.
J Med Chem 48: 7847-59 (2005)
Umr Cnrs/Ulp 7081
Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach.
J Med Chem 48: 7829-46 (2005)
School Of Natural Sciences--Chemistry
Adenosine kinase inhibitors. 6. Synthesis, water solubility, and antinociceptive activity of 5-phenyl-7-(5-deoxy-beta-D-ribofuranosyl)pyrrolo[2,3-d]pyrimidines substituted at C4 with glycinamides and related compounds.
J Med Chem 48: 7808-20 (2005)
Metabasis Therapeutics
Design, synthesis, and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors.
J Med Chem 48: 7789-95 (2005)
Sapienza University Of Rome
Small molecule inhibitors of dynamin I GTPase activity: development of dimeric tyrphostins.
J Med Chem 48: 7781-8 (2005)
The University Of Newcastle
Structure-activity relationships in 1,4-benzodioxan-related compounds. 8.(1) {2-[2-(4-chlorobenzyloxy)phenoxy]ethyl}-[2-(2,6-dimethoxyphenoxy)ethyl]amine (clopenphendioxan) as a tool to highlight the involvement of alpha1D- and alpha1B-adrenoreceptor subtypes in the regulation of human PC-3 prostate
J Med Chem 48: 7750-63 (2005)
Universit£
Syntheses, biological evaluation, and molecular modeling of 18F-labeled 4-anilidopiperidines as mu-opioid receptor imaging agents.
J Med Chem 48: 7720-32 (2005)
Technische UniversitäT MüNchen
Mono- or diphenylpyridazines connected to N-(2,4-difluorophenyl)-N'-heptylurea as acyl-CoA:cholesterol acyltransferase inhibitors.
J Med Chem 48: 7708-13 (2005)
Università
Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
J Med Chem 48: 7688-707 (2005)
Rheinische Friedrich-Wilhelms-Universitat Bonn
Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
J Med Chem 48: 7675-87 (2005)
Universit£
Conformationally constrained CCK4 analogues incorporating IBTM and BTD beta-turn mimetics.
J Med Chem 48: 7667-74 (2005)
Instituto De QuíMica MéDica (Csic)
N-benzylisatin sulfonamide analogues as potent caspase-3 inhibitors: synthesis, in vitro activity, and molecular modeling studies.
J Med Chem 48: 7637-47 (2005)
Washington University
Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase.
J Med Chem 48: 7604-14 (2005)
Oxford University
3,6-disubstituted coumarins as mechanism-based inhibitors of thrombin and factor Xa.
J Med Chem 48: 7592-603 (2005)
University Of Namur
2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2.
J Med Chem 48: 7560-81 (2005)
Wyeth Research
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
J Med Chem 48: 7535-43 (2005)
Merck Frosst Centre For Therapeutic Research
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
J Med Chem 48: 7520-34 (2005)
Celera Genomics
Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist.
J Med Chem 48: 7517-9 (2005)
Acadia Pharmaceuticals
Rhodamine-labeled 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)tropane analogues as high-affinity fluorescent probes for the dopamine transporter.
J Med Chem 48: 7513-6 (2005)
National Institute On Drug Abuse-Intramural Research Program
Substituted 4-hydroxyphenyl sulfonamides as pathway-selective estrogen receptor ligands.
Bioorg Med Chem Lett 16: 854-8 (2006)
Wyeth Research
Aplysamine-1 and related analogs as histamine H3 receptor antagonists.
Bioorg Med Chem Lett 16: 897-900 (2006)
Johnson & Johnson Pharmaceutical Research And Development
Inhibition of DNA helicases with DNA-competitive inhibitors.
Bioorg Med Chem Lett 16: 923-7 (2006)
Novartis Institutes For Biomedical Research
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors possessing augmented P2' side chains.
Bioorg Med Chem Lett 16: 859-63 (2006)
University Of Pennsylvania
Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective opioid antagonists.
Bioorg Med Chem Lett 16: 864-8 (2006)
Adolor
Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 5.
Bioorg Med Chem Lett 16: 2347-51 (2006)
Eli Lilly
Novel non-nucleobase inhibitors of Staphylococcus aureus DNA polymerase IIIC.
Bioorg Med Chem Lett 16: 891-6 (2006)
Targanta Therapeutics
Enhanced FTase activity achieved via piperazine interaction with catalytic zinc.
Bioorg Med Chem Lett 16: 984-8 (2006)
Schering-Plough Research Institute
Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists.
Bioorg Med Chem Lett 16: 839-44 (2006)
Pfizer
Hit-to-Lead studies: the discovery of potent, orally bioavailable thiazolopyrimidine CXCR2 receptor antagonists.
Bioorg Med Chem Lett 16: 960-3 (2006)
Astrazeneca R&D Charnwood
Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.
Bioorg Med Chem Lett 16: 954-9 (2006)
Wyeth Research
Synthesis and evaluation of 2-anilino-3-phenylsulfonyl-6-methylpyridines as corticotropin-releasing factor1 receptor ligands.
Bioorg Med Chem Lett 16: 934-7 (2006)
Pharmaceutical Research Institute
Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor.
Bioorg Med Chem Lett 16: 2341-6 (2006)
Eli Lilly
Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.
Bioorg Med Chem Lett 16: 989-94 (2006)
The Schering Plough Research Institute
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
Bioorg Med Chem Lett 16: 978-83 (2006)
Glaxosmithkline
Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.
Bioorg Med Chem Lett 16: 938-42 (2006)
Cephalon
Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1.
Bioorg Med Chem Lett 16: 905-10 (2006)
Pfizer
Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase.
Bioorg Med Chem Lett 16: 1040-4 (2006)
Kudos Pharmaceuticals
Phenolic P2/P3 core motif as thrombin inhibitors--design, synthesis, and X-ray co-crystal structure.
Bioorg Med Chem Lett 16: 1032-6 (2006)
Universit£
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.
Bioorg Med Chem Lett 16: 1084-90 (2006)
Nerviano Medical Sciences
Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II"selective" inhibitor celecoxib.
Bioorg Med Chem Lett 16: 437-42 (2005)
Istituto Di Biostrutture E Bioimmagini-Cnr
Inhibition of GABA shunt enzymes' activity by 4-hydroxybenzaldehyde derivatives.
Bioorg Med Chem Lett 16: 592-5 (2005)
Huazhong University Of Science And Technology
Pyridazines part 41: synthesis, antiplatelet activity and SAR of 2,4,6-substituted 5-(3-oxo-3-phenylprop-1-en-1-yl)- or 5-(3-phenylprop-2-enoyl)pyridazin-3(2H)-ones.
Bioorg Med Chem Lett 16: 1080-3 (2006)
Universidad De Santiago De Compostela
Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions.
Bioorg Med Chem Lett 16: 1065-9 (2006)
Schering-Plough Research Institute
Design of novel hexahydropyrazinoquinolines as potent and selective dopamine D3 receptor ligands with improved solubility.
Bioorg Med Chem Lett 16: 443-6 (2005)
University Of Michigan
Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: 1H-pyrimidin-2-one derivatives.
Bioorg Med Chem Lett 16: 490-4 (2005)
Abbott
Identification of Darmstoff analogs as selective agonists and antagonists of lysophosphatidic acid receptors.
Bioorg Med Chem Lett 16: 451-6 (2005)
University Of Tennessee Health Science Center
Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification.
Bioorg Med Chem 14: 1792-804 (2006)
Vernalis (R&D)
PTP-1B inhibitors: cyclopenta[d][1,2]-oxazine derivatives.
Bioorg Med Chem Lett 16: 499-502 (2005)
Korea Research Institute Of Chemical Technology
Conversion of potent MMP inhibitors into selective TACE inhibitors.
Bioorg Med Chem Lett 16: 1028-31 (2006)
Bristol-Myers Squibb Pharmaceutical Research Institute
Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety.
Bioorg Med Chem Lett 16: 596-601 (2005)
National Institute Of Diabetes And Digestive And Kidney Diseases
6-Acylamino-2-amino-4-methylquinolines as potent melanin-concentrating hormone 1 receptor antagonists: structure-activity exploration of eastern and western parts.
Bioorg Med Chem Lett 16: 1070-5 (2006)
7Tm Pharma
Guiding farnesyltransferase inhibitors from an ECLiPS library to the catalytic zinc.
Bioorg Med Chem Lett 16: 507-11 (2005)
Pharmacopeia
A novel nicotinic acetylcholine receptor antagonist radioligand for PET studies.
Bioorg Med Chem Lett 16: 1049-53 (2006)
Brookhaven National Laboratory
Intermolecular interactions in the crystal structures of potential HIV-1 integrase inhibitors.
Bioorg Med Chem Lett 16: 1005-9 (2006)
Jagiellonian University
The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex--Part 2.
Bioorg Med Chem Lett 16: 1060-4 (2006)
Pfizer
Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modeling.
Bioorg Med Chem 14: 1378-90 (2006)
Fujisawa Pharmaceutical
In silico design and synthesis of piperazine-1-pyrrolidine-2,5-dione scaffold-based novel malic enzyme inhibitors.
Bioorg Med Chem Lett 16: 525-8 (2005)
Cytrx Laboratories
Random chemistry as a new tool for the generation of small compound libraries: development of a new acetylcholinesterase inhibitor.
J Med Chem 48: 7496-9 (2005)
University Of WüRzburg
Synthesis and pharmacological characterization of exo-2-(2'-chloro-5-pyridinyl)-7-(endo and exo)-aminobicyclo[2.2.1]heptanes as novel epibatidine analogues.
J Med Chem 48: 7491-5 (2005)
Research Triangle Institute
1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: new templates among the CB1 cannabinoid receptor inverse agonists.
J Med Chem 48: 7486-90 (2005)
Universit£
Anilinodialkoxyquinazolines: screening epidermal growth factor receptor tyrosine kinase inhibitors for potential tumor imaging probes.
J Med Chem 48: 7445-56 (2005)
Lawrence Berkeley National Laboratory
Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes.
J Med Chem 48: 7437-44 (2005)
Research Triangle Institute
Irreversible inactivation of trypanothione reductase by unsaturated Mannich bases: a divinyl ketone as key intermediate.
J Med Chem 48: 7400-10 (2005)
Biochemie-Zentrum Der UniversitäT Heidelberg
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
J Med Chem 48: 7374-88 (2005)
Abbott Laboratories
Tricyclic pyrazoles. 3. Synthesis, biological evaluation, and molecular modeling of analogues of the cannabinoid antagonist 8-chloro-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide.
J Med Chem 48: 7351-62 (2005)
Università
Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors.
J Med Chem 48: 7343-50 (2005)
Universit£
Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach to designing exopeptidase inhibitors.
J Med Chem 48: 7333-42 (2005)
University College London
Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach.
J Med Chem 48: 7282-9 (2005)
University Of Bologna
Radioiodinated flavones for in vivo imaging of beta-amyloid plaques in the brain.
J Med Chem 48: 7253-60 (2005)
Nagasaki University
Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase.
J Med Chem 48: 7243-52 (2005)
University Of Michigan
Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease.
J Med Chem 48: 7223-33 (2005)
Neuropharma
Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrofolate reductase and thymidylate synthase and a
J Med Chem 48: 7215-22 (2005)
Duquesne University
Synthesis and 3D QSAR of new pyrazolo[3,4-b]pyridines: potent and selective inhibitors of A1 adenosine receptors.
J Med Chem 48: 7172-85 (2005)
Università
Virtual screening of novel CB2 ligands using a comparative model of the human cannabinoid CB2 receptor.
J Med Chem 48: 7166-71 (2005)
University Of Kuopio
Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-(1H)- pyrazole derivatives.
J Med Chem 48: 7113-22 (2005)
Sapienza University Of Rome
SAR and 3D-QSAR studies on thiadiazolidinone derivatives: exploration of structural requirements for glycogen synthase kinase 3 inhibitors.
J Med Chem 48: 7103-12 (2005)
Instituto De Quimica Medica (Csic)
Synthesis and characterization of the novel fluorescent prolyl oligopeptidase inhibitor 4-fluoresceinthiocarbamoyl-6-aminocaproyl-L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine.
J Med Chem 48: 7093-5 (2005)
University Of Kuopio
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.
J Med Chem 48: 7089-92 (2005)
Merck Sharp And Dohme Research Laboratories
Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S.
J Mol Biol 354: 789-800 (2005)
Georgia State University
Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists.
Bioorg Med Chem Lett 16: 302-6 (2005)
Cv Therapeutics
Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.
Bioorg Med Chem Lett 16: 373-7 (2005)
Ucb Pharma
Synthesis and biological activity of the first cyclic biphalin analogues.
Bioorg Med Chem Lett 16: 367-72 (2005)
University Of Arizona
Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors.
Bioorg Med Chem Lett 16: 311-6 (2006)
Wyeth Research
New tyrosinase inhibitors selected by atomic linear indices-based classification models.
Bioorg Med Chem Lett 16: 324-30 (2005)
Central University Of Las Villas
Substituted indanylacetic acids as PPAR-alpha-gamma activators.
Bioorg Med Chem Lett 16: 297-301 (2005)
Bayer Research Center
4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.
Bioorg Med Chem Lett 16: 280-4 (2006)
Merck Research Laboratories
Design and synthesis of substituted phenylpropanoic acid derivatives as human peroxisome proliferator-activated receptor alpha/delta dual agonists.
Bioorg Med Chem Lett 16: 554-8 (2005)
University Of Tokyo
Pyrrolopyridazine MEK inhibitors.
Bioorg Med Chem Lett 16: 628-32 (2005)
Pharmaceutical Research Institute
5-heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure-activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog.
Bioorg Med Chem Lett 16: 288-92 (2005)
Veterinary Medicine Research And Development Pfizer
Design, synthesis, and vasorelaxant and platelet antiaggregatory activities of coumarin-resveratrol hybrids.
Bioorg Med Chem Lett 16: 257-61 (2005)
Universidad De Santiago De Compostela
N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II.
Bioorg Med Chem Lett 16: 602-6 (2006)
Chemical Diversity
A new chemical tool for exploring the physiological function of the PDE2 isozyme.
Bioorg Med Chem Lett 16: 307-10 (2005)
Pfizer
Tethering identifies fragment that yields potent inhibitors of human caspase-1.
Bioorg Med Chem Lett 16: 559-62 (2005)
Sunesis Pharmaceuticals
Design and synthesis of 3,4-dihydro-1H-[1]-benzothieno[2,3-c]pyran and 3,4-dihydro-1H-pyrano[3,4-b]benzofuran derivatives as non-nucleoside inhibitors of HCV NS5B RNA dependent RNA polymerase.
Bioorg Med Chem Lett 16: 457-60 (2005)
Wyeth Research
Isolation and cholinesterase-inhibition studies of sterols from Haloxylon recurvum.
Bioorg Med Chem Lett 16: 573-80 (2005)
University Of Karachi
Design, synthesis and structure-activity relationships of new phosphinate inhibitors of MurD.
Bioorg Med Chem Lett 16: 343-8 (2005)
University Of Ljubljana
Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.geneste@abbott.com.
Bioorg Med Chem Lett 16: 658-62 (2005)
Abbott
Side-chain modified analogues of histaprodifen: asymmetric synthesis and histamine H1-receptor activity.
Bioorg Med Chem Lett 16: 672-6 (2006)
Universit£T Regensburg
Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.
Bioorg Med Chem Lett 16: 681-5 (2005)
Merck Research Laboratories
New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.
Bioorg Med Chem Lett 16: 731-6 (2005)
Pfizer
Synthesis and pharmacological evaluation of second-generation phosphatidic acid derivatives as lysophosphatidic acid receptor ligands.
Bioorg Med Chem Lett 16: 633-40 (2005)
University Of Tennessee Health Science Center
Conformationally biased P3 amide replacements of beta-secretase inhibitors.
Bioorg Med Chem Lett 16: 641-4 (2006)
Merck Research Laboratories
Design, synthesis and in vitro antimalarial activity of an acylhydrazone library.
Bioorg Med Chem Lett 16: 31-5 (2005)
Universit£
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
Bioorg Med Chem Lett 16: 718-21 (2005)
Pfizer
Novel phenylamino acetamide derivatives as potent and selective kappa opioid receptor agonists.
Bioorg Med Chem Lett 16: 645-8 (2005)
Adolor
A concise asymmetric route for the synthesis of a novel class of glucocorticoid mimetics containing a trifluoromethyl-substituted alcohol.
Bioorg Med Chem Lett 16: 654-7 (2005)
Boehringer Ingelheim Pharmaceuticals
The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.
Bioorg Med Chem Lett 16: 378-81 (2005)
Glaxosmithkline
Synthesis of N-benzylated-2-aminoquinolines as ligands for the Tec SH3 domain.
Bioorg Med Chem Lett 16: 387-90 (2005)
The University Of Adelaide
Tetrahydrobenzothiophene inhibitors of hepatitis C virus NS5B polymerase.
Bioorg Med Chem Lett 16: 100-3 (2005)
Viropharma
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
Bioorg Med Chem Lett 16: 677-80 (2005)
Vernalis
Derivatives of tramadol for increased duration of effect.
Bioorg Med Chem Lett 16: 691-4 (2005)
Sepracor
Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.
Bioorg Med Chem Lett 16: 710-3 (2005)
Celera
Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 1: Weakly basic azoles.
Bioorg Med Chem Lett 16: 338-42 (2005)
Merck Research Laboratories
Design and synthesis of heterocyclic malonyl-CoA decarboxylase inhibitors.
Bioorg Med Chem Lett 16: 695-700 (2005)
Chugai Pharma Usa
Anti-inflammatory acylphloroglucinol derivatives from Hops (Humulus lupulus).
J Nat Prod 68: 1545-8 (2005)
Fr. 8.2 Pharmakognosie Und Analytische Phytochemie Der UniversitäT Des Saarlandes
Phenolic and triterpene glycosides from the stems of Ilex litseaefolia.
J Nat Prod 68: 1531-5 (2005)
Chinese Academy Of Sciences
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.
J Nat Prod 68: 1514-8 (2005)
Chinese Academy Of Sciences
Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors.
J Med Chem 48: 7084-8 (2005)
Università
Synthesis and antibacterial activity of 3-substituted-6-(3-ethyl-4-methylanilino)uracils.
J Med Chem 48: 7063-74 (2005)
Glsynthesis
Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency.
J Med Chem 48: 7040-8 (2005)
University Of Bonn
Synthesis of 5-nitro-2-furancarbohydrazides and their cis-diamminedichloroplatinum complexes as bitopic and irreversible human thioredoxin reductase inhibitors.
J Med Chem 48: 7024-39 (2005)
Umr 8525 Cnrs-Université
11C-labeling of n-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]arylcarboxamide derivatives and evaluation as potential radioligands for PET imaging of dopamine D3 receptors.
J Med Chem 48: 7018-23 (2005)
University Of Milano/Bicocca
Extraction and visualization of potential pharmacophore points using support vector machines: application to ligand-based virtual screening for COX-2 inhibitors.
J Med Chem 48: 6997-7004 (2005)
Johann Wolfgang Goethe-UniversitäT
Fast small molecule similarity searching with multiple alignment profiles of molecules represented in one-dimension.
J Med Chem 48: 6980-90 (2005)
Pharmacopeia
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics.
J Med Chem 48: 6956-69 (2005)
Glaxosmithkline
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.
J Med Chem 48: 6948-55 (2005)
Universit£
Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library.
J Med Chem 48: 6908-17 (2005)
Brown University
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
J Med Chem 48: 6887-96 (2005)
Universit£
Azepanone-based inhibitors of human cathepsin L.
J Med Chem 48: 6870-8 (2005)
Glaxosmithkline
Synthesis, structure-activity relationships, and biological properties of 1-heteroaryl-4-[omega-(1H-indol-3-yl)alkyl]piperazines, novel potential antipsychotics combining potent dopamine D2 receptor antagonism with potent serotonin reuptake inhibition.
J Med Chem 48: 6855-69 (2005)
Solvay Pharma
Pyrazolo[3,4-c]pyridazines as novel and selective inhibitors of cyclin-dependent kinases.
J Med Chem 48: 6843-54 (2005)
Universidad San Pablo Ceu
Molecular modeling and molecular dynamics simulation of the human A2B adenosine receptor. The study of the possible binding modes of the A2B receptor antagonists.
J Med Chem 48: 6813-20 (2005)
M.V. Lomonosov Moscow State University
Optimization of the in vitro and in vivo properties of a novel series of 2,4,5-trisubstituted imidazoles as potent cholecystokinin-2 (CCK2) antagonists.
J Med Chem 48: 6803-12 (2005)
James Black Foundation
Scaffold hopping with molecular field points: identification of a cholecystokinin-2 (CCK2) receptor pharmacophore and its use in the design of a prototypical series of pyrrole- and imidazole-based CCK2 antagonists.
J Med Chem 48: 6790-802 (2005)
James Black Foundation
A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats.
J Med Chem 48: 6772-5 (2005)
Eli Lilly
Design and synthesis of peptidomimetic severe acute respiratory syndrome chymotrypsin-like protease inhibitors.
J Med Chem 48: 6767-71 (2005)
Purdue University
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.
Proc Natl Acad Sci U S A 102: 16078-83 (2005)
Glaxosmithkline
The structure of dimeric ROCK I reveals the mechanism for ligand selectivity.
J Biol Chem 281: 260-8 (2006)
Vertex Pharmaceuticals
Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B.
Bioorg Med Chem 14: 1255-73 (2006)
Uk Centre For Cancer Therapeutics
Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.
Bioorg Med Chem Lett 16: 262-6 (2005)
Novartis Institutes For Biomedical Research
Macrocyclic peptidomimetic inhibitors of beta-secretase (BACE): first X-ray structure of a macrocyclic peptidomimetic-BACE complex.
Bioorg Med Chem Lett 16: 191-5 (2006)
Eli Lilly
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
Curr Drug Metab 6: 413-54 (2005)
F. Hoffmann-La Roche
Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitors.
Bioorg Med Chem Lett 16: 40-3 (2005)
Novartis Institute For Tropical Diseases
Development and evaluation of a pharmacophore model for inhibitors of aldosterone synthase (CYP11B2).
Bioorg Med Chem Lett 16: 25-30 (2006)
Saarland University
Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile.
Bioorg Med Chem Lett 16: 354-7 (2005)
F. Hoffmann-La Roche
1-[4-(1H-Benzoimidazol-2-yl)-phenyl]-3-[4-(1H-benzoimidazol-2-yl)-phenyl]-urea derivatives as small molecule heparanase inhibitors.
Bioorg Med Chem Lett 16: 409-12 (2005)
Imclone Systems
Biphenyl-4-ylcarbamoyl thiophene carboxylic acids as potent DHODH inhibitors.
Bioorg Med Chem Lett 16: 267-70 (2006)
4Sc
Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors.
Bioorg Med Chem Lett 16: 349-53 (2005)
F. Hoffmann-La Roche
Pentacyclic triterpenes. Part 2: Synthesis and biological evaluation of maslinic acid derivatives as glycogen phosphorylase inhibitors.
Bioorg Med Chem Lett 16: 722-6 (2005)
China Pharmaceutical University
Hexylitaconic acid: a new inhibitor of p53-HDM2 interaction isolated from a marine-derived fungus, Arthrinium sp.
Bioorg Med Chem Lett 16: 69-71 (2006)
Kanazawa University
Peptide inhibitors of Dengue virus NS3 protease. Part 1: Warhead.
Bioorg Med Chem Lett 16: 36-9 (2005)
Novartis Institute For Tropical Diseases
Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.
Bioorg Med Chem Lett 16: 395-9 (2005)
The Schering Plough Research Institute
N-(4-{[4-(1H-Benzoimidazol-2-yl)-arylamino]-methyl}-phenyl)-benzamide derivatives as small molecule heparanase inhibitors.
Bioorg Med Chem Lett 16: 404-8 (2005)
Imclone Systems
Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I).
Bioorg Med Chem Lett 16: 225-7 (2005)
Fudan University
M2 and M3 muscarinic receptor activation of urinary bladder contractile signal transduction. I. Normal rat bladder.
J Pharmacol Exp Ther 316: 869-74 (2006)
Temple University
A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression.
Chem Biol 12: 1103-15 (2005)
Gpc Biotech
Thioureido N-acetyllactosamine derivatives as potent galectin-7 and 9N inhibitors.
Bioorg Med Chem 14: 1215-20 (2006)
Lund University
N-Hydroxyurea as zinc binding group in matrix metalloproteinase inhibition: mode of binding in a complex with MMP-8.
Bioorg Med Chem Lett 16: 20-4 (2005)
Università
Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors.
Bioorg Med Chem Lett 16: 421-6 (2006)
Abbott Laboratories
Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative.
Bioorg Med Chem Lett 16: 55-8 (2005)
Fujisawa Pharmaceutical
Synthesis and biological activity of novel 4-phenyl-1,8-naphthyridin-2(1H)-on-3-yl ureas: potent acyl-CoA:cholesterol acyltransferase inhibitor with improved aqueous solubility.
Bioorg Med Chem Lett 16: 44-8 (2005)
Sumitomo Pharmaceuticals
p38 MAP kinase inhibitors: metabolically stabilized piperidine-substituted quinolinones and naphthyridinones.
Bioorg Med Chem Lett 16: 64-8 (2005)
Merck
Diastereomeric molecular recognition and binding behavior of bile acids by L/D-tryptophan-modified beta-cyclodextrins.
J Org Chem 70: 8703-11 (2005)
Nankai University
4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists.
Bioorg Med Chem Lett 16: 146-9 (2005)
Johnson And Johnson Pharmaceutical Research And Development
N-Sulfonyl hydroxamate derivatives as inhibitors of class II fructose-1,6-diphosphate aldolase.
Bioorg Med Chem Lett 15: 5375-7 (2005)
Université
3-Substituted indolizine-1-carbonitrile derivatives as phosphatase inhibitors.
Bioorg Med Chem Lett 16: 59-63 (2005)
Technische UniversitäT MüNchen
NBD-labeled derivatives of the immunomodulatory drug FTY720 as tools for metabolism and mode of action studies.
Bioorg Med Chem Lett 16: 84-7 (2006)
Novartis Institutes For Biomedical Research
Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK.
Bioorg Med Chem Lett 16: 108-12 (2005)
Novartis Institutes For Biomedical Research
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 16: 123-8 (2006)
Johnson & Johnson Pharmaceutical
Optimization of CCR4 antagonists: side-chain exploration.
Bioorg Med Chem Lett 16: 204-7 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Toll-like receptor 2 antagonists. Part 1: preliminary SAR investigation of novel synthetic phospholipids.
Bioorg Med Chem Lett 15: 5494-8 (2005)
Eisai Research Institute
Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[aryl or heteroaryl]phenyltropanes.
Bioorg Med Chem Lett 16: 217-20 (2005)
Yale University
The first de novo designed inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.
Bioorg Med Chem Lett 16: 88-92 (2006)
University Of Leeds
Donepezil-tacrine hybrid related derivatives as new dual binding site inhibitors of AChE.
Bioorg Med Chem 13: 6588-97 (2005)
Neuropharma
Molecular docking and 3D-QSAR on 2-(oxalylamino) benzoic acid and its analogues as protein tyrosine phosphatase 1B inhibitors.
Bioorg Med Chem Lett 15: 5521-5 (2005)
Graduate University Of Chinese Academy Of Sciences
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.
J Med Chem 48: 6713-30 (2005)
Pfizer
Investigation of the binding determinants of phosphopeptides targeted to the SRC homology 2 domain of the signal transducer and activator of transcription 3. Development of a high-affinity peptide inhibitor.
J Med Chem 48: 6661-70 (2005)
The University Of Texas At Houston
Improving the antiviral efficacy and selectivity of HIV-1 reverse transcriptase inhibitor TSAO-T by the introduction of functional groups at the N-3 position.
J Med Chem 48: 6653-60 (2005)
Instituto De QuíMica MéDica (Csic)
Discovery of iodinated somatostatin analogues selective for hsst2 and hsst5 with excellent inhibition of growth hormone and prolactin release from rat pituitary cells.
J Med Chem 48: 6643-52 (2005)
University Of California San Diego
Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.
J Med Chem 48: 6632-42 (2005)
Saarland University
Angiotensin II pseudopeptides containing 1,3,5-trisubstituted benzene scaffolds with high AT2 receptor affinity.
J Med Chem 48: 6620-31 (2005)
Uppsala University
Hydroxyethylene sulfones as a new scaffold to address aspartic proteases: design, synthesis, and structural characterization.
J Med Chem 48: 6607-19 (2005)
Philipps-Universitat Marburg
Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists.
J Med Chem 48: 6597-606 (2005)
Astellas Pharma
Receptor flexibility in de novo ligand design and docking.
J Med Chem 48: 6585-96 (2005)
De Novo Pharmaceuticals
Selective inhibition of MCF-7(piGST) breast tumors using glutathione transferase-derived 2-methylene-cycloalkenones.
J Med Chem 48: 6549-52 (2005)
University Of Maryland
Structure-based design and discovery of protein tyrosine phosphatase inhibitors incorporating novel isothiazolidinone heterocyclic phosphotyrosine mimetics.
J Med Chem 48: 6544-8 (2005)
Incyte
Designed multiple ligands. An emerging drug discovery paradigm.
J Med Chem 48: 6523-43 (2005)
Organon Laboratories
Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs.
Bioorg Med Chem Lett 15: 5567-73 (2005)
Abbott
Metalloform-selective inhibition: synthesis and structure-activity analysis of Mn(II)-form-selective inhibitors of Escherichia coli methionine aminopeptidase.
Bioorg Med Chem Lett 15: 5386-91 (2005)
Graduate School Of Chinese Academy Of Sciences
Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
Bioorg Med Chem Lett 15: 5562-6 (2005)
Pfizer
Novel inhibitors of the mitochondrial respiratory chain: oximes and pyrrolines isolated from Penicillium brevicompactum and synthetic analogues.
J Agric Food Chem 53: 8296-301 (2005)
Universidad Polit£Cnica De Valencia
Novel triazole based inhibitors of Ras farnesyl transferase.
Bioorg Med Chem Lett 15: 5407-11 (2005)
Janssen Research Foundation
Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists.
Bioorg Med Chem Lett 15: 5478-82 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1beta converting enzyme inhibitors.
Bioorg Med Chem Lett 15: 5434-8 (2005)
Procter & Gamble Pharmaceuticals
3-Arylpiperazinylethyl-1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione derivatives as novel, high-affinity and selective alpha(1)-adrenoceptor ligands.
Bioorg Med Chem Lett 16: 150-3 (2005)
Università
Biological evaluation of 1-alkyl-3-phenylthioureas as orally active HDL-elevating agents.
Bioorg Med Chem Lett 16: 113-7 (2005)
Novartis Institutes For Biomedical Research
Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases.
Bioorg Med Chem Lett 16: 129-33 (2005)
Korea Research Institute Of Chemical Technology
Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.
Bioorg Med Chem Lett 16: 96-9 (2005)
Abbott Laboratories
New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists.
Bioorg Med Chem Lett 16: 167-70 (2005)
Università
Synthesis and biological evaluation of novel heterocyclic quinones as inhibitors of the dual specificity protein phosphatase CDC25C.
Bioorg Med Chem Lett 16: 171-5 (2005)
Institut Henri Beaufour
Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor.
Bioorg Med Chem Lett 15: 5365-9 (2005)
University Of WüRzburg
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.
Bioorg Med Chem Lett 16: 118-22 (2005)
Abbott Bioresearch Center
Pulvinones as bacterial cell wall biosynthesis inhibitors.
Bioorg Med Chem Lett 16: 176-80 (2006)
Wyeth Research
Synthesis and biological evaluation of novel EG5 inhibitors.
Chembiochem 6: 2005-13 (2005)
University Of Leipzig
Synthesis and preliminary evaluation of [3H]PSB-0413, a selective antagonist radioligand for platelet P2Y12 receptors.
Bioorg Med Chem Lett 15: 5450-2 (2005)
University Of Bonn
Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonists.
Bioorg Med Chem Lett 16: 200-3 (2005)
Pharmacopeia Drug Discovery
N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands.
Bioorg Med Chem Lett 15: 5419-23 (2005)
National Institute On Drug Abuse-Intramural Research Program
Conformationally restricted analogs of Combretastatin A-4 derived from SU5416.
Bioorg Med Chem Lett 15: 5382-5 (2005)
The Ohio State University
New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studies.
Bioorg Med Chem Lett 16: 138-41 (2005)
Institute Of Biomolecular Chemistry
3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone.
Bioorg Med Chem Lett 15: 5197-201 (2005)
Vernalis (R&D)
Structural basis for the GSK-3beta binding affinity and selectivity against CDK-2 of 1-(4-aminofurazan-3yl)-5-dialkylaminomethyl-1H-[1,2,3] triazole-4-carboxylic acid derivatives.
Bioorg Med Chem Lett 15: 5129-35 (2005)
Universidade Do Porto
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.
Bioorg Med Chem Lett 15: 5453-8 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues.
Bioorg Med Chem Lett 16: 196-9 (2005)
Universit£
Geometric diversity through permutation of backbone configuration in cyclic peptide libraries.
Bioorg Med Chem Lett 15: 5329-34 (2005)
Harvard Medical School
Synthesis and structure-activity relationships of novel benzene sulfonamides with potent binding affinity for bovine carbonic anhydrase II.
Bioorg Med Chem Lett 15: 5429-33 (2005)
Griffith University
Inhibitors designed for the active site of dihydroorotase.
Bioorg Chem 33: 470-83 (2005)
Texas A&M University
Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors.
Bioorg Med Chem Lett 15: 5344-52 (2005)
F. Hoffmann-La Roche
Tyrosinase inhibition: conformational analysis based studies on molecular dynamics calculations of bipiperidine based inhibitors.
J Enzyme Inhib Med Chem 20: 401-7 (2005)
University Of Karachi
6-(N-benzoylamino)purine as a novel and potent inhibitor of xanthine oxidase: inhibition mechanism and molecular modeling studies.
J Enzyme Inhib Med Chem 20: 317-24 (2005)
National Institute Of Pharmaceutical Education And Research
The structure of Cryptococcus neoformans thymidylate synthase suggests strategies for using target dynamics for species-specific inhibition.
Acta Crystallogr D Biol Crystallogr 61: 1320-34 (2005)
University Of California San Francisco
Differential effects of the phosphodiesterase type 5 inhibitors sildenafil, vardenafil, and tadalafil in rat aorta.
J Pharmacol Exp Ther 316: 654-61 (2006)
Medical College Of Georgia
Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus.
Bioorg Med Chem Lett 15: 5311-4 (2005)
Merck Research Laboratories
Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides.
Bioorg Med Chem Lett 15: 5192-6 (2005)
Universit£
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
Bioorg Med Chem Lett 15: 5499-503 (2005)
Abbott Laboratories
Potent and highly selective kappa opioid receptor agonists incorporating chroman- and 2,3-dihydrobenzofuran-based constraints.
Bioorg Med Chem Lett 15: 5114-9 (2005)
Adolor
New heterocyclic analogues of 4-(2-chloro-5-methoxyanilino)quinazolines as potent and selective c-Src kinase inhibitors.
Bioorg Med Chem Lett 15: 5446-9 (2005)
Astrazeneca
Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.
Bioorg Med Chem Lett 15: 5124-8 (2005)
Merck Research Laboratories
Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.
Bioorg Med Chem Lett 15: 5293-7 (2005)
Abbott Laboratories
Preparation of human Melanocortin-4 receptor agonist libraries: linear peptides X-Y-DPhe7-Arg8-Trp(or 2-Nal)9-Z-NH2.
Bioorg Med Chem Lett 15: 5504-8 (2005)
Roche Research Center
Surfing the piperazine core of tricyclic farnesyltransferase inhibitors.
Bioorg Med Chem Lett 15: 5537-43 (2005)
Pharmacopeia
Structure-based discovery of a new class of Hsp90 inhibitors.
Bioorg Med Chem Lett 15: 5187-91 (2005)
Vernalis (R&D)
Cyclohexyl-linked tricyclic isoxazoles are potent and selective modulators of the multidrug resistance protein (MRP1).
Bioorg Med Chem Lett 15: 5526-30 (2005)
Eli Lilly
Synthesis and monoamine transporter affinity of 3-aryl substituted trop-2-enes.
Bioorg Med Chem Lett 15: 5488-93 (2005)
University Of Illinois At Chicago
Sulfonamide chalcone as a new class of alpha-glucosidase inhibitors.
Bioorg Med Chem Lett 15: 5514-6 (2005)
Gyeongsang National University
Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists.
Bioorg Med Chem Lett 15: 5234-6 (2005)
Schering-Plough Research Institute
Transforming bivalent ligands into retractable enzyme inhibitors through polypeptide-protein interactions.
Bioorg Med Chem Lett 15: 5120-3 (2005)
National Research Council Of Canada
Novel 7-methoxy-6-oxazol-5-yl-2,3-dihydro-1H-quinazolin-4-ones as IMPDH inhibitors.
Bioorg Med Chem Lett 15: 5335-9 (2005)
Ucb Pharma
Isolation, catalytic properties, and competitive inhibitors of the zinc-dependent murine glutaminyl cyclase.
Biochemistry 44: 13415-24 (2005)
Probiodrug
Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors.
Bioorg Med Chem Lett 15: 5467-73 (2005)
Genomics Institute Of The Novartis Research Foundation
Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 1: 4'-substituted triclosan derivatives.
Bioorg Med Chem Lett 15: 5247-52 (2005)
Jacobus Pharmaceutical
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Bioorg Med Chem Lett 15: 5160-4 (2005)
Novartis Institutes For Biomedical Research
Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases.
Bioorg Med Chem Lett 15: 5474-7 (2005)
Imclone Systems
Heteroaryl-O-glucosides as novel sodium glucose co-transporter 2 inhibitors. Part 1.
Bioorg Med Chem Lett 15: 5202-6 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and pharmacological evaluation of 1H-imidazoles as ligands for the estrogen receptor and cytotoxic inhibitors of the cyclooxygenase.
J Med Chem 48: 6516-21 (2005)
Free University Of Berlin
Design, synthesis, and preliminary pharmacological evaluation of a set of small molecules that directly activate gi proteins.
J Med Chem 48: 6491-503 (2005)
Universit£
Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency.
J Med Chem 48: 6482-90 (2005)
Abbott Laboratories
Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28.
J Med Chem 48: 6461-71 (2005)
Vrije Universiteit
Synthesis of leukotriene B4 antagonists labeled with In-111 or Tc-99m to image infectious and inflammatory foci.
J Med Chem 48: 6442-53 (2005)
Bristol-Myers Squibb Medical Imaging
Adenosine kinase inhibitors. 5. Synthesis, enzyme inhibition, and analgesic activity of diaryl-erythro-furanosyltubercidin analogues.
J Med Chem 48: 6430-41 (2005)
Metabasis Therapeutics
High affinity electrophilic and photoactivatable covalent endocannabinoid probes for the CB1 receptor.
J Med Chem 48: 6423-9 (2005)
Northeastern University
Synthesis and antiinflammatory activity of coumarin derivatives.
J Med Chem 48: 6400-8 (2005)
Aristotle University Of Thessaloniki
Potent cannabinergic indole analogues as radioiodinatable brain imaging agents for the CB1 cannabinoid receptor.
J Med Chem 48: 6386-92 (2005)
Northeastern University
Structure-activity relationships of new A,D-ring modified steroids as aromatase inhibitors: design, synthesis, and biological activity evaluation.
J Med Chem 48: 6379-85 (2005)
University Of Oporto
Alkyl-substituted polyaminohydroxamic acids: a novel class of targeted histone deacetylase inhibitors.
J Med Chem 48: 6350-65 (2005)
Wayne State University
Design, synthesis, and activity of analogues of phosphinothricin as inhibitors of glutamine synthetase.
J Med Chem 48: 6340-9 (2005)
Wroclaw University Of Technology
A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
J Med Chem 48: 6326-39 (2005)
Pfizer
Synthesis, binding affinity at glutamic acid receptors, neuroprotective effects, and molecular modeling investigation of novel dihydroisoxazole amino acids.
J Med Chem 48: 6315-25 (2005)
Università
Simple but highly effective three-dimensional chemical-feature-based pharmacophore model for diketo acid derivatives as hepatitis C virus RNA-dependent RNA polymerase inhibitors.
J Med Chem 48: 6304-14 (2005)
Sapienza University Of Rome
5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.
J Med Chem 48: 6261-70 (2005)
Bristol-Myers Squibb
Design, synthesis, and biological activity of m-tyrosine-based 16- and 17-membered macrocyclic inhibitors of hepatitis C virus NS3 serine protease.
J Med Chem 48: 6229-35 (2005)
Schering-Plough Research Institute
Design and synthesis of specific probes for human 5-HT4 receptor dimerization studies.
J Med Chem 48: 6220-8 (2005)
Université
Ligand recognition by RAR and RXR receptors: binding and selectivity.
J Med Chem 48: 6212-9 (2005)
Universidad De Santiago De Compostela
Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.
J Med Chem 48: 6194-201 (2005)
Cnrs Umr-8113
Acyl ureas as human liver glycogen phosphorylase inhibitors for the treatment of type 2 diabetes.
J Med Chem 48: 6178-93 (2005)
Sanofi-Aventis Deutschland
Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2.
J Med Chem 48: 6174-7 (2005)
Oxagen
Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.
J Med Chem 48: 6169-73 (2005)
Merck Research Laboratories
Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.
Bioorg Med Chem Lett 15: 5176-81 (2005)
Santhera Pharmaceuticals
Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome.
Bioorg Med Chem Lett 15: 5266-9 (2005)
Merck
Rapamycin analogs with reduced systemic exposure.
Bioorg Med Chem Lett 15: 5340-3 (2005)
Abbott Laboratories
Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors.
Bioorg Med Chem Lett 15: 5298-302 (2005)
Virginia Commonwealth University
Inhibitors of the serotonin transporter protein (SERT): the design and synthesis of biotinylated derivatives of 3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1H-indoles. High-affinity serotonergic ligands for conjugation with quantum dots.
Bioorg Med Chem Lett 15: 5307-10 (2005)
Vanderbilt University
A new antitumor compound from the plant Oryctanthus sp. as a VEGF receptor binding inhibitor.
Bioorg Med Chem Lett 15: 4907-9 (2005)
Schering-Plough Research Institute
Structure-activity relationship studies on a series of cyclohexylpiperazines bearing a phanylacetamide as ligands of the human melanocortin-4 receptor.
Bioorg Med Chem Lett 15: 5237-40 (2005)
Neurocrine Biosciences
Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1.
Bioorg Med Chem Lett 15: 4979-84 (2005)
Gnf
Synthesis of desthio prenylcysteine analogs: sulfur is important for biological activity.
Bioorg Med Chem Lett 15: 5080-3 (2005)
Purdue University
Synthesis and HIV-1 integrase inhibitory activities of caffeic acid dimers derived from Salvia officinalis.
Bioorg Med Chem Lett 15: 5053-6 (2005)
Université
3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists.
Bioorg Med Chem Lett 15: 5061-4 (2005)
Merck Research Laboratories
Nonsteroidal anti-inflammatory drugs and their analogues as inhibitors of aldo-keto reductase AKR1C3: new lead compounds for the development of anticancer agents.
Bioorg Med Chem Lett 15: 5170-5 (2005)
University Of Ljubljana
New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.
Bioorg Med Chem Lett 15: 5517-20 (2005)
Kobe Gakuin University
Structure-based discovery of a boronic acid bioisostere of combretastatin A-4.
Chem Biol 12: 1007-14 (2005)
University Of Virginia
Methylxanthine drugs are chitinase inhibitors: investigation of inhibition and binding modes.
Chem Biol 12: 973-80 (2005)
University Of Dundee
Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents.
J Nat Prod 68: 1437-40 (2005)
Merck Research Laboratories
Design, synthesis, and evaluation of octahydropyranopyrrole-based inhibitors of mammalian ribonucleotide reductase.
Bioorg Med Chem Lett 15: 5146-9 (2005)
University Of Pennsylvania
An experimental and molecular-modeling study of the binding of linked sulfated tetracyclitols to FGF-1 and FGF-2.
Chembiochem 6: 1882-90 (2005)
Progen Industries
3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation.
Bioorg Med Chem Lett 15: 4889-97 (2005)
Pfizer
Solid-phase binding assays of peptides using EGFP-Src SH2 domain fusion protein and biotinylated Src SH2 domain.
Bioorg Med Chem Lett 15: 4994-7 (2005)
University Of Rhode Island
Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.
Bioorg Med Chem Lett 15: 5319-23 (2005)
University Of Kansas
Two classes of p38alpha MAP kinase inhibitors having a common diphenylether core but exhibiting divergent binding modes.
Bioorg Med Chem Lett 15: 5274-9 (2005)
Locus Pharmaceuticals
Pentacyclic triterpenes. Part 1: the first examples of naturally occurring pentacyclic triterpenes as a new class of inhibitors of glycogen phosphorylases.
Bioorg Med Chem Lett 15: 4944-8 (2005)
China Pharmaceutical University
Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides.
Bioorg Med Chem Lett 15: 4910-4 (2005)
Roche Research Center
A lead compound for the development of ABA 8'-hydroxylase inhibitors.
Bioorg Med Chem Lett 15: 5226-9 (2005)
Gifu University
Privileged structure based ligands for melanocortin receptors--substituted benzylic piperazine derivatives.
Bioorg Med Chem Lett 15: 4973-8 (2005)
Eli Lilly
Design, synthesis, and enzymatic property of a sulfur-substituted analogue of trigalacturonic acid.
Bioorg Med Chem Lett 15: 4932-5 (2005)
Hirosaki University
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides.
Bioorg Med Chem Lett 15: 4862-6 (2005)
Università
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists.
Bioorg Med Chem Lett 15: 4989-93 (2005)
Glaxosmithkline
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.
Bioorg Med Chem Lett 15: 5241-6 (2005)
Merck Frosst Centre For Therapeutic Research
N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides: human dopamine D4 ligands with high affinity for the 5-HT2A receptor.
Bioorg Med Chem Lett 15: 5253-6 (2005)
Nps Pharmaceuticals
Phosphinate, sulfonate, and sulfonamidate dipeptides as potential inhibitors of Escherichia coli aminopeptidase N.
Bioorg Med Chem Lett 15: 5150-3 (2005)
Miami University
Topological model for the prediction of MRP1 inhibitory activity of pyrrolopyrimidines and templates derived from pyrrolopyrimidine.
Bioorg Med Chem Lett 15: 4967-72 (2005)
M.D. University
2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV.
Bioorg Med Chem Lett 15: 5257-61 (2005)
Glaxosmithkline
High affinity ligands for the alpha7 nicotinic receptor that show no cross-reactivity with the 5-HT3 receptor.
Bioorg Med Chem Lett 15: 4727-30 (2005)
Eli Lilly
Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT-2.
Bioorg Med Chem Lett 15: 4985-8 (2005)
Wyeth Research
Structure-based design of 7-carbamate analogs of geldanamycin.
Bioorg Med Chem Lett 15: 5016-21 (2005)
Kosan Biosciences
Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates.
Bioorg Med Chem Lett 15: 4656-61 (2005)
Sapienza University Of Rome
Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with benzo[b]thiophene 1,1-dioxide sulfonamides.
Bioorg Med Chem Lett 15: 4872-6 (2005)
Università
The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines.
Bioorg Med Chem Lett 15: 4915-8 (2005)
Wake Forest University Health Sciences
Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.
Bioorg Med Chem Lett 15: 5288-92 (2005)
Wyeth Research
Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.
J Med Chem 48: 6162-5 (2005)
National Institute Of Pharmaceutical Education And Research
Synthesis, anti-HIV activity, and metabolic stability of new alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors.
J Med Chem 48: 6140-55 (2005)
Purdue University
Bisphosphonate inhibition of the exopolyphosphatase activity of the Trypanosoma brucei soluble vacuolar pyrophosphatase.
J Med Chem 48: 6128-39 (2005)
University Of Illinois At Urbana-Champaign
Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations.
J Med Chem 48: 6090-106 (2005)
Uppsala University
Molecular modeling, synthesis, and preliminary biological evaluation of glutathione-S-transferase inhibitors as potential therapeutic agents.
J Med Chem 48: 6084-9 (2005)
Università
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.
J Med Chem 48: 6066-83 (2005)
Abbott Laboratories
Rational design, synthesis, and characterization of novel inhibitors for human beta1,4-galactosyltransferase.
J Med Chem 48: 6054-65 (2005)
Hokkaido University
Conformationally restricted homotryptamines. 2. Indole cyclopropylmethylamines as selective serotonin reuptake inhibitors.
J Med Chem 48: 6023-34 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
A new pyridazine series of GABAA alpha5 ligands.
J Med Chem 48: 6004-11 (2005)
Merck Sharp & Dohme Research Laboratories
Differential response of estrogen receptor subtypes to 1,3-diarylindene and 2,3-diarylindene ligands.
J Med Chem 48: 5989-6003 (2005)
University Of California
F-18 stilbenes as PET imaging agents for detecting beta-amyloid plaques in the brain.
J Med Chem 48: 5980-8 (2005)
University Of Pennsylvania
Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent.
J Med Chem 48: 5966-79 (2005)
Takeda Pharmaceutical
Deoxyuridine triphosphate nucleotidohydrolase as a potential antiparasitic drug target.
J Med Chem 48: 5942-54 (2005)
Cardiff University
Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine: the first CGRP antagonist
J Med Chem 48: 5921-31 (2005)
Boehringer Ingelheim Pharma
4-Anilino-7,8-dialkoxybenzo[g]quinoline-3-carbonitriles as potent Src kinase inhibitors.
J Med Chem 48: 5909-20 (2005)
Wyeth Research
Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor.
J Med Chem 48: 5900-8 (2005)
Bayer Healthcare
Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.
J Med Chem 48: 5888-91 (2005)
Abbott Laboratories
Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents.
J Med Chem 48: 5884-7 (2005)
Schering-Plough Research Institute
Complexation of ferrocene derivatives by the cucurbit[7]uril host: a comparative study of the cucurbituril and cyclodextrin host families.
J Am Chem Soc 127: 12984-9 (2005)
University Of Miami
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
Bioorg Med Chem Lett 15: 4741-4 (2005)
Merck Frosst Centre For Therapeutic Research
Bis(indole) alkaloids as sortase A inhibitors from the sponge Spongosorites sp.
Bioorg Med Chem Lett 15: 4927-31 (2005)
Seoul National University
Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides.
Bioorg Med Chem Lett 15: 5012-5 (2005)
Astrazeneca
Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
Bioorg Med Chem Lett 15: 5035-8 (2005)
Merck Research Laboratories
Activity and QSAR study of baogongteng A and its derivatives as muscarinic agonists.
Bioorg Med Chem Lett 15: 4814-8 (2005)
Shanghai Second Medical University
Identification of a potent and selective 5-HT1B receptor antagonist.
Bioorg Med Chem Lett 15: 4708-12 (2005)
Glaxosmithkline
(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators.
Bioorg Med Chem Lett 15: 5003-6 (2005)
Wyeth Research
Synthesis of 4-(5-[18F]fluoromethyl-3-phenylisoxazol-4-yl)benzenesulfonamide, a new [18F]fluorinated analogue of valdecoxib, as a potential radiotracer for imaging cyclooxygenase-2 with positron emission tomography.
Bioorg Med Chem Lett 15: 4699-702 (2005)
University Of California Los Angeles
An efficient synthesis of argifin: a natural product chitinase inhibitor with chemotherapeutic potential.
Bioorg Med Chem Lett 15: 4717-21 (2005)
University Of Dundee
Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.
Bioorg Med Chem Lett 15: 5022-6 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Pyrazolopyridinones as functionally selective GABAA ligands.
Bioorg Med Chem Lett 15: 4998-5002 (2005)
Merck Sharp & Dohme Research Laboratories
Synthesis and SAR of highly selective MMP-13 inhibitors.
Bioorg Med Chem Lett 15: 4961-6 (2005)
Wyeth Research
Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists.
Bioorg Med Chem Lett 15: 4809-13 (2005)
Biogen Idec
The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold.
Bioorg Med Chem Lett 15: 4666-70 (2005)
University College London
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
Bioorg Med Chem Lett 15: 4691-5 (2005)
Chungbuk National University
SAR, species specificity, and cellular activity of cyclopentene dicarboxylic acid amides as DHODH inhibitors.
Bioorg Med Chem Lett 15: 4854-7 (2005)
4Sc
Synthesis and biological evaluation of 1,3-diphenylprop-2-yn-1-ones as dual inhibitors of cyclooxygenases and lipoxygenases.
Bioorg Med Chem Lett 15: 4842-5 (2005)
University Of Alberta
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 7- and 5-, 6-, 8-positions.
Bioorg Med Chem Lett 15: 4745-51 (2005)
Maxim Pharmaceuticals
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
Bioorg Med Chem Lett 15: 4786-9 (2005)
Columbia University College Of Physicians And Surgeons
Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors.
Bioorg Med Chem Lett 15: 4713-6 (2005)
Pfizer
Novel indole alpha-methylene-gamma-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases.
Bioorg Med Chem Lett 15: 4799-802 (2005)
Chinese Academy Of Sciences
Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase.
Bioorg Med Chem Lett 15: 4685-90 (2005)
Universidad De Buenos Aires
Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase.
Bioorg Med Chem Lett 15: 4696-8 (2005)
Imclone Systems
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.
Bioorg Med Chem Lett 15: 4867-71 (2005)
Glaxosmithkline
Synthesis and evaluation of 3-anilino-quinoxalinones as glycogen phosphorylase inhibitors.
Bioorg Med Chem Lett 15: 4790-3 (2005)
Johnson & Johnson Pharmaceutical Research And Development
Diamino-C,N-diarylpyridine positional isomers as inhibitors of lysophosphatidic acid acyltransferase-beta.
Bioorg Med Chem Lett 15: 4703-7 (2005)
Cell Therapeutics
The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases.
Bioorg Med Chem Lett 16: 2337-40 (2006)
Pfizer
Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3.
Bioorg Med Chem Lett 15: 5095-9 (2005)
Astrazeneca R&D SöDertäLje
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 1.
Bioorg Med Chem Lett 15: 4833-7 (2005)
Université
Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity.
Bioorg Med Chem Lett 15: 4794-8 (2005)
Solvay Pharma
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 2.
Bioorg Med Chem Lett 15: 4828-32 (2005)
Université
Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents.
Bioorg Med Chem Lett 15: 4819-23 (2005)
University Of Erlangen-Nuremberg
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.
Bioorg Med Chem Lett 15: 4411-6 (2005)
Merck Research Laboratories
Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.
Bioorg Med Chem Lett 15: 4421-6 (2005)
Cnrs Umr 6052
Design and synthesis of phthalimide-type histone deacetylase inhibitors.
Bioorg Med Chem Lett 15: 4427-31 (2005)
The University Of Tokyo Yayoi
1-Aryl-3,4-dihydro-1H-quinolin-2-one derivatives, novel and selective norepinephrine reuptake inhibitors.
Bioorg Med Chem Lett 15: 4432-7 (2005)
Eli Lilly
Docking studies on monoamine oxidase-B inhibitors: estimation of inhibition constants (K(i)) of a series of experimentally tested compounds.
Bioorg Med Chem Lett 15: 4438-46 (2005)
Kadir Has University
4-Phenylcoumarins as HIV transcription inhibitors.
Bioorg Med Chem Lett 15: 4447-50 (2005)
Instituto De Salud Carlos Iii
A chemical strategy to promote helical peptide-protein interactions involved in apoptosis.
Bioorg Med Chem Lett 15: 4467-9 (2005)
University Of Illinois At Urbana-Champaign
Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist.
J Pharmacol Exp Ther 315: 1278-87 (2005)
Acadia Pharmaceuticals
Discovery of potent, nonsystemic apical sodium-codependent bile acid transporter inhibitors (Part 2).
J Med Chem 48: 5853-68 (2005)
Pfizer
Discovery of potent, nonsystemic apical sodium-codependent bile acid transporter inhibitors (Part 1).
J Med Chem 48: 5837-52 (2005)
Pharmacia
Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents.
J Med Chem 48: 5823-36 (2005)
Seoul National University
Synthesis and structure-activity relationship of a novel series of aminoalkylindoles with potential for imaging the neuronal cannabinoid receptor by positron emission tomography.
J Med Chem 48: 5813-22 (2005)
National Institute On Drug Abuse
Modifications to the tetracaine scaffold produce cyclic nucleotide-gated channel blockers with widely varying efficacies.
J Med Chem 48: 5805-12 (2005)
Oregon Health And Science University
4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases.
J Med Chem 48: 5794-804 (2005)
Pharmacia
Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.
J Med Chem 48: 5780-93 (2005)
Neurocrine Biosciences
Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists.
J Med Chem 48: 5771-9 (2005)
Friedrich-Alexander University
E-ring modified steroids as novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.
J Med Chem 48: 5749-70 (2005)
University Of Bath
Conformationally constrained analogues of diacylglycerol (DAG). 25. Exploration of the sn-1 and sn-2 carbonyl functionality reveals the essential role of the sn-1 carbonyl at the lipid interface in the binding of DAG-lactones to protein kinase C.
J Med Chem 48: 5738-48 (2005)
National Cancer Institute-Frederick
Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase.
J Med Chem 48: 5728-37 (2005)
Pfizer
Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II.
J Med Chem 48: 5721-7 (2005)
Istituto Di Biostrutture E Bioimmagini-Cnr
Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.
J Med Chem 48: 5705-20 (2005)
Chiesi Farmaceutici
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode.
J Med Chem 48: 5684-97 (2005)
7Tm Pharma
Impact of induced fit on ligand binding to the androgen receptor: a multidimensional QSAR study to predict endocrine-disrupting effects of environmental chemicals.
J Med Chem 48: 5666-74 (2005)
University Of Basel
Factorizing selectivity determinants of inhibitor binding toward aldose and aldehyde reductases: structural and thermodynamic properties of the aldose reductase mutant Leu300Pro-fidarestat complex.
J Med Chem 48: 5659-65 (2005)
Institute Of Genetics And Molecular And Cellular Biology (Igbmc)
4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.
J Med Chem 48: 5644-7 (2005)
Gsk
Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
J Med Chem 48: 5639-43 (2005)
Bristol-Myers Squibb
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.
J Med Chem 48: 5613-38 (2005)
The Scripps Research Institute
Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists.
Bioorg Med Chem Lett 15: 4780-5 (2005)
Wyeth Research
Lead optimization of 7-benzyloxy 2-(4'-pyridylmethyl)thio isoflavone aromatase inhibitors.
Bioorg Med Chem 13: 6571-7 (2005)
Ohio State University
The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex.
Bioorg Med Chem Lett 15: 4752-6 (2005)
Pfizer
Design, synthesis, and structure-activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosis.
Bioorg Med Chem Lett 15: 4574-8 (2005)
Merck Research Laboratories
Inhibition of Src kinase activity by 7-[(2,4-dichloro-5-methoxyphenyl)amino]-2-heteroaryl-thieno[3,2-b]pyridine-6-carbonitriles.
Bioorg Med Chem Lett 15: 4681-4 (2005)
Wyeth Research
Phaeochromycins A-E, anti-inflammatory polyketides isolated from the soil actinomycete Streptomyces phaeochromogenes LL-P018.
J Nat Prod 68: 1262-5 (2005)
Wyeth Research
Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources.
J Nat Prod 68: 1247-52 (2005)
Merck Research Laboratories
Sesterterpenoids, terretonins A-D, and an alkaloid, asterrelenin, from Aspergillus terreus.
J Nat Prod 68: 1243-6 (2005)
The Chinese Academy Of Sciences
Iminosugar-producing Thai medicinal plants.
J Nat Prod 68: 1238-42 (2005)
Hokuriku University
A fragment-based approach to understanding inhibition of 1-deoxy-D-xylulose-5-phosphate reductoisomerase.
Chembiochem 6: 1866-74 (2005)
University Of Bristol
Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies.
Bioorg Med Chem Lett 15: 4417-20 (2005)
Schering-Plough Research Institute
New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 15: 4770-3 (2005)
Pfizer
Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Bioorg Med Chem Lett 15: 4589-93 (2005)
Merck Research Laboratories
Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands.
Bioorg Med Chem Lett 15: 4463-6 (2005)
University Of Kentucky
Hepatitis C virus NS3-4A serine protease inhibitors: use of a P2-P1 cyclopropyl alanine combination for improved potency.
Bioorg Med Chem Lett 15: 4515-9 (2005)
Schering-Plough Research Institute
Privileged structure-based ligands for melanocortin receptors-tetrahydroquinolines, indoles, and aminotetralines.
Bioorg Med Chem Lett 15: 4459-62 (2005)
Eli Lilly
Synthesis and biological activity of macrocyclic inhibitors of hepatitis C virus (HCV) NS3 protease.
Bioorg Med Chem Lett 15: 4475-8 (2005)
Schering-Plough Research Institute
Aza-bicyclic amino acid carboxamides as alpha4beta1/alpha4beta7 integrin receptor antagonists.
Bioorg Med Chem 13: 6693-702 (2005)
Johnson & Johnson Pharmaceutical
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand.
Bioorg Med Chem Lett 15: 4761-9 (2005)
Boehringer Ingelheim Pharmaceuticals
New dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Bioorg Med Chem Lett 15: 4774-9 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH.
J Med Chem 48: 5608-11 (2005)
University Of Cagliari
Novel 2,3-dihydrobenzofuran-2-carboxylic acids: highly potent and subtype-selective PPARalpha agonists with potent hypolipidemic activity.
J Med Chem 48: 5589-99 (2005)
Merck Research Laboratories
Novel 8-substituted dipyridodiazepinone inhibitors with a broad-spectrum of activity against HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors.
J Med Chem 48: 5580-8 (2005)
Boehringer Ingelheim (Canada)
Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter.
J Med Chem 48: 5551-60 (2005)
University Of Kentucky
Inhibition of carboxylesterases by benzil (diphenylethane-1,2-dione) and heterocyclic analogues is dependent upon the aromaticity of the ring and the flexibility of the dione moiety.
J Med Chem 48: 5543-50 (2005)
St. Jude Children'S Research Hospital
Structure of aldehyde reductase holoenzyme in complex with the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity.
J Med Chem 48: 5536-42 (2005)
Monash University (Parkville Campus)
Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
J Med Chem 48: 5530-5 (2005)
The Ohio State University
Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.
J Med Chem 48: 5509-19 (2005)
Università
New 5-hydroxytryptamine(1A) receptor ligands containing a norbornene nucleus: synthesis and in vitro pharmacological evaluation.
J Med Chem 48: 5495-503 (2005)
Università
Development of a three-dimensional model for the N-methyl-D-aspartate NR2A subunit.
J Med Chem 48: 5489-94 (2005)
Universit£
A combination of docking, QM/MM methods, and MD simulation for binding affinity estimation of metalloprotein ligands.
J Med Chem 48: 5437-47 (2005)
North Dakota State University
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
J Med Chem 48: 5419-22 (2005)
Glaxosmithkline
Indolin-2-ones with high in vivo efficacy in a model for multiple sclerosis.
J Med Chem 48: 5412-4 (2005)
Leo Pharma
A molecular target for suppression of the evolution of antibiotic resistance: inhibition of the Escherichia coli RecA protein by N(6)-(1-naphthyl)-ADP.
J Med Chem 48: 5408-11 (2005)
University Of North Carolina At Chapel Hill
Farnesoid X receptor: from structure to potential clinical applications.
J Med Chem 48: 5383-403 (2005)
Universit£
Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists.
Bioorg Med Chem Lett 15: 4564-9 (2005)
Merck Research Laboratories
A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells.
Bioorg Med Chem Lett 15: 4550-4 (2005)
Merck Research Laboratories
A new class of high affinity thyromimetics containing a phenyl-naphthylene core.
Bioorg Med Chem Lett 15: 4579-84 (2005)
Pharmaceutical Research Institute
Heteroaromatic side-chain analogs of pregabalin.
Bioorg Med Chem Lett 16: 2329-32 (2006)
Pgrd Michigan Laboratories
1,8-Naphthyridin-4-one derivatives as new ligands of A2A adenosine receptors.
Bioorg Med Chem Lett 15: 4604-10 (2005)
Dipartimento Di Scienze Farmaceutiche
4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors.
Bioorg Med Chem Lett 15: 4221-5 (2005)
Fujisawa Pharmaceutical
ERbeta ligands. Part 4: Synthesis and structure-activity relationships of a series of 2-phenylquinoline derivatives.
Bioorg Med Chem Lett 15: 4520-5 (2005)
Wyeth Research
Synthesis and antibacterial activity of a novel series of DNA gyrase inhibitors: 5-[(E)-2-arylvinyl]pyrazoles.
Bioorg Med Chem Lett 15: 4299-303 (2005)
Dainippon Pharmaceutical
Hydroxylated N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives as potent broad-spectrum anticoccidial agents.
Bioorg Med Chem Lett 15: 4570-3 (2005)
Merck Research Laboratories
8-Substituted 3,4-dihydroquinolinones as a novel scaffold for atypical antipsychotic activity.
Bioorg Med Chem Lett 15: 4560-3 (2005)
Pfizer
Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency.
Bioorg Med Chem Lett 15: 4180-4 (2005)
Schering-Plough Research Institute
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.
Bioorg Med Chem Lett 15: 4239-42 (2005)
Activx Biosciences
Novel, selective indole-based ECE inhibitors: lead optimization via solid-phase and classical synthesis.
Bioorg Med Chem Lett 15: 4201-5 (2005)
Bayer Healthcare
Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.
Bioorg Med Chem Lett 15: 4174-9 (2005)
Abbott Laboratories
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors.
Bioorg Med Chem Lett 15: 4256-60 (2005)
Activx Biosciences
Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates.
Bioorg Med Chem Lett 15: 4345-9 (2005)
Wyeth Research
Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer.
J Med Chem 48: 5373-7 (2005)
Novartis Institutes For Biomedical Research
Design and synthesis of 4-(alpha-hydroxymalonyl)phenylalanine as a new phosphotyrosyl mimetic and its use in growth factor receptor bound 2 src-homology 2 (Grb2 SH2) domain-binding peptides.
J Med Chem 48: 5369-72 (2005)
National Cancer Institute-Frederick
High-affinity epidermal growth factor receptor (EGFR) irreversible inhibitors with diminished chemical reactivities as positron emission tomography (PET)-imaging agent candidates of EGFR overexpressing tumors.
J Med Chem 48: 5337-48 (2005)
Hadassah Hebrew University
Synthesis of classical, four-carbon bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.
J Med Chem 48: 5329-36 (2005)
Duquesne University
Novel fluorinated prodrugs for activation by carboxypeptidase G2 showing good in vivo antitumor activity in gene-directed enzyme prodrug therapy.
J Med Chem 48: 5321-8 (2005)
Institute Of Cancer Research
Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.
J Med Chem 48: 5305-20 (2005)
Eli Lilly
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
J Med Chem 48: 5295-304 (2005)
Abbott Laboratories
Development of dual-acting benzofurans for thromboxane A2 receptor antagonist and prostacyclin receptor agonist: synthesis, structure-activity relationship, and evaluation of benzofuran derivatives.
J Med Chem 48: 5279-94 (2005)
Toray Industries
Androsterone 3alpha-ether-3beta-substituted and androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase: chemical synthesis and structure-activity relationship.
J Med Chem 48: 5257-68 (2005)
Chuq-Pavillon Chul And Universit£
A-ring-substituted estrogen-3-O-sulfamates: potent multitargeted anticancer agents.
J Med Chem 48: 5243-56 (2005)
University Of Bath
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
J Med Chem 48: 5232-42 (2005)
Wockhardt
2-Acetylamino-3-[4-(2-acetylamino-2-carboxyethylsulfanylcarbonylamino)- phenylcarbamoylsulfanyl]propionic acid and its derivatives as a novel class of glutathione reductase inhibitors.
J Med Chem 48: 5224-31 (2005)
South Dakota State University
Discovery and structure-activity relationship of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers and potential anticancer agents.
J Med Chem 48: 5215-23 (2005)
Maxim Pharmaceuticals
Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics.
J Med Chem 48: 5175-90 (2005)
Universite De Montreal At Succursale Centre-Ville
Novel, highly potent adenosine deaminase inhibitors containing the pyrazolo[3,4-d]pyrimidine ring system. Synthesis, structure-activity relationships, and molecular modeling studies.
J Med Chem 48: 5162-74 (2005)
Universit£
6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency.
J Med Chem 48: 5131-9 (2005)
University Of Virginia
Ligand selectivity for the acetylcholine binding site of the rat alpha4beta2 and alpha3beta4 nicotinic subtypes investigated by molecular docking.
J Med Chem 48: 5123-30 (2005)
Swiss Federal Institute Of Technology Zurich
Discovery of cell-permeable non-peptide inhibitors of beta-secretase by high-throughput docking and continuum electrostatics calculations.
J Med Chem 48: 5108-11 (2005)
University Of ZüRich
Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.
J Med Chem 48: 5104-7 (2005)
Neurocrine Biosciences
Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone.
J Med Chem 48: 5100-3 (2005)
Inotek Pharmaceuticals
A positron emission tomography radioligand for the in vivo labeling of metabotropic glutamate 1 receptor: (3-ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone.
J Med Chem 48: 5096-9 (2005)
Columbia University College Of Physicians And Surgeons
Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.
J Med Chem 48: 5092-5 (2005)
Women'S Health Research Institute
Design and synthesis of depeptidized macrocyclic inhibitors of hepatitis C NS3-4A protease using structure-based drug design.
J Med Chem 48: 5088-91 (2005)
Schering-Plough Research Institute
The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications.
J Med Chem 48: 5059-87 (2005)
Universit£
Characterization of a novel bivalent morphinan possessing kappa agonist and micro agonist/antagonist properties.
J Pharmacol Exp Ther 315: 821-7 (2005)
University Of Rochester
Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes.
Bioorg Med Chem Lett 15: 4286-90 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Bioorg Med Chem Lett 15: 4555-9 (2005)
Organix
5-Substituted 4-anilinoquinazolines as potent, selective and orally active inhibitors of erbB2 receptor tyrosine kinase.
Bioorg Med Chem Lett 15: 4226-9 (2005)
Astrazeneca
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.
Bioorg Med Chem Lett 15: 4230-4 (2005)
Carlsson Research
Cyclic sulfamide gamma-secretase inhibitors.
Bioorg Med Chem Lett 15: 4212-6 (2005)
Merck Sharp And Dohme Research Laboratories
Design and synthesis of a novel peptidomimetic inhibitor of HIV-1 Tat-TAR interactions: squaryldiamide as a new potential bioisostere of unsubstituted guanidine.
Bioorg Med Chem Lett 15: 4243-6 (2005)
University Of Massachusetts Medical School
Synthesis and antipicornavirus activity of (R)- and (S)-1-[5-(4'-chlorobiphenyl-4-yloxy)-3-methylpentyl]-3-pyridin-4-yl-imidazolidin-2-one.
Bioorg Med Chem Lett 15: 4206-11 (2005)
National Health Research Institutes
Characterization of isoprenaline- and salmeterol-stimulated interactions between beta2-adrenoceptors and beta-arrestin 2 using beta-galactosidase complementation in C2C12 cells.
J Pharmacol Exp Ther 315: 839-48 (2005)
Institute Of Cell Signaling
Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues.
Bioorg Med Chem Lett 15: 4169-73 (2005)
Harvard Medical School
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.
Proc Natl Acad Sci U S A 102: 11011-6 (2005)
Ambit
Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: inhibition of interleukin-1beta-converting enzyme.
Bioorg Med Chem Lett 15: 4322-6 (2005)
Procter & Gamble Pharmaceuticals
Discovery of novel conformationally restricted diazocan peptidomimetics as inhibitors of interleukin-1beta synthesis.
Bioorg Med Chem Lett 15: 4291-4 (2005)
Procter & Gamble Pharmaceuticals
Discovery and structure-activity relationships of novel sulfonamides as potent PTP1B inhibitors.
Bioorg Med Chem Lett 15: 4336-41 (2005)
Affymax
Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors.
Bioorg Med Chem Lett 15: 3992-5 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
J Pharmacol Exp Ther 315: 711-21 (2005)
F. Hoffmann-La Roche
Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists.
Bioorg Med Chem Lett 15: 4350-3 (2005)
Merck Research Laboratories
3-(2-Aminoethyl)pyridine analogs as alpha4beta2 nicotinic cholinergic receptor ligands.
Bioorg Med Chem Lett 15: 4308-12 (2005)
Virginia Commonwealth University
Carbonic anhydrase inhibitors: design of thioureido sulfonamides with potent isozyme II and XII inhibitory properties and intraocular pressure lowering activity in a rabbit model of glaucoma.
Bioorg Med Chem Lett 15: 3821-7 (2005)
Universita Degli Studi
8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands.
Bioorg Med Chem Lett 15: 4370-4 (2005)
Glaxosmithkline
Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors.
Bioorg Med Chem Lett 15: 4385-8 (2005)
Columbia University College Of Physicians And Surgeons
Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides.
Bioorg Med Chem Lett 15: 3828-33 (2005)
Kochi Medical School
Defining Cdk5 ligand chemical space with small molecule inhibitors of tau phosphorylation.
Chem Biol 12: 811-23 (2005)
Harvard Medical School
Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors.
Bioorg Med Chem Lett 15: 4037-42 (2005)
Nih
Influence of acid surrogates toward potency of VLA-4 antagonist.
Bioorg Med Chem Lett 15: 4053-6 (2005)
Merck Research Laboratories
Inhibition of mandelate racemase by the substrate-intermediate-product analogue 1,1-diphenyl-1-hydroxymethylphosphonate.
Bioorg Med Chem Lett 15: 4342-4 (2005)
Dalhousie University
Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)-5-{2-[3-(substituted)-1-azetidinyl]-ethyl}-2-piperidones. Part 2: Improving oral absorption.
Bioorg Med Chem Lett 15: 3957-61 (2005)
Pfizer
Structural revision of aspernigrin A, reisolated from Cladosporium herbarum IFB-E002.
J Nat Prod 68: 1106-8 (2005)
Nanjing University
Latifolians A and B, novel JNK3 kinase inhibitors from the Papua New Guinean plant Gnetum latifolium.
J Nat Prod 68: 1080-2 (2005)
Griffith University
Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674.
J Nat Prod 68: 1061-5 (2005)
Mitsubishi Pharma
Expanding the ChemGPS chemical space with natural products.
J Nat Prod 68: 985-91 (2005)
Uppsala University
Acylphloroglucinol derivatives from Mahurea palustris.
J Nat Prod 68: 979-84 (2005)
National Center For Scientific Research (Cnrs)-Pierre Fabre
Effect of a 6-cyano substituent in 14-oxygenated N-methylmorphinans on opioid receptor binding and antinociceptive potency.
J Med Chem 48: 5052-5 (2005)
University Of Innsbruck
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
J Med Chem 48: 5025-37 (2005)
Bristol-Myers Squibb Pharmaceutical Research Institute
New 2-arylpyrazolo[4,3-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists.
J Med Chem 48: 5001-8 (2005)
Università
Synthesis and radioligand binding studies of C-5- and C-8-substituted 1-(3,4-dimethoxybenzyl)-2,2-dimethyl-1,2,3,4-tetrahydroisoquinoliniums as SK channel blockers related to N-methyl-laudanosine and N-methyl-noscapine.
J Med Chem 48: 4972-82 (2005)
University Of Li£Ge
Discovery of novel trisubstituted asymmetric derivatives of (2S,4R,5R)-2-benzhydryl-5-benzylaminotetrahydropyran-4-ol, exhibiting high affinity for serotonin and norepinephrine transporters in a stereospecific manner.
J Med Chem 48: 4962-71 (2005)
Wayne State University
Synthesis and structure-activity relationships of a new series of retinoid-related biphenyl-4-ylacrylic acids endowed with antiproliferative and proapoptotic activity.
J Med Chem 48: 4931-46 (2005)
Università
Synthesis, structure-activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptor ligands, activators of PPARgamma, and inhibitors of autotaxin.
J Med Chem 48: 4919-30 (2005)
University Of Tennessee Health Science Center
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
J Med Chem 48: 4910-8 (2005)
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.
J Med Chem 48: 4892-909 (2005)
Johnson & Johnson Pharmaceutical
Structure-based design, synthesis, and biological evaluation of inhibitors of Mycobacterium tuberculosis type II dehydroquinase.
J Med Chem 48: 4871-81 (2005)
Universidad De Santiago De Compostela
Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II.
J Med Chem 48: 4851-60 (2005)
Salk Institute
Combination of molecular modeling, site-directed mutagenesis, and SAR studies to delineate the binding site of pyridopyrimidine antagonists on the human CCK1 receptor.
J Med Chem 48: 4842-50 (2005)
Instituto De QuíMica MéDica (Csic)
Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors.
J Med Chem 48: 4834-41 (2005)
Università
Control of protein-protein interactions: structure-based discovery of low molecular weight inhibitors of the interactions between Pin1 WW domain and phosphopeptides.
J Med Chem 48: 4815-23 (2005)
Cnrs-University Of Lille 2 Umr 8525
Inhibitors of Trypanosoma cruzi trypanothione reductase revealed by virtual screening and parallel synthesis.
J Med Chem 48: 4793-802 (2005)
Universit£T Heidelberg
Structural analysis of isoform-specific inhibitors targeting the tetrahydrobiopterin binding site of human nitric oxide synthases.
J Med Chem 48: 4783-92 (2005)
Sanofi-Aventis
Dicarboxylic acid azacycle l-prolyl-pyrrolidine amides as prolyl oligopeptidase inhibitors and three-dimensional quantitative structure-activity relationship of the enzyme-inhibitor interactions.
J Med Chem 48: 4772-82 (2005)
University Of Kuopio
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
J Med Chem 48: 4765-71 (2005)
The University Of Iowa
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
J Med Chem 48: 4754-64 (2005)
University Of Innsbruck
Rational design of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors: predicting enzyme conformational change and metabolism.
J Med Chem 48: 4750-3 (2005)
Fujisawa Pharmaceutical
Biaryl ureas as potent and orally efficacious melanin concentrating hormone receptor 1 antagonists for the treatment of obesity.
J Med Chem 48: 4746-9 (2005)
Schering-Plough Research Institute
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
J Med Chem 48: 4705-45 (2005)
The Danish University Of Pharmaceutical Sciences
Terphenyl-Based Bak BH3 alpha-helical proteomimetics as low-molecular-weight antagonists of Bcl-xL.
J Am Chem Soc 127: 10191-6 (2005)
Yale University
Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors.
Bioorg Med Chem Lett 15: 3886-90 (2005)
Merck Frosst Canada
Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities.
Bioorg Med Chem Lett 15: 4327-31 (2005)
The University Of Tokyo
Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT2.
Mol Pharmacol 68: 974-82 (2005)
Wyeth Research
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
Bioorg Med Chem Lett 15: 4048-52 (2005)
Universitá
Discovery of hydroxamic acid analogs as dual inhibitors of phosphodiesterase-1 and -5.
Bioorg Med Chem Lett 15: 4085-90 (2005)
Sumitomo Pharmaceuticals
Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: discovery of the dihydropyridazinone motif.
Bioorg Med Chem Lett 15: 4023-8 (2005)
Merck Research Laboratories
1-(4-Amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine derivatives as melanin-concentrating hormone receptor-1 antagonists.
Bioorg Med Chem Lett 15: 3701-6 (2005)
Neurocrine Biosciences
Identification of potent type I MetAPs inhibitors by simple bioisosteric replacement. Part 2: SAR studies of 5-heteroalkyl substituted TCAT derivatives.
Bioorg Med Chem Lett 15: 4130-5 (2005)
Shanghai Graduate School Of The Chinese Academy Of Sciences
1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Bioorg Med Chem Lett 15: 4110-3 (2005)
Clemson University
Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): efficacy in an animal model for schizophrenia.
Bioorg Med Chem Lett 15: 4068-72 (2005)
Merck Research Laboratories
Identification of potent and selective MMP-13 inhibitors.
Bioorg Med Chem Lett 15: 4105-9 (2005)
Wyeth Research
The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion.
Bioorg Med Chem Lett 15: 3874-80 (2005)
University Of Florida
Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.
Bioorg Med Chem Lett 15: 4136-42 (2005)
Seoul National University
Inhibition of tumor cell proliferation by thieno[2,3-d]pyrimidin-4(1H)-one-based analogs.
Bioorg Med Chem Lett 15: 3763-6 (2005)
Wyeth Research
High-speed synthesis of potent C2-symmetric HIV-1 protease inhibitors by in-situ aminocarbonylations.
J Comb Chem 7: 611-7 (2005)
Uppsala University
Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors.
Bioorg Med Chem Lett 15: 3787-90 (2005)
Pfizer
Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Bioorg Med Chem Lett 15: 3853-6 (2005)
Taisho Pharmaceutical
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.
Bioorg Med Chem Lett 15: 4014-8 (2005)
Glaxosmithkline
Phenylpyrroles, a new chemolibrary virtual screening class of 5-HT7 receptor ligands.
Bioorg Med Chem Lett 15: 3753-7 (2005)
Université
New HIV-1 replication inhibitors of the styryquinoline class bearing aroyl/acyl groups at the C-7 position: synthesis and biological activity.
Bioorg Med Chem Lett 15: 4019-22 (2005)
Unité
New pyrrolo[2,1-f]purine-2,4-dione and imidazo[2,1-f]purine-2,4-dione derivatives as potent and selective human A3 adenosine receptor antagonists.
J Med Chem 48: 4697-701 (2005)
Università
Second generation transition state analogue inhibitors of human 5'-methylthioadenosine phosphorylase.
J Med Chem 48: 4679-89 (2005)
Industrial Research
The taming of capsaicin. Reversal of the vanilloid activity of N-acylvanillamines by aromatic iodination.
J Med Chem 48: 4663-9 (2005)
University Of Piemonte Orientale
Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases.
J Med Chem 48: 4628-53 (2005)
University Of Auckland
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