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3-Alkyl-3-hydroxyglutaric acids: a new class of hypocholesterolemic HMG CoA reductase inhibitors. 1.
J Med Chem 28: 597-601 (1985)
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Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 10. Base- and amino acid modified analogues of S-aristeromycinyl-L-homocysteine.
J Med Chem 28: 478-82 (1985)
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Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 9. 2',3'-Dialdehyde derivatives of carbocyclic purine nucleosides as inhibitors of S-adenosylhomocysteine hydrolase.
J Med Chem 28: 471-7 (1985)
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Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
J Med Chem 28: 367-75 (1985)
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3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 1. Structural modification of 5-substituted 3,5-dihydroxypentanoic acids and their lactone derivatives.
J Med Chem 28: 347-58 (1985)
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Receptor-based design of dihydrofolate reductase inhibitors: comparison of crystallographically determined enzyme binding with enzyme affinity in a series of carboxy-substituted trimethoprim analogues.
J Med Chem 28: 303-11 (1985)
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Structure-activity relationships of C-terminal tri- and tetrapeptide fragments that inhibit gastrin activity.
J Med Chem 28: 273-8 (1985)
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Chemistry and antitumor evaluation of selected classical 2,4-diaminoquinazoline analogues of folic acid.
J Med Chem 28: 209-15 (1985)
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Analogues of aminoglutethimide: selective inhibition of aromatase.
J Med Chem 28: 200-4 (1985)
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Enzyme-activated irreversible inhibitors of monoamine oxidase: phenylallylamine structure-activity relationships.
J Med Chem 28: 186-93 (1985)
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2-(beta-Arylethylamino)- and 4-(beta-arylethylamino)quinazolines as phosphodiesterase inhibitors.
J Med Chem 28: 12-7 (1985)
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Synthesis of some quaternary ammonium alkylating agents and their effects on soman-inhibited acetylcholinesterase.
J Med Chem 28: 111-6 (1985)
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N-2,3-Butadienyl-1,4-butanediamine derivatives: potent irreversible inactivators of mammalian polyamine oxidase.
J Med Chem 28: 1-2 (1985)
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Synthesis and evaluation of 4-(substituted thio)-4-androstene-3,17-dione derivatives as potential aromatase inhibitors.
J Med Chem 29: 582-4 (1986)
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Thromboxane synthetase inhibitors and antihypertensive agents. 1. N-[(1H-imidazol-1-yl)alkyl]aryl amides and N-[(1H-1,2,4-triazol-1-yl)alkyl]aryl amides.
J Med Chem 29: 523-30 (1986)
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Neurochemistry of aging. 1. Toxins for an animal model of Alzheimer's disease.
J Med Chem 29: 376-80 (1986)
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Isozyme-specific enzyme inhibitors. 10. Adenosine 5'-triphosphate derivatives as substrates or inhibitors of methionine adenosyltransferases of rat normal and hepatoma tissues.
J Med Chem 29: 318-22 (1986)
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Unsaturated heterocyclic amines as potent time-dependent inhibitors of dopamine beta-hydroxylase.
J Med Chem 29: 315-7 (1986)
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Cardiotonic agents. 3. Synthesis and biological activity of novel 6-(substituted 1H-imidazol-4(5)-yl)-3(2H)-pyridazinones.
J Med Chem 29: 261-7 (1986)
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5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues.
J Med Chem 29: 194-9 (1986)
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Troponoids. 7. Chemistry and dopamine agonist activity of ciladopa and related aralkyltroponylpiperazines.
J Med Chem 29: 186-93 (1986)
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3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 3. 7-(3,5-Disubstituted [1,1'-biphenyl]-2-yl)-3,5-dihydroxy-6-heptenoic acids and their lactone derivatives.
J Med Chem 29: 170-81 (1986)
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3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 2. Structural modification of 7-(substituted aryl)-3,5-dihydroxy-6-heptenoic acids and their lactone derivatives.
J Med Chem 29: 159-69 (1986)
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Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines.
J Med Chem 29: 8-19 (1986)
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Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
J Med Chem 29: 61-9 (1986)
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Synthesis of alkyl-substituted arecoline derivatives as gamma-aminobutyric acid uptake inhibitors.
J Med Chem 29: 125-32 (1986)
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Carboxyl-modified amino acids and peptides as protease inhibitors.
J Med Chem 29: 104-11 (1986)
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Quantitative structure-activity relationship of antifolate inhibition of bacteria cell cultures resistant and sensitive to methotrexate.
J Med Chem 28: 1910-6 (1985)
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Synthesis, absolute configuration, and conformation of the aldose reductase inhibitor sorbinil.
J Med Chem 28: 1716-20 (1985)
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Selective thromboxane synthetase inhibitors. 1. 1-[(Aryloxy)alkyl]-1H-imidazoles.
J Med Chem 28: 1427-32 (1985)
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Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
J Med Chem 28: 841-9 (1985)
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Imidazo[1,5-a]pyridines: a new class of thromboxane A2 synthetase inhibitors.
J Med Chem 28: 164-70 (1985)
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Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine.
J Med Chem 28: 1779-90 (1986)
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A uniquely potent renin inhibitor and its unanticipated plasma binding component.
J Med Chem 28: 1755-6 (1986)
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Difluorostatine- and difluorostatone-containing peptides as potent and specific renin inhibitors.
J Med Chem 28: 1553-5 (1985)
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New bidentates as full inhibitors of enkephalin-degrading enzymes: synthesis and analgesic properties.
J Med Chem 28: 1158-69 (1985)
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Pepstatin-derived inhibitors of aspartic proteinases. A close look at an apparent transition-state analogue inhibitor.
J Med Chem 28: 263-73 (1985)
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Synthesis and dihydropteridine reductase inhibitory effects of potential metabolites of the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine.
J Med Chem 28: 311-7 (1985)
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Acylamino boronic acids and difluoroborane analogues of amino acids: potent inhibitors of chymotrypsin and elastase.
J Med Chem 28: 1917-25 (1986)
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Substituted 2-pyrones, 2-pyridones, and other congeners of elasnin as potential agents for the treatment of chronic obstructive lung diseases.
J Med Chem 28: 1106-9 (1985)
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Amino acid derived latent isocyanates: irreversible inactivation of porcine pancreatic elastase and human leukocyte elastase.
J Med Chem 28: 204-9 (1985)
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The characterization of [3H]sulpiride binding sites in rat striatal membranes.
Brain Res 402: 331-8 (1987)
St, Marianna University School Of Medicine
Dopamine autoreceptor agonists: resolution and pharmacological activity of 2,6-diaminotetrahydrobenzothiazole and an aminothiazole analogue of apomorphine.
J Med Chem 30: 494-8 (1987)
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Multisubstrate inhibitors of dopamine beta-hydroxylase. 2. Structure-activity relationships at the phenethylamine binding site.
J Med Chem 30: 486-94 (1987)
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Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
J Med Chem 30: 400-5 (1987)
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Molecular modification of anticholinergics as probes for muscarinic receptors. 3. Conformationally restricted analogues of benactyzine.
J Med Chem 30: 278-85 (1987)
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Structural requirements for the inhibition of 5-lipoxygenase by 15-hydroxyeicosa-5,8,11,13-tetraenoic acid analogues.
J Med Chem 30: 254-63 (1987)
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Synthesis and structure-activity relationships of pyrazolo[4,3-d]pyrimidin-7-ones as adenosine receptor antagonists.
J Med Chem 30: 91-6 (1987)
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Dopamine agonists related to 3-allyl-6-chloro-2,3,4,5-tetrahydro-1-(4-hydroxyphenyl)-1H-3-benzaz epi ne-7, 8-diol. 6-Position modifications.
J Med Chem 30: 35-40 (1987)
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Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.
J Med Chem 30: 211-4 (1987)
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Synthesis, cell growth inhibition, and antitumor screening of 2-(p-n-butylanilino)purines and their nucleoside analogues.
J Med Chem 30: 109-16 (1987)
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Analogues of caffeine and theophylline: effect of structural alterations on affinity at adenosine receptors.
J Med Chem 29: 1305-8 (1987)
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Structure-activity study of 6-substituted 2-pyranones as inactivators of alpha-chymotrypsin.
J Med Chem 29: 1159-63 (1987)
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Characterization of high affinity [3H]pirenzepine and (-)-[3H] quinuclidinyl benzilate binding to muscarinic cholinergic receptors in rabbit peripheral lung.
J Pharmacol Exp Ther 240: 51-8 (1987)
University Of Arizona
Antidepressant biochemical profile of the novel bicyclic compound Wy-45,030, an ethyl cyclohexanol derivative.
Biochem Pharmacol 35: 4493-7 (1986)
Wyeth Laboratories
Inhibition of cathepsin D by substrate analogues containing statine and by analogues of pepstatin.
J Med Chem 29: 2519-24 (1987)
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Multisubstrate inhibitors of dopamine beta-hydroxylase. 1. Some 1-phenyl and 1-phenyl-bridged derivatives of imidazole-2-thione.
J Med Chem 29: 2465-72 (1987)
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2,3-Dialkyl(dimethylamino)indoles: interaction with 5HT1, 5HT2, and rat stomach fundal serotonin receptors.
J Med Chem 29: 2415-8 (1986)
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5-HT1 and 5-HT2 binding characteristics of some quipazine analogues.
J Med Chem 29: 2375-80 (1986)
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Furanose-pyranose isomerization of reduced pyrimidine and cyclic urea ribosides.
J Med Chem 29: 2351-8 (1986)
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Azasteroids: structure-activity relationships for inhibition of 5 alpha-reductase and of androgen receptor binding.
J Med Chem 29: 2298-315 (1986)
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Syntheses of 5,6,7- and 5,7,8-trioxygenated 3',4'-dihydroxyflavones having alkoxy groups and their inhibitory activities against arachidonate 5-lipoxygenase.
J Med Chem 29: 2256-62 (1986)
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Antibacterial activity of phosphono dipeptides related to alafosfalin.
J Med Chem 29: 2212-7 (1986)
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Alkylglycidic acids: potential new hypoglycemic agents.
J Med Chem 29: 2184-90 (1986)
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Nonquaternary cholinesterase reactivators. 3. 3(5)-Substituted 1,2,4-oxadiazol-5(3)-aldoximes and 1,2,4-oxadiazole-5(3)-thiocarbohydroximates as reactivators of organophosphonate-inhibited eel and human acetylcholinesterase in vitro.
J Med Chem 29: 2174-83 (1986)
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Cardiotonic agents. 4. Synthesis and biological evaluation of N-substituted 2,4,4a,5-tetrahydro-3H-indeno[1,2-c]pyridazin-3-ones: rigid structures derived from CI-930 and analogues.
J Med Chem 29: 2142-8 (1986)
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Synthesis of 10-acetyl-5,8-dideazafolic acid: a potent inhibitor of glycinamide ribonucleotide transformylase.
J Med Chem 29: 2117-9 (1986)
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Binding requirements of phenolic phenylethylamines in the benzonorbornene skeleton at the active site of phenylethanolamine N-methyltransferase.
J Med Chem 29: 1972-82 (1986)
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Cholecystokinin antagonists. Synthesis of asperlicin analogues with improved potency and water solubility.
J Med Chem 29: 1941-5 (1986)
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Synthesis and dopaminergic binding of 2-aryldopamine analogues: phenethylamines, 3-benzazepines, and 9-(aminomethyl)fluorenes.
J Med Chem 29: 1904-12 (1986)
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Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics.
J Med Chem 29: 1889-95 (1986)
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Inactivation of gamma-aminobutyric acid aminotransferase by (S,E)-4-amino-5-fluoropent-2-enoic acid and effect on the enzyme of (E)-3-(1-aminocyclopropyl)-2-propenoic acid.
J Med Chem 29: 1840-6 (1986)
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Isozyme-specific enzyme inhibitors. 12. C- and N-methylmethionines as substrates and inhibitors of methionine adenosyltransferases of normal and hepatoma rat tissues.
J Med Chem 29: 1743-8 (1986)
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Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
J Med Chem 29: 520-3 (1986)
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Kinetics and mechanism of interaction of 10-propargyl-5,8-dideazafolate with thymidylate synthase.
J Med Chem 29: 478-82 (1986)
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Quinazoline antifolates inhibiting thymidylate synthase: benzoyl ring modifications.
J Med Chem 29: 468-72 (1986)
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Thiol addition to quinones: model reactions for the inactivation of thymidylate synthase by 5-p-benzoquinonyl-2'-deoxyuridine 5'-phosphate.
J Med Chem 29: 1714-20 (1986)
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Nonquaternary cholinesterase reactivators. 4. Dialkylaminoalkyl thioesters of alpha-keto thiohydroximic acids as reactivators of ethyl methylphosphonyl- and 1,2,2-trimethylpropyl methylphosphonyl-acetylcholinesterase in vitro.
J Med Chem 29: 1689-96 (1986)
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In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.
J Med Chem 29: 1663-8 (1986)
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Selective thromboxane synthetase inhibitors. 3. 1H-imidazol-1-yl-substituted benzo[b]furan-, benzo[b]thiophene-, and indole-2- and -3-carboxylic acids.
J Med Chem 29: 1637-43 (1986)
TBA
Design and synthesis of sodium (beta R*, gamma S*)-4-[[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl] thio]-gamma-hydroxy-beta-methylbenzenebutanoate: a novel, selective, and orally active receptor antagonist of leukotriene D4.
J Med Chem 29: 1573-6 (1986)
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N-Substituted sulfonamide carbonic anhydrase inhibitors with topical effects on intraocular pressure.
J Med Chem 29: 1488-94 (1986)
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5-(Halomethyl)-2-pyranones as irreversible inhibitors of alpha-chymotrypsin.
J Med Chem 29: 1483-7 (1986)
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Selective monoamine oxidase inhibitors. 3. Cyclic compounds related to 4-aminophenethylamine. Preparation and neuron-selective action of some 5-(2-aminoethyl)-2,3-dihydroindoles.
J Med Chem 29: 1406-12 (1986)
TBA
Synthesis of pyrimidin-2-one nucleosides as acid-stable inhibitors of cytidine deaminase.
J Med Chem 29: 1374-80 (1986)
TBA
Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones.
J Med Chem 29: 1362-9 (1986)
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Substituted 1-benzylimidazole-2-thiols as potent and orally active inhibitors of dopamine beta-hydroxylase.
J Med Chem 29: 887-9 (1986)
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Synthesis and biological activity of resolved C-10 diastereomers of 10-methyl- and 10-ethyl-10-deazaminopterin.
J Med Chem 29: 1056-61 (1986)
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Synthesis and biological activities of oligo(8-bromoadenylates) as analogues of 5'-O-triphosphoadenylyl(2'----5')adenylyl(2'----5')adenosine.
J Med Chem 29: 1015-22 (1986)
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A novel class of conformationally restricted heterocyclic muscarinic agonists.
J Med Chem 29: 1004-9 (1986)
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The binding of L-[3H]nicotine to a single class of high affinity sites in rat brain membranes.
Mol Pharmacol 29: 448-54 (1986)
R. J. Reynolds Tobacco
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 5. 6-(Fluoren-9-yl)- and 6-(fluoren-9-ylidenyl)-3,5-dihydroxyhexanoic acids and their lactone derivatives.
J Med Chem 29: 852-5 (1986)
TBA
4-Amino-2-(substituted methyl)-2-butenoic acids: substrates and potent inhibitors of gamma-aminobutyric acid aminotransferase.
J Med Chem 29: 764-70 (1986)
TBA
Bipyridine cardiotonics: the three-dimensional structures of amrinone and milrinone.
J Med Chem 29: 635-40 (1986)
TBA
Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents.
J Med Chem 29: 630-4 (1986)
TBA
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones.
J Med Chem 30: 2277-83 (1988)
Medical Research Division Of American Cyanamid
Novel 1H-benzimidazol-4-ols with potent 5-lipoxygenase inhibitory activity.
J Med Chem 30: 2216-21 (1988)
Beecham Pharmaceuticals Research Division
Inhibition of phenylethanolamine N-methyltransferase (PNMT) by aromatic hydroxy-substituted 1,2,3,4,-tetrahydroisoquinolines: further studies on the hydrophilic pocket of the aromatic ring binding region of the active site.
J Med Chem 30: 2208-16 (1988)
University Of Kansas
Binding orientation of amphetamine and norfenfluramine analogues in the benzonorbornene and benzobicyclo[3.2.1]octane ring systems at the active site of phenylethanolamine N-methyltransferase (PNMT)
J Med Chem 30: 2191-208 (1988)
University Of Kansas
In vivo characterization of hydroxamic acid inhibitors of 5-lipoxygenase.
J Med Chem 30: 2121-6 (1987)
Abbott Laboratories
Phenylephrine derivatives as leukotriene D4 antagonists.
J Med Chem 30: 2087-93 (1987)
Wyeth Laboratories
Carbamate ester derivatives as potential prodrugs of the presynaptic dopamine autoreceptor agonist (-)-3-(3-hydroxyphenyl)-N-propylpiperidine.
J Med Chem 30: 2008-12 (1987)
Astra Alab
Angiotensin-converting enzyme inhibitors: perhydro-1,4-thiazepin-5-one derivatives.
J Med Chem 30: 1984-91 (1987)
Sankyo
Synthesis of some [N-(2-haloalkyl)amino]tetralin derivatives as potential irreversible labels for bovine anterior pituitary D2 dopamine receptors.
J Med Chem 30: 1879-87 (1987)
Queen'S Medical Centre
Total synthesis and biological evaluation of structural analogues of compactin and dihydromevinolin.
J Med Chem 30: 1858-73 (1987)
University Of California
Thromboxane synthase inhibitors. Synthesis and pharmacological activity of (R)-, (S)-, and (+/-)-2,2-dimethyl-6-[2-(1H-imidazol-1-yl)-1-[[(4-methoxyphenyl)- methoxy]methyl]ethoxy]hexanoic acids.
J Med Chem 30: 1812-8 (1987)
Searle Research And Development
Cardiotonic agents. 6. Synthesis and inotropic activity of 2,4-dihydro-5-[4-(1H-imidazol-1-yl)phenyl]-3H-pyrazol-3-ones: ring-contracted analogues of imazodan (CI-914).
J Med Chem 30: 1724-8 (1987)
Warner-Lambert/Parke-Davis Pharmaceutical Research
Inactivation of thymidylate synthase at an alternate high-affinity binding site.
J Med Chem 30: 1705-6 (1987)
University Of Kansas
Inhibition of human sputum elastase by substituted 2-pyrones.
J Med Chem 30: 1017-23 (1987)
TBA
Peptidyl carbamates incorporating amino acid isosteres as novel elastase inhibitors.
J Med Chem 29: 1468-76 (1986)
TBA
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 4. Side chain ester derivatives of mevinolin.
J Med Chem 29: 849-52 (1986)
TBA
Anticoagulant peptides: nature of the interaction of the C-terminal region of hirudin with a noncatalytic binding site on thrombin.
J Med Chem 30: 1688-91 (1987)
TBA
Phosphorus amino acid analogues as inhibitors of leucine aminopeptidase.
J Med Chem 30: 1603-9 (1987)
TBA
Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.
J Med Chem 30: 1550-4 (1987)
TBA
Aromatase inhibition by 5-substituted pyrimidines and dihydropyrimidines.
J Med Chem 30: 1359-65 (1987)
TBA
Inhibitors of dopamine beta-hydroxylase. 3. Some 1-(pyridylmethyl)imidazole-2-thiones.
J Med Chem 30: 1309-13 (1987)
TBA
Folate analogues. 30. Synthesis and biological evaluation of N10-propargyl-5,8-dideaza-5,6,7,8-tetrahydrofolic acid and related compounds.
J Med Chem 30: 1256-61 (1987)
TBA
N10-substituted 5,8-dideazafolate inhibitors of glycinamide ribonucleotide transformylase.
J Med Chem 30: 1254-6 (1987)
TBA
Quantitative structure-activity relationship of triazine-antifolate inhibition of Leishmania dihydrofolate reductase and cell growth.
J Med Chem 30: 1218-24 (1987)
TBA
Synthesis and 5-lipoxygenase inhibitory activity of 5-hydroperoxy-6,8,11,14-eicosatetraenoic acid analogues.
J Med Chem 30: 1177-86 (1987)
TBA
Resolution of (+/-)-2-tetradecyloxiranecarboxylic acid. Absolute configuration and chiral synthesis of the hypoglycemic R enantiomer and biological activity of enantiomers.
J Med Chem 30: 1094-7 (1987)
TBA
Synthesis, structure, and biological activity of certain 2-deoxy-beta-D-ribo-hexopyranosyl nucleosides and nucleotides.
J Med Chem 30: 1044-54 (1987)
TBA
Thromboxane synthetase inhibitors and antihypertensive agents. 3. N-[(1H-imidazol-1-yl)alkyl]heteroaryl amides as potent enzyme inhibitors.
J Med Chem 30: 1036-40 (1987)
TBA
Cardiotonic agents. 5. 1,2-Dihydro-5-[4-(1H-imidazol-1-yl)phenyl]-6-methyl-2-oxo-3- pyridinecarbonitriles and related compounds. Synthesis and inotropic activity.
J Med Chem 30: 1023-9 (1987)
TBA
N6-phenyladenosines: pronounced effect of phenyl substituents on affinity for A2 adenosine receptors.
J Med Chem 30: 954-6 (1987)
TBA
N-methyl derivatives of the 5-HT2 agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane.
J Med Chem 30: 930-2 (1987)
TBA
Isozyme-specific enzyme inhibitors. 13. S-[5'(R)-[(N-triphosphoamino)methyl]adenosyl]-L-homocysteine, a potent inhibitor of rat methionine adenosyltransferases.
J Med Chem 30: 888-94 (1987)
TBA
Synthesis and biological activity of partially modified retro-inverso pseudopeptide derivatives of the C-terminal tetrapeptide of gastrin.
J Med Chem 30: 758-63 (1987)
TBA
Synthesis and binding affinities of analogues of cholecystokinin-(30-33) as probes for central nervous system cholecystokinin receptors.
J Med Chem 30: 729-32 (1987)
TBA
Synthesis and antiarrhythmic activity of novel 3-alkyl-1-[omega-[4-[(alkylsulfonyl)amino]phenyl]-omega- hydroxyalkyl]-1H-imidazolium salts and related compounds.
J Med Chem 30: 696-704 (1987)
TBA
Thienothiopyran-2-sulfonamides: a novel class of water-soluble carbonic anhydrase inhibitors.
J Med Chem 30: 591-7 (1987)
TBA
Design of alternate substrate inhibitors of serine proteases. Synergistic use of alkyl substitution to impede enzyme-catalyzed deacylation.
J Med Chem 30: 589-591 (1987)
TBA
The structural basis for the interaction between L-tryptophan and the Escherichia coli trp aporepressor.
J Biol Chem 262: 4922-7 (1987)
University Of Chicago
alpha-Methylproline-containing renin inhibitory peptides: in vivo evaluation in an anesthetized, ganglion-blocked, hog renin infused rat model.
J Med Chem 30: 536-41 (1987)
TBA
Central serotonin receptors as targets for drug research.
J Med Chem 30: 1-12 (1987)
TBA
Pepstatin analogues as novel renin inhibitors.
J Med Chem 29: 1152-9 (1987)
TBA
Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo.
J Med Chem 29: 2088-93 (1986)
TBA
Design and synthesis of potent and specific renin inhibitors containing difluorostatine, difluorostatone, and related analogues.
J Med Chem 29: 2080-7 (1986)
TBA
Synthesis and alpha-D-glucosidase inhibitory activity of N-substituted valiolamine derivatives as potential oral antidiabetic agents.
J Med Chem 29: 1038-46 (1986)
TBA
Thromboxane synthetase inhibitors and antihypertensive agents. 2. N-[(1H-imidazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones and N-[(1H-1,2,4-triazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones as unique antihypertensive agents.
J Med Chem 29: 816-9 (1986)
TBA
1H NMR configurational correlation for retro-inverso dipeptides: application to the determination of the absolute configuration of"enkephalinase" inhibitors. Relationships between stereochemistry and enzyme recognition.
J Med Chem 29: 751-7 (1986)
TBA
Enol lactone inhibitors of serine proteases. The effect of regiochemistry on the inactivation behavior of phenyl-substituted (halomethylene)tetra- and -dihydrofuranones and (halomethylene)tetrahydropyranones toward alpha-chymotrypsin: stable acyl enzyme intermediate.
J Med Chem 29: 230-8 (1986)
TBA
Isozyme-specific enzyme inhibitors. 14. 5'(R)-C-[(L-homocystein-S-yl)methyl]adenosine 5'-(beta,gamma-imidotriphosphate), a potent inhibitor of rat methionine adenosyltransferases.
J Med Chem 30: 1599-603 (1987)
TBA
Inhibition of the mammalian beta-lactamase renal dipeptidase (dehydropeptidase-I) by (Z)-2-(acylamino)-3-substituted-propenoic acids.
J Med Chem 30: 1074-90 (1987)
TBA
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.
J Med Chem 30: 805-9 (1987)
TBA
Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids.
J Med Chem 29: 1436-41 (1986)
TBA
Isozyme-specific enzyme inhibitors. 11. L-homocysteine-ATP S-C5' covalent adducts as inhibitors of rat methionine adenosyltransferases.
J Med Chem 29: 1030-8 (1986)
TBA
Synthesis of glycopyranosylphosphonate analogues of certain natural nucleoside diphosphate sugars as potential inhibitors of glycosyltransferases.
J Med Chem 30: 1383-91 (1987)
TBA
Folate analogues as inhibitors of thymidylate synthase.
J Med Chem 30: 675-8 (1987)
TBA
Methotrexate analogues. 28. Synthesis and biological evaluation of new gamma-monoamides of aminopterin and methotrexate.
J Med Chem 29: 1703-9 (1986)
TBA
In vitro inhibition of estrogen sulfoconjugation by some 2- and 4-substituted estra-1,3,5(10)-trien-17 beta-ols1a.
J Med Chem 29: 692-8 (1986)
TBA
Inhibitory effects of various flavonoids isolated from leaves of persimmon on angiotensin-converting enzyme activity.
J Nat Prod 50: 680-3
Ehime University
Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers.
Neuropharmacology 27: 399-408 (1988)
Organon International
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 11. Molecular dissections of neplanocin A as potential inhibitors of S-adenosylhomocysteine hydrolase.
J Med Chem 31: 1729-38 (1988)
University Of Kansas
Synthesis, configuration, and evaluation of two conformationally restrained analogues of phencyclidine.
J Med Chem 31: 1571-5 (1988)
National Institute Of Diabetes, Digestive And Kidney Diseases
Stereoisomers of allenic amines as inactivators of monoamine oxidase type B. Stereochemical probes of the active site.
J Med Chem 31: 1558-66 (1988)
Syntex Research
Substituted benzamides. 1. Potential nondopaminergic antagonists of chemotherapy-induced nausea and emesis.
J Med Chem 31: 1548-58 (1988)
Bristol-Myers
Dicarbavasopressin antagonist analogues exhibit reduced in vivo agonist activity.
J Med Chem 31: 1487-9 (1988)
Smith Kline & French Laboratories
Synthesis and estrogen receptor selectivity of 1,1-bis(4-hydroxyphenyl)-2-(p-halophenyl)ethylenes.
J Med Chem 31: 1471-5 (1988)
University Of Georgia
Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists.
J Med Chem 31: 1463-6 (1988)
Nova Pharmaceutical
Synthesis and serotonin receptor affinities of a series of enantiomers of alpha-methyltryptamines: evidence for the binding conformation of tryptamines at serotonin 5-HT1B receptors.
J Med Chem 31: 1406-12 (1988)
Purdue University
Synthesis and dopamine agonist and antagonist effects of (R)-(-)- and (S)-(+)-11-hydroxy-N-n-propylnoraporphine.
J Med Chem 31: 1392-6 (1988)
Northeastern University
Cardiotonic agents. Synthesis and inotropic activity of a series of isoquinolin-3-ol derivatives.
J Med Chem 31: 1363-8 (1988)
Ortho Pharmaceutical
Methotrexate analogues. 33. N delta-acyl-N alpha-(4-amino-4-deoxypteroyl)-L-ornithine derivatives: synthesis and in vitro antitumor activity.
J Med Chem 31: 1332-7 (1988)
Harvard Medical School
Methotrexate analogues. 32. Chain extension, alpha-carboxyl deletion, and gamma-carboxyl replacement by sulfonate and phosphonate: effect on enzyme binding and cell-growth inhibition.
J Med Chem 31: 1326-31 (1988)
Harvard Medical School
Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.
J Med Chem 31: 1312-6 (1988)
Royal Danish School Of Pharmacy
N6-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)ethyl]adenosine and its uronamide derivatives. Novel adenosine agonists with both high affinity and high selectivity for the adenosine A2 receptor.
J Med Chem 31: 1282-5 (1988)
Warner-Lambert
(+/-)-9-Amino-1,2,3,4-tetrahydroacridin-1-ol. A potential Alzheimer's disease therapeutic of low toxicity.
J Med Chem 31: 1278-9 (1988)
Hoechst-Roussel Pharmaceuticals
Chemical and pharmaceutical studies on medicinal plants in Paraguay. Geraniin, an angiotensin-converting enzyme inhibitor from "paraparai mi," Phyllanthus niruri.
J Nat Prod 51: 357-359 (1988)
TBA
Inhibition of Cow's Milk Xanthine Oxidase by Flavonoids
J Nat Prod 51: 345-348 (1988)
TBA
Chemical synthesis and biological activities of 5-deazaaminopterin analogues bearing substituent(s) at the 5- and/or 7-position(s).
J Med Chem 31: 1209-15 (1988)
Cornell University
Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.
J Med Chem 31: 1179-83 (1988)
Universit£
Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine.
J Med Chem 31: 1169-74 (1988)
Dr. Karl Thomae
Linear free energy relationship studies of enzyme active site binding: thymidylate synthase.
J Med Chem 31: 1141-7 (1988)
University Of Kansas
Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor.
J Med Chem 31: 1087-93 (1988)
Merrell Dow Research Institute
Analogues of aminoglutethimide based on 1-phenyl-3-azabicyclo[3.1.0]hexane-2,4-dione: selective inhibition of aromatase activity.
J Med Chem 31: 971-6 (1988)
Institute Of Cancer Research
Analogues of gamma-hydroxybutyric acid. Synthesis and binding studies.
J Med Chem 31: 893-7 (1988)
Centre De Neurochimie Du Cnrs
(Acyloxy)benzophenones and (acyloxy)-4-pyrones. A new class of inhibitors of human neutrophil elastase.
J Med Chem 31: 1052-61 (1988)
Searle Research And Development
Structure-activity profile of a series of novel triazoloquinazoline adenosine antagonists.
J Med Chem 31: 1014-20 (1988)
Ciba-Geigy
[1,2,4]Triazolo[4,3-a]quinoxalin-4-amines: a new class of A1 receptor selective adenosine antagonists.
J Med Chem 31: 1011-4 (1988)
Warner-Lambert
Synthesis and evaluation of 3-substituted analogues of 1,2,3,4-tetrahydroisoquinoline as inhibitors of phenylethanolamine N-methyltransferase.
J Med Chem 31: 824-30 (1988)
University Of Kansas
Synthesis, intramolecular hydrogen bonding, and biochemical studies of clitocine, a naturally occurring exocyclic amino nucleoside.
J Med Chem 31: 786-90 (1988)
Nucleic Acid Research Institute
Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines.
J Med Chem 31: 779-85 (1988)
Kyowa Hakko Kogyo
Methotrexate analogues. 31. Meta and ortho isomers of aminopterin, compounds with a double bond in the side chain, and a novel analogue modified at the alpha-carbon: chemical and in vitro biological studies.
J Med Chem 31: 763-8 (1988)
Institute
Photoaffinity labeling adenosine A1 receptors with an antagonist 125I-labeled aryl azide derivative of 8-phenylxanthine.
J Med Chem 31: 752-6 (1988)
University Of Virginia School Of Medicine
125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors.
J Med Chem 31: 745-51 (1988)
University Of Virginia School Of Medicine
Beta-substituted phenethylamines as high-affinity mechanism-based inhibitors of dopamine beta-hydroxylase.
J Med Chem 31: 704-6 (1988)
Smith Kline & French Laboratories
6- and 8-hydroxy-3,4-dihydro-3-(dipropylamino)-2H-1-benzopyrans. Dopamine agonists with autoreceptor selectivity.
J Med Chem 31: 688-91 (1988)
Warner-Lambert
8-Aryl-and 8-cycloalkyl-1,3-dipropylxanthines: further potent and selective antagonists for A1-adenosine receptors.
J Med Chem 31: 613-7 (1988)
National Institute Of Diabetes, Digestive And Kidney Diseases
Derivatives of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.
J Med Chem 31: 577-82 (1988)
University Of Uppsala
Synthesis and biological characterization of pyridohomotropanes. Structure-activity relationships of conformationally restricted nicotinoids.
J Med Chem 31: 506-9 (1988)
Stauffer Chemical
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
J Med Chem 31: 503-6 (1988)
Warner-Lambert
9-(trans-2',trans-3'-dihydroxycyclopent-4'-enyl) derivatives of adenine and 3-deazaadenine: potent inhibitors of bovine liver S-adenosylhomocysteine hydrolase.
J Med Chem 31: 500-3 (1988)
University Of Kansas
Acetohydroxamic acids as potent, selective, orally active 5-lipoxygenase inhibitors.
J Med Chem 31: 499-500 (1988)
Wellcome Research Laboratories
Pyrido[2,1-b]quinazolinecarboxamide derivatives as platelet activating factor antagonists.
J Med Chem 31: 466-72 (1988)
Hoffmann-La Roche
Conformational and steric aspects of the inhibition of phenylethanolamine N-methyltransferase by benzylamines.
J Med Chem 31: 433-44 (1988)
University Of Kansas
Angiotensin-converting enzyme inhibitors. 2. Perhydroazepin-2-one derivatives.
J Med Chem 31: 422-8 (1988)
Sankyo
Adenosine deaminase inhibitors. Synthesis and biological activity of deaza analogues of erythro-9-(2-hydroxy-3-nonyl)adenine.
J Med Chem 31: 390-3 (1988)
Universit£
Crystal structures and pharmacologic activities of 1,4-dihydropyridine calcium channel antagonists of the isobutyl methyl 2,6-dimethyl-4-(substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylate (nisoldipine) series.
J Med Chem 31: 300-5 (1988)
University Of Oslo
New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships.
J Med Chem 31: 84-91 (1988)
Ono Pharmaceutical
Conformational preference for the binding of biaryl substrates and inhibitors to the active site of phenylethanolamine N-methyltransferase.
J Med Chem 31: 60-5 (1988)
University Of Kansas
Orally active hydroxamic acid inhibitors of leukotriene biosynthesis.
J Med Chem 31: 3-5 (1988)
Abbott Laboratories
N6-(arylalkyl)adenosines. Identification of N6-(9-fluorenylmethyl)adenosine as a highly potent agonist for the adenosine A2 receptor.
J Med Chem 31: 271-3 (1988)
Warner-Lambert
Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted 1,4-benzodiazepin-2-amines.
J Med Chem 31: 264-8 (1988)
Merck Sharp & Dohme Research Laboratories
Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.
J Med Chem 31: 176-81 (1988)
Merck Sharp & Dohme Research Laboratories
Conformational requirements of substrates for activity with phenylethanolamine N-methyltransferase.
J Med Chem 31: 169-71 (1988)
University Of Kansas
Dimethylsulfonium and thiolanium analogues of the muscarinic agent oxotremorine.
J Med Chem 31: 164-8 (1988)
University Of California
Renin inhibitors. Free-Wilson and correlation analysis of the inhibitory potency of a series of pepstatin analogues on plasma renin.
J Med Chem 30: 2287-91 (1988)
Sanofi Recherche
Renin inhibitors based on novel dipeptide analogues. Incorporation of the dehydrohydroxyethylene isostere at the scissile bond.
J Med Chem 30: 1978-83 (1987)
Abbott Laboratories
Renin inhibitors. Statine-containing tetrapeptides with varied hydrophobic carboxy termini.
J Med Chem 30: 1853-7 (1987)
Merck Sharp & Dohme Research Laboratories
alpha,alpha-Difluoro-beta-aminodeoxystatine-containing renin inhibitory peptides.
J Med Chem 30: 1837-42 (1987)
Upjohn
Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond.
J Med Chem 30: 1729-37 (1987)
Abbott Laboratories
Fluoro ketone containing peptides as inhibitors of human renin.
J Med Chem 30: 1617-22 (1987)
TBA
New inhibitors of human renin that contain novel Leu-Val replacements.
J Med Chem 30: 1609-16 (1987)
TBA
Structure-activity relationships in an imidazole-based series of thromboxane synthase inhibitors.
J Med Chem 30: 1588-95 (1987)
TBA
Analysis of structure-activity relationships in renin substrate analogue inhibitory peptides.
J Med Chem 30: 1287-95 (1987)
TBA
Novel renin inhibitors containing analogues of statine retro-inverted at the C-termini: specificity at the P2 histidine site.
J Med Chem 30: 1224-8 (1987)
TBA
Renin inhibitors. Design of angiotensinogen transition-state analogues containing novel. (2R,3R,4R,5S)-5-amino-3,4-dihydroxy-2-isopropyl-7-methyloctanoic acid.
J Med Chem 30: 976-82 (1987)
TBA
The hypothetical active site lattice. An approach to modelling active sites from data on inhibitor molecules.
J Med Chem 31: 1396-406 (1988)
Uniroyal Chemical
Synthesis and renin inhibitory activity of angiotensinogen analogues having dehydrostatine, Leu psi [CH2S]Val, or Leu psi [CH2SO]Val at the P1-P1' cleavage site.
J Med Chem 31: 1377-82 (1988)
Upjohn
Conformationally constrained renin inhibitory peptides: gamma-lactam-bridged dipeptide isostere as conformational restriction.
J Med Chem 31: 1369-76 (1988)
Upjohn
Evaluation of 5-enolpyruvoylshikimate-3-phosphate synthase substrate and inhibitor binding by stopped-flow and equilibrium fluorescence measurements.
Biochemistry 27: 1604-10 (1988)
Monsanto Agricultural
Design of potent cyclic gonadotropin releasing hormone antagonists.
J Med Chem 31: 677-82 (1988)
Salk Institute
Renin inhibitors containing psi[CH2O] pseudopeptide inserts.
J Med Chem 31: 671-7 (1988)
Upjohn
New inhibitors of human renin that contain novel Leu-Val replacements. Examination of the P1 site.
J Med Chem 31: 532-9 (1988)
Abbott Laboratories
Quantitative structure-activity relationships for the inhibition of Escherichia coli dihydrofolate reductase by 5-(substituted benzyl)-2,4-diaminopyrimidines.
J Med Chem 31: 366-70 (1988)
Beijing Medical University
Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogues of angiotensinogen.
J Med Chem 31: 284-95 (1988)
Abbott Laboratories
Design, structure-activity, and molecular modeling studies of potent renin inhibitory peptides having N-terminal Nin-For-Trp (Ftr): angiotensinogen congeners modified by P1-P1' Phe-Phe, Sta, Leu psi[CH(OH)CH2]Val or leu psi[CH2NH]Val substitutions.
J Med Chem 31: 18-30 (1988)
Upjohn
Evaluation of the importance of hydrophobic interactions in drug binding to dihydrofolate reductase.
J Med Chem 31: 129-37 (1988)
Pennsylvania State University
Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes.
Neuron 1: 403-10 (1988)
National Institute Of Mental Health
A photoaffinity label for the D-1 dopamine receptor, (RS)-7-[125I]Iodo-8-hydroxy-3-methyl-1-(4'-azidophenyl)-2,3,4,5- tetrahydro-1H-3-benzazepine, selectively identifies the ligand binding subunits of the receptor.
J Med Chem 31: 2069-71 (1988)
Northeastern University
1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine analogues. Inactivation of monoamine oxidase by conformationally rigid analogues of N,N-dimethylcinnamylamine.
J Med Chem 31: 1566-70 (1988)
Northwestern University
Toward the synthesis of isozyme-specific enzyme inhibitors. Potent inhibitors of rat methionine adenosyltransferases. Effect of one-atom elongation of the ribose-P alpha bridge in two covalent adducts of L-methionine and beta,gamma-imido-ATP.
J Med Chem 31: 384-9 (1988)
Fox Chase Cancer Center
N-aryl 3-halogenated azetidin-2-ones and benzocarbacephems, inhibitors of beta-lactamases.
J Med Chem 31: 370-4 (1988)
Cnrs-Cercoa
Characterization of cardiac A1 adenosine receptors by ligand binding and photoaffinity labeling.
J Pharmacol Exp Ther 244: 1150-6 (1988)
University Of Illinois At Chicago
2-Chloro-N6-cyclopentyladenosine: a highly selective agonist at A1 adenosine receptors.
Naunyn Schmiedebergs Arch Pharmacol 337: 687-9 (1988)
Pharmakologisches Institut, Heidelberg
2',3'-Dideoxy-N6-cyclohexyladenosine: an adenosine derivative with antagonist properties at adenosine receptors.
Eur J Pharmacol 156: 157-60 (1988)
Pharmakologisches Institut
Inhibition of arginine aminopeptidase by bestatin and arphamenine analogues. Evidence for a new mode of binding to aminopeptidases.
Biochemistry 27: 7301-10 (1988)
University Of Wisconsin
Synthesis and anticholinesterase activity of (-)-N1-norphysostigmine, (-)-eseramine, and other N(1)-substituted analogues of (-)-physostigmine.
J Med Chem 31: 2297-300 (1989)
Niddk
Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity.
J Med Chem 31: 2221-7 (1988)
Ortho Pharmaceutical
Synthesis of sulfur-containing analogues of bestatin. Inhibition of aminopeptidases by alpha-thiolbestatin analogues.
J Med Chem 31: 2193-9 (1988)
University Of Wisconsin
Synthesis and antifolate activity of 5-methyl-5,10-dideaza analogues of aminopterin and folic acid and an alternative synthesis of 5,10-dideazatetrahydrofolic acid, a potent inhibitor of glycinamide ribonucleotide formyltransferase.
J Med Chem 31: 2164-9 (1988)
Southern Research Institute
A pyrimidine-based"flexible" bisubstrate analogue inhibitor of human thymidylate synthase.
J Med Chem 31: 2126-32 (1988)
University Of Utah
Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.
J Med Chem 31: 2034-9 (1988)
Merrell Dow Research Institute
(S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo- 2-methoxybenzamide hydrochloride, a new selective radioligand for dopamine D-2 receptors.
J Med Chem 31: 2027-33 (1988)
Vanderbilt University
Stereochemical aspects of phenylethanolamine analogues as substrates of phenylethanolamine N-methyltransferase.
J Med Chem 31: 1984-6 (1988)
University Of Kansas
Arylpiperazine derivatives as high-affinity 5-HT1A serotonin ligands.
J Med Chem 31: 1968-71 (1988)
Virginia Commonwealth University
Structure-activity analysis of a class of orally active hydroxamic acid inhibitors of leukotriene biosynthesis.
J Med Chem 31: 1960-4 (1988)
Abbott Laboratories
Nucleosides of 1,4-thiazin-3-one and derivatives as tetrahedral intermediate analogues of enzymes in pyrimidine nucleoside metabolism.
J Med Chem 31: 1575-9 (1988)
Washington State University
Novel photoaffinity label for the dopamine D2 receptor: synthesis of 4-azido-5-iodo-2-methoxy-N-[1-(phenylmethyl)-4-piperidinyl] benzamide (iodoazidoclebopride, IAC) and the corresponding 125I-labeled analogue (125IAC).
J Med Chem 28: 405-7 (1985)
TBA
Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability.
J Med Chem 31: 2277-88 (1989)
Abbott Laboratories
Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a dihydroxyethylene transition-state mimic at the scissile bond to impart greater inhibitory potency.
J Med Chem 31: 2264-76 (1989)
Abbott Laboratories
Putative selective 5-HT-2 antagonists block serotonin 5-HT-1c receptors in the choroid plexus.
J Pharmacol Exp Ther 247: 169-73 (1988)
Vanderbilt University
Synthesis and biological activity of some transition-state inhibitors of human renin.
J Med Chem 31: 1839-46 (1988)
Ciba-Geigy
Phosphinic acid inhibitors of D-alanyl-D-alanine ligase.
J Med Chem 31: 1772-8 (1988)
Merck Sharp And Dohme Research Laboratories
Substrate analogue inhibitors of the IgA1 proteinases from Neisseria gonorrhoeae.
J Med Chem 31: 1647-51 (1988)
University Hospital
4-Hydroxy-3-quinolinecarboxamides with antiarthritic and analgesic activities.
J Med Chem 31: 1453-62 (1988)
Centre De Recherches Roussel-Uclaf
Glucosamine synthetase from Escherichia coli: kinetic mechanism and inhibition by N3-fumaroyl-L-2,3-diaminopropionic derivatives.
Biochemistry 27: 2282-7 (1988)
Enscp
7-[3-(4-[2,3-Dimethylphenyl]piperazinyl)propoxy]-2(1H)-quinolinone (OPC-4392), a presynaptic dopamine autoreceptor agonist and postsynaptic D2 receptor antagonist.
Life Sci 42: 1941-54 (1988)
Tokushima Research Institute
New human renin inhibitors containing an unnatural amino acid, norstatine.
J Med Chem 31: 701-4 (1988)
Kissei Pharmaceutical
Inhibition of porcine pepsin by two substrate analogues containing statine. The effect of histidine at the P2 subsite on the inhibition of aspartic proteinases.
J Med Chem 31: 625-9 (1988)
University Of Wisconsin
Synthesis and evaluation of 5-amino-1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamidine and certain related nucleosides as inhibitors of purine nucleoside phosphorylase.
J Med Chem 31: 330-5 (1988)
Nucleic Acid Research Institute
Spiro hydantoin aldose reductase inhibitors.
J Med Chem 31: 230-43 (1988)
Pfizer
Synthesis and biological evaluation of 8-deazahomofolic acid and its tetrahydro derivative.
J Med Chem 31: 150-3 (1988)
Sri International
Optimization and in vivo evaluations of a series of small, potent, and specific renin inhibitors containing a novel Leu-Val replacement.
J Med Chem 30: 2137-44 (1987)
Abbott Laboratories
Novel inhibitors of rat lens aldose reductase: N-[[(substituted amino)phenyl]sulfonyl]glycines.
J Med Chem 30: 1595-8 (1987)
TBA
Methotrexate analogues. 30. Dihydrofolate reductase inhibition and in vitro tumor cell growth inhibition by N epsilon-(haloacetyl)-L-lysine and N delta-(haloacetyl)-L-ornithine analogues and an acivicin analogue of methotrexate.
J Med Chem 30: 1463-9 (1987)
TBA
Benzimidazole derivatives with atypical antiinflammatory activity.
J Med Chem 30: 726-9 (1987)
TBA
Synthetic and enzyme inhibition studies of pepstatin analogues containing hydroxyethylene and ketomethylene dipeptide isosteres.
J Med Chem 30: 374-83 (1987)
TBA
Inhibition of aspartic proteinases by peptides containing lysine and ornithine side-chain analogues of statine.
J Med Chem 30: 286-95 (1987)
TBA
Folate analogues. 25. Synthesis and biological evaluation of N10-propargylfolic acid and its reduced derivatives.
J Med Chem 29: 1263-9 (1987)
TBA
Potential antiatherosclerotic agents. 5. An acyl-CoA:cholesterol O-acyltransferase inhibitor with hypocholesterolemic activity.
J Med Chem 29: 1131-3 (1987)
TBA
Synthesis and biological evaluation of irreversible inhibitors of aldose reductase.
J Med Chem 29: 2384-9 (1986)
TBA
Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids.
J Med Chem 29: 2347-51 (1986)
TBA
Synthesis of 8-amino-3-deazaguanine via imidazole precursors. Antitumor activity and inhibition of purine nucleoside phosphorylase.
J Med Chem 29: 2034-7 (1986)
TBA
Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives.
J Med Chem 29: 2024-8 (1986)
TBA
Inhibitors of human purine nucleoside phosphorylase. Synthesis, purine nucleoside phosphorylase inhibition, and T-cell cytotoxicity of 2,5-diaminothiazolo[5,4-d]pyrimidin-7(6H)-one and 2,5-diaminothiazolo[4,5-d]pyrimidin-7(6H)-one. Two thio isosteres of 8-aminoguanine.
J Med Chem 29: 1804-6 (1986)
TBA
Synthesis and antifolate properties of 5,10-methylenetetrahydro-8,10-dideazaminopterin.
J Med Chem 29: 1786-9 (1986)
TBA
Folate analogues. 26. Syntheses and antifolate activity of 10-substituted derivatives of 5,8-dideazafolic acid and of the poly-gamma-glutamyl metabolites of N10-propargyl-5,8-dideazafolic acid (PDDF).
J Med Chem 29: 1754-60 (1986)
TBA
Selective thromboxane synthetase inhibitors. 4. 2-(1H-imidazol-1-ylmethyl) carboxylic acids of benzo[b]furan, benzo[b]thiophene, indole, and naphthalene.
J Med Chem 29: 1643-50 (1986)
TBA
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
J Med Chem 29: 1429-35 (1986)
TBA
Antiinflammatory activity of substituted 6-hydroxypyrimido[2,1-f]purine-2,4,8(1H,3H,9H)-triones. Atypical nonsteroidal antiinflammatory agents.
J Med Chem 29: 1099-113 (1986)
TBA
Synthesis and rat lens aldose reductase inhibitory activity of some benzopyran-2-ones.
J Med Chem 29: 1094-9 (1986)
TBA
Inhibitors of Bacillus subtilis DNA polymerase III. Influence of modifications in the pyrimidine ring of anilino- and (benzylamino)pyrimidines.
J Med Chem 29: 676-81 (1986)
TBA
Design and synthesis of 2-(arylamino)-4(3H)-quinazolinones as novel inhibitors of rat lens aldose reductase.
J Med Chem 29: 627-9 (1986)
TBA
Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues.
J Med Chem 29: 342-6 (1986)
TBA
(beta-Chloro-alpha-aminoethyl)phosphonic acids as inhibitors of alanine racemase and D-alanine:D-alanine ligase.
J Med Chem 29: 148-51 (1986)
TBA
Interactive binding between the substrate and allosteric sites of carbamoyl-phosphate synthetase.
Biochemistry 27: 8050-6 (1988)
Pennsylvania State University
Synthesis and pharmacological characterization of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as dopamine receptor ligands.
J Med Chem 31: 1941-6 (1988)
University Of North Carolina
Renin inhibitors containing hydrophilic groups. Tetrapeptides with enhanced aqueous solubility and nanomolar potency.
J Med Chem 31: 1918-23 (1988)
Merck Sharp & Dohme Research Laboratories
Synthesis and evaluation of multisubstrate inhibitors of an oncogene-encoded tyrosine-specific protein kinase. 2.
J Med Chem 31: 1768-72 (1988)
Smith Kline & French Laboratories
Design of rat renin inhibitory peptides.
J Med Chem 31: 1679-86 (1988)
Massachusetts General Hospital
X-ray crystal structure of the opioid ligand naltrexonazine.
J Med Chem 30: 1489-94 (1987)
TBA
Synthesis and antidepressant properties of novel 2-substituted 4,5-dihydro-1H-imidazole derivatives.
J Med Chem 30: 1482-9 (1987)
TBA
Synthesis and beta-lactamase inhibitory properties of 2 beta-[(1,2,3-triazol-1-yl)methyl]-2 alpha-methylpenam-3 alpha-carboxylic acid 1,1-dioxide and related triazolyl derivatives.
J Med Chem 30: 1469-74 (1987)
TBA
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
J Med Chem 30: 1433-54 (1987)
TBA
Synthesis and cardiotonic activity of a series of substituted 4-alkyl-2(1H)-quinazolinones.
J Med Chem 30: 1421-6 (1987)
TBA
Tricyclic compounds as selective antimuscarinics. 1. Structural requirements for selectivity toward the muscarinic acetylcholine receptor in a series of pirenzepine and imipramine analogues.
J Med Chem 30: 1378-82 (1987)
TBA
Cardiotonic agents. 2. (Imidazolyl)aroylimidazolones, highly potent and selective positive inotropic agents.
J Med Chem 30: 1342-7 (1987)
TBA
Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.
J Med Chem 30: 1241-4 (1987)
TBA
Synthesis and structure-activity relationships of potent new angiotensin converting enzyme inhibitors containing saturated bicyclic amino acids.
J Med Chem 30: 992-8 (1987)
TBA
High-affinity leukotriene receptor antagonists. Synthesis and pharmacological characterization of 2-hydroxy-3-[(2-carboxyethyl)thio]-3-[2-(8-phenyloctyl)phenyl] propanoic acid.
J Med Chem 30: 959-61 (1987)
TBA
Characterization of the binding of a morphine (mu) receptor-specific ligand: Tyr-Pro-NMePhe-D-Pro-NH2, [3H]-PL17.
Mol Pharmacol 31: 326-33 (1987)
Burroughs Wellcome
Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. A new structural type of narcotic antagonists.
J Med Chem 30: 947-50 (1987)
TBA
Synthesis and biological activity of unsaturated carboacyclic purine nucleoside analogues.
J Med Chem 30: 943-7 (1987)
TBA
Leukotriene receptor antagonists. 2. The [[(tetrazol-5-ylaryl)oxy]methyl]acetophenone derivatives.
J Med Chem 30: 911-8 (1987)
TBA
1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-ethyluracil. A highly selective antiherpes simplex agent.
J Med Chem 30: 867-71 (1987)
TBA
Synthesis and pharmacological evaluation of gamma-aminobutyric acid analogues. New ligand for GABAB sites.
J Med Chem 30: 743-6 (1987)
TBA
5-Quinone derivatives of 2'-deoxyuridine 5'-phosphate: inhibition and inactivation of thymidylate synthase, antitumor cell, and antiviral studies.
J Med Chem 30: 409-19 (1987)
TBA
Inhibitors of cyclic AMP phosphodiesterase. 2. Structural variations of N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro- 2-oxoimidazo[2,1-b]quinazolin-7-yl)-oxy]butyramide (RS-82856).
J Med Chem 30: 303-18 (1987)
TBA
Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide.
J Med Chem 30: 295-303 (1987)
TBA
Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of gamma-aminobutyric acid acting as selective GABA-A antagonists.
J Med Chem 30: 239-49 (1987)
TBA
Substituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis.
J Med Chem 30: 173-8 (1987)
TBA
Structure-activity relationships of kadsurenone analogues.
J Med Chem 30: 136-42 (1987)
TBA
Spin probes as mechanistic inhibitors and active site probes of thymidylate synthetase.
J Med Chem 29: 1237-42 (1987)
TBA
Stereoselectivity of a potent calcium antagonist, 1-benzyl-3-pyrrolidinyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.
J Med Chem 29: 2504-11 (1986)
TBA
Probes for narcotic receptor mediated phenomena. 13. Potential irreversible narcotic antagonist-based ligands derived from 6,14-endo-ethenotetrahydronororipavine with 7-(methoxyfumaroyl)amino, (bromoacetyl)amino, or isothiocyanate electrophiles: chemistry, biochemistry, and pharmacology.
J Med Chem 29: 2136-41 (1986)
TBA
Synthesis and adrenergic activity of ring-fluorinated phenylephrines.
J Med Chem 29: 1982-8 (1986)
TBA
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
J Med Chem 29: 1953-61 (1986)
TBA
Conformation and activity of tetrahydrofuran lignans and analogues as specific platelet activating factor antagonists.
J Med Chem 29: 1917-21 (1986)
TBA
Irreversible blockage of opioid receptor types by ester homologues of beta-funaltrexamine.
J Med Chem 29: 1868-71 (1986)
TBA
Synthesis and biological activity of analogues of beta-chlornaltrexamine and beta-funaltrexamine at opioid receptors.
J Med Chem 29: 1861-4 (1986)
TBA
Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors.
J Med Chem 29: 1855-61 (1986)
TBA
N6-substituted N-alkyladenosine-5'-uronamides: bifunctional ligands having recognition groups for A1 and A2 adenosine receptors.
J Med Chem 29: 1683-9 (1986)
TBA
Analogues of 1,3-dipropyl-8-phenylxanthine: enhancement of selectivity at A1-adenosine receptors by aryl substituents.
J Med Chem 29: 1520-4 (1986)
TBA
Anticonvulsant activity of piperidinol and (dialkylamino)alkanol esters.
J Med Chem 29: 1512-6 (1986)
TBA
Synthesis and structure-activity relationship studies of a series of 5-aryl-4,6-dithianonanedioic acids and related compounds: a novel class of leukotriene antagonists.
J Med Chem 29: 1442-52 (1986)
TBA
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.
J Med Chem 29: 1394-8 (1986)
TBA
Pharmacological and autoradiographic discrimination of sigma and phencyclidine receptor binding sites in brain with (+)-[3H]SKF 10,047, (+)-[3H]-3-[3-hydroxyphenyl]-N-(1-propyl)piperidine and [3H]-1-[1-(2-thienyl)cyclohexyl]piperidine.
J Pharmacol Exp Ther 238: 739-48 (1986)
The Johns Hopkins University
Design of potent, orally effective, nonpeptidal antagonists of the peptide hormone cholecystokinin.
Proc Natl Acad Sci U S A 83: 4918-22 (1986)
Merck Sharp & Dohme Research Laboratories
Probes for narcotic receptor mediated phenomena. 12. cis-(+)-3-Methylfentanyl isothiocyanate, a potent site-directed acylating agent for delta opioid receptors. Synthesis, absolute configuration, and receptor enantioselectivity.
J Med Chem 29: 1087-93 (1986)
TBA
(-)-[3H] desmethoxyverapamil labels multiple calcium channel modulator receptors in brain and skeletal muscle membranes: differentiation by temperature and dihydropyridines.
J Pharmacol Exp Ther 237: 731-8 (1986)
Johns Hopkins University
Partial identity of the 2-oxoglutarate and ascorbate binding sites of prolyl 4-hydroxylase.
J Biol Chem 261: 7819-23 (1986)
University Of Oulu
Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes.
Mol Pharmacol 29: 331-46 (1986)
Warner-Lambert/Parke-Davis Pharmaceutical Research
Angiotensin-converting enzyme inhibitors: new orally active 1,4-thiazepine-2,5-diones, 1,4-thiazine-2,5-diones, and 1,4-benzothiazepine-2,5-diones possessing antihypertensive activity.
J Med Chem 29: 784-96 (1986)
TBA
Probes for narcotic receptor mediated phenomena. 9. Synthesis of (+/-)-(3 alpha,6a alpha,11a beta)-1,3,4,5,6,11a-hexahydro-2-methyl-2H-3,6a- methanobenzofuro[2,3-c]azocin-10-ol, an oxide-bridged 5-(m-hydroxyphenyl)morphan.
J Med Chem 29: 748-51 (1986)
TBA
Photoaffinity labeling of the Ah receptor.
J Biol Chem 261: 6352-65 (1986)
University Of Wisconsin
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
J Med Chem 29: 531-7 (1986)
TBA
Angiotensin converting enzyme inhibitors as antihypertensive agents: 1-[(2-mercaptocycloalkyl)carbonyl]-L-prolines.
J Med Chem 29: 411-7 (1986)
TBA
Ribose-modified adenosine analogues as adenosine receptor agonists.
J Med Chem 29: 346-53 (1986)
TBA
Conformationally restricted inhibitors of angiotensin converting enzyme: synthesis and computations.
J Med Chem 29: 251-60 (1986)
TBA
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