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Structural requirements for the binding of the pituitary adenylate-cyclase-activating peptide to receptors and adenylate-cyclase activation in pancreatic and neuronal membranes.BDB
Eur J Biochem 195: 535-41 (1991)
UniversitÉ
Synthesis and protein-tyrosine kinase inhibitory activities of flavonoid analogues.EBI
J Med Chem 34: 798-806 (1991)
Purdue University
Romazarit: a potential disease-modifying antirheumatic drug.EBI
J Med Chem 34: 772-7 (1991)
Roche Products
Synthesis of 3-carbamoylecgonine methyl ester analogues as inhibitors of cocaine binding and dopamine uptake.EBI
J Med Chem 34: 702-5 (1991)
University Of Maryland
Muscarinic cholinergic agonists and antagonists of the 3-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,2,5,6-tetrahydropyridine type. Synthesis and structure-activity relationships.EBI
J Med Chem 34: 687-92 (1991)
Ferrosan
Configuration and preferential solid-state conformations of perindoprilat (S-9780). Comparison with the crystal structures of other ACE inhibitors and conclusions related to structure-activity relationships.EBI
J Med Chem 34: 663-9 (1991)
Institut De Chimie Des Substances Naturelles
4',5'-unsaturated 5'-halogenated nucleosides. Mechanism-based and competitive inhibitors of S-adenosyl-L-homocysteine hydrolase.EBI
J Med Chem 34: 647-56 (1991)
Merrell Dow Research Institute
Renin inhibitory peptides. Incorporation of polar, hydrophilic end groups into an active renin inhibitory peptide template and their evaluation in a human renin infused rat model and in conscious sodium-depleted monkeys.EBI
J Med Chem 34: 633-42 (1991)
Upjohn
Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase.EBI
J Med Chem 34: 624-8 (1991)
Pfizer
Novel benzamides as selective and potent gastrokinetic agents. 2. Synthesis and structure-activity relationships of 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2- morpholinyl]methyl] benzamide citrate (AS-4370) and related compounds.EBI
J Med Chem 34: 616-24 (1991)
Dainippon Pharmaceutical
Synthesis and biological activity of 5,11-methylenetetrahydro-5- deazahomofolic acid.EBI
J Med Chem 34: 611-6 (1991)
Duquesne University
Synthesis and biological activity of methotrexate analogues with two acid groups and a hydrophobic aromatic ring in the side chain.EBI
J Med Chem 34: 574-9 (1991)
Harvard Medical School
Molecular and crystal structures of MDL27,467A hydrochloride and quinapril hydrochloride, two ester derivatives of potent angiotensin converting enzyme inhibitors.EBI
J Med Chem 34: 511-7 (1991)
University Of Calgary
A 3-D model for 5-HT1A-receptor agonists based on stereoselective methyl-substituted and conformationally restricted analogues of 8-hydroxy-2-(dipropylamino)tetralin.EBI
J Med Chem 34: 497-510 (1991)
Uppsala University
The renewed potential for folate antagonists in contemporary cancer chemotherapy.EBI
J Med Chem 34: 479-85 (1991)
Parke-Davis Pharmaceutical Research Division
Antagonist binding profiles of five cloned human muscarinic receptor subtypes.BDB
J Pharmacol Exp Ther 256: 727-33 (1991)
National Institute Of Neurological Disorders And Stroke
Design of potent protein kinase inhibitors using the bisubstrate approach.EBI
J Med Chem 34: 73-8 (1991)
Ura Cnrs 1309
Design of a well-absorbed renin inhibitor.EBI
J Med Chem 34: 469-71 (1991)
Abbott Laboratories
8-(Dicyclopropylmethyl)-1,3-dipropylxanthine: a potent and selective adenosine A1 antagonist with renal protective and diuretic activities.EBI
J Med Chem 34: 466-9 (1991)
Kyowa Hakko Kogyo
Relationship between tissue selectivity and lipophilicity for inhibitors of HMG-CoA reductase.EBI
J Med Chem 34: 463-6 (1991)
Warner-Lambert
trans-3-n-propyl-L-proline is a highly favorable, conformationally restricted replacement for methionine in the C-terminal tetrapeptide of cholecystokinin. Stereoselective synthesis of 3-allyl- and 3-n-propyl-L-proline derivatives from 4-hydroxy-L-proline.EBI
J Med Chem 34: 455-7 (1991)
Abbott Laboratories
Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats.EBI
J Med Chem 34: 439-47 (1991)
Research And Development Laboratories
Disubstituted tetrahydrofurans and dioxolanes and PAF antagonists.EBI
J Med Chem 34: 373-86 (1991)
J. Uriach & CíA.
Inhibitors of cholesterol biosynthesis. 4. trans-6-[2-(substituted-quinolinyl)ethenyl/ethyl]tetrahydro-4-hydroxy-2 H-pyran-2-ones, a novel series of HMG-CoA reductase inhibitors.EBI
J Med Chem 34: 367-73 (1991)
Warner-Lambert
Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl)ethyl]-2H-pyran-2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing substituents at positions three and four of the pyrrole nucleus.EBI
J Med Chem 34: 357-66 (1991)
Warner-Lambert
Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl]-2-imidazolidinones.EBI
J Med Chem 34: 291-8 (1991)
Pfizer
2,3-Dihydrobenzofuran analogues of hallucinogenic phenethylamines.EBI
J Med Chem 34: 276-81 (1991)
Purdue University
Dual inhibitors of thromboxane A2 synthase and 5-lipoxygenase with scavenging activity of active oxygen species. Synthesis of a novel series of (3-pyridylmethyl)benzoquinone derivatives.EBI
J Med Chem 34: 267-76 (1991)
Takeda Chemical Industries
Synthesis and biological activity of the 2-desamino and 2-desamino-2-methyl analogues of aminopterin and methotrexate.EBI
J Med Chem 34: 227-34 (1991)
Institute
Folate analogues. 34. Synthesis and antitumor activity of non-polyglutamylatable inhibitors of dihydrofolate reductase.EBI
J Med Chem 34: 222-7 (1991)
University Of South Alabama
Analogues of methotrexate and aminopterin with gamma-methylene and gamma-cyano substitution of the glutamate side chain: synthesis and in vitro biological activity.EBI
J Med Chem 34: 203-8 (1991)
Institute
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 3.1 Synthesis and biological properties of aminodeoxystatine and difluorostatone derivatives.EBI
J Med Chem 34: 151-7 (1991)
Ici Pharmaceuticals Group
Novel 5-HT3 antagonists. Indole oxadiazoles.EBI
J Med Chem 34: 140-51 (1991)
Merck Sharp And Dohme Research Laboratories
In vitro pharmacological profile of a novel structural class of oxytocin antagonists.BDB
J Pharmacol Exp Ther 256: 304-8 (1991)
Merck Sharp & Dohme Research Laboratories
[3H]cytisine binding to nicotinic cholinergic receptors in brain.BDB
Mol Pharmacol 39: 9-12 (1991)
Georgetown University
Neurochemical profile of eltoprazine.BDB
Drug Metabol Drug Interact 8: 85-114 (1990)
Duphar
Potent anticonflict activity and lessening of memory impairment with a series of novel [1]benzothieno[2,3-c]pyridines and 1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines.EBI
J Med Chem 33: 3110-6 (1990)
Asahi Chemical Industry
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.EBI
J Med Chem 33: 2961-3 (1990)
Merrell Dow Research Institute
(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist.EBI
J Med Chem 33: 2948-50 (1990)
Abbott Laboratories
2-Phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives: synthesis and antidepressant activity.EBI
J Med Chem 33: 2899-905 (1990)
Wyeth-Ayerst Research
Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity.EBI
J Med Chem 33: 2883-91 (1990)
Berlex Laboratories
Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.BDB
Nature 347: 146-51 (1990)
U. 109
Synthesis and structure-activity relationships of N,N'-di-o-tolylguanidine analogues, high-affinity ligands for the haloperidol-sensitive sigma receptor.EBI
J Med Chem 33: 2421-9 (1990)
University Of Oregon
Synthesis and dopamine receptor affinities of 2-(4-fluoro-3- hydroxyphenyl)ethylamine and N-substituted derivatives.EBI
J Med Chem 33: 2408-12 (1990)
University Of Camerino
Potential antipsychotic agents. 7. Synthesis and antidopaminergic properties of the atypical highly potent (S)-5-bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide and related compounds. A comparative study.EBI
J Med Chem 33: 2305-9 (1990)
Astra Research Centre
Conformational analysis and structure-activity relationships of selective dopamine D-1 receptor agonists and antagonists of the benzazepine series.EBI
J Med Chem 33: 2197-204 (1990)
Royal Danish School Of Pharmacy
Design and synthesis of highly potent and selective cyclic dynorphin A analogues.EBI
J Med Chem 33: 1874-9 (1990)
University Of Arizona
Synthesis and dopamine receptor affinities of enantiomers of 2-substituted apomorphines and their N-n-propyl analogues.EBI
J Med Chem 33: 1800-5 (1990)
Northeastern University
trans-10,11-dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine: a highly potent selective dopamine D1 full agonist.EBI
J Med Chem 33: 1756-64 (1990)
Purdue University
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.EBI
J Med Chem 33: 1155-63 (1990)
Astra Research Centre
Dehydrogenase binding by tiazofurin anabolites.EBI
J Med Chem 33: 1123-7 (1990)
University Of Rochester Medical Center
Characteristics of 125I-iodocyanopindolol binding to beta-adrenergic and serotonin-1B receptors of rat brain: selectivity of beta-adrenergic agents.BDB
Jpn J Pharmacol 52: 195-200 (1990)
Niigata College Of Pharmacy
Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model.EBI
J Med Chem 33: 1015-22 (1990)
University Of Lund
Synthesis and immunosuppressive activity of some side-chain variants of mycophenolic acid.EBI
J Med Chem 33: 833-8 (1990)
Syntex Research
Analogues of carbamyl aspartate as inhibitors of dihydroorotase: preparation of boronic acid transition-state analogues and a zinc chelator carbamylhomocysteine.EBI
J Med Chem 33: 819-23 (1990)
Mayo Clinic
Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.EBI
J Med Chem 33: 809-14 (1990)
Vanderbilt University
Nonneurotoxic tetralin and indan analogues of 3,4-(methylenedioxy)amphetamine (MDA).EBI
J Med Chem 33: 703-10 (1990)
Purdue University
Synthesis and dopamine agonist properties of (+-)-trans-3,4,4a,10b-tetrahydro-4-propyl-2H,5H-[1]benzopyrano [4,3-b]-1,4-oxazin-9-ol and its enantiomers.EBI
J Med Chem 33: 445-50 (1990)
Warner-Lambert
Histamine H3 ligands: just pharmacological tools or potential therapeutic agents?EBI
J Med Chem 33: 4-11 (1990)
Vrije Universiteit
4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties.EBI
J Med Chem 33: 311-7 (1990)
Warner-Lambert
Synthesis and beta-adrenergic antagonist activity of stereoisomeric practolol and propranolol derivatives.EBI
J Med Chem 33: 216-23 (1990)
University Of California
Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues.EBI
J Med Chem 33: 206-12 (1990)
Eisai
NMDA receptor agonists derived from ibotenic acid. Preparation, neuroexcitation and neurotoxicity.BDB
Eur J Pharmacol 189: 381-91 (1990)
Royal Danish School Of Pharmacy
Novel binding mode of highly potent HIV-proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere.EBI
J Med Chem 34: 3340-2 (1991)
Roche Products
Gossypol and derivatives: a new class of aldose reductase inhibitors.EBI
J Med Chem 34: 3301-5 (1991)
University Of New Mexico School Of Medicine
Substrate analogue renin inhibitors containing replacements of histidine in P2 or isosteres of the amide bond between P3 and P2 sites.EBI
J Med Chem 34: 3267-80 (1991)
E. Merck Darmstadt
Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype.EBI
J Med Chem 34: 3248-60 (1991)
Warner-Lambert
Fluorescent probes for dopamine receptors: synthesis and characterization of fluorescein and 7-nitrobenz-2-oxa-1,3-diazol-4-yl conjugates of D-1 and D-2 receptor ligands.EBI
J Med Chem 34: 3235-41 (1991)
Research Biochemicals
Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors.EBI
J Med Chem 34: 3229-34 (1991)
Alcon Laboratories
(Aminoalkyl)carbamates of forskolin: intermediates for the synthesis of functionalized derivatives of forskolin with different specificities for adenylyl cyclase and the glucose transporter.EBI
J Med Chem 34: 3204-12 (1991)
Food And Drug Administration
Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues.EBI
J Med Chem 34: 3164-71 (1991)
Research Triangle Institute
Bisbenzylisoquinoline AlkaloidsEBI
J Nat Prod 54: 645-749 (1991)
TBA
Affinities of fluoxetine, its enantiomers, and other inhibitors of serotonin uptake for subtypes of serotonin receptors.BDB
Neuropsychopharmacology 5: 43-7 (1991)
Eli Lilly
[123I]-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane: high-affinity SPECT radiotracer of monoamine reuptake sites in brain.EBI
J Med Chem 34: 3144-6 (1991)
Research Biochemicals
Development of a small RGD peptide fibrinogen receptor antagonist with potent antiaggregatory activity in vitro.EBI
J Med Chem 34: 3114-25 (1991)
Smithkline Beecham Pharmaceuticals Research And Development
Nonpeptidic angiotensin II antagonists: synthesis and in vitro activity of a series of novel naphthalene and tetrahydronaphthalene derivatives.EBI
J Med Chem 34: 3105-14 (1991)
Ciba-Geigy
Muscarinic receptor binding profile of para-substituted caramiphen analogues.EBI
J Med Chem 34: 2984-9 (1991)
Virginia Commonwealth University
Interphenylene 7-oxabicyclo[2.2.1]heptane thromboxane A2 antagonists. Semicarbazone omega-chains.EBI
J Med Chem 34: 2882-91 (1991)
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679.BDB
J Med Chem 34: 2852-7 (1991)
Merck Sharp And Dohme Research Laboratories
Rational design of quinazoline-based irreversible inhibitors of human erythrocyte purine nucleoside phosphorylase.BDB
Biochemistry 30: 8480-7 (1991)
Arizona State University
Targeting 5'-deoxy-5'-(methylthio)adenosine phosphorylase by 5'-haloalkyl analogues of 5'-deoxy-5'-(methylthio)adenosine.EBI
J Med Chem 34: 2600-6 (1991)
Institute
Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.EBI
J Med Chem 34: 2504-20 (1991)
Wyeth-Ayerst Research
Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists.EBI
J Med Chem 34: 2477-83 (1991)
Centre De Recherches De Vitry Alfortville Rh£Ne-Poulenc Rorer
Relative structure-inhibition analyses of the N-benzoyl and N-(phenylsulfonyl) amino acid aldose reductase inhibitors.EBI
J Med Chem 34: 2120-6 (1991)
Auburn University
5-Lipoxygenase inhibitors: the synthesis and structure-activity relationships of a series of 1-phenyl-3-pyrazolidinones.EBI
J Med Chem 34: 1560-70 (1991)
Sterling Research Group
Quinazolineacetic acids and related analogues as aldose reductase inhibitors.EBI
J Med Chem 34: 1492-503 (1991)
Wyeth-Ayerst Research
New inhibitors of human renin that contain novel replacements at the P2 site.EBI
J Med Chem 34: 1258-71 (1991)
Warner-Lambert
Antinociceptive (aminoalkyl)indoles.EBI
J Med Chem 34: 1099-110 (1991)
Sterling Research Group
A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate, and its congeners.EBI
J Med Chem 34: 1011-8 (1991)
Pfizer
On the optimization of hydrophobic and hydrophilic substituent interactions of 2,4-diamino-5-(substituted-benzyl)pyrimidines with dihydrofolate reductase.EBI
J Med Chem 34: 46-54 (1991)
Pomona College
Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners.EBI
J Med Chem 34: 108-22 (1991)
Pfizer
A selective, reversible, competitive inhibitor of monoamine oxidase A containing no nitrogen, with negligible potentiation of tyramine-induced blood pressure rise.EBI
J Med Chem 34: 2931-3 (1991)
Burroughs Wellcome
Substituted 2-(aminomethyl)piperidines: a novel class of selective protein kinase C inhibitors.EBI
J Med Chem 34: 2928-31 (1991)
Nova Pharmaceutical
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.EBI
J Med Chem 34: 2919-22 (1991)
Exploratory Chemistry Merck Sharp And Dohme Research Laboratories
Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogues of 1-methylisoguanosine.EBI
J Med Chem 34: 2892-8 (1991)
Griffith University
N6,9-disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor.EBI
J Med Chem 34: 2877-82 (1991)
University Of South Florida
Modification of the enkephalin"message" with an artificial polycationic C-terminus.EBI
J Med Chem 34: 2816-21 (1991)
Case Western Reserve University
Comparison of azabicyclic esters and oxadiazoles as ligands for the muscarinic receptor.EBI
J Med Chem 34: 2726-35 (1991)
Smithkline Beecham Pharmaceuticals
Synthesis, ligand binding, QSAR, and CoMFA study of 3 beta-(p-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters.EBI
J Med Chem 34: 2719-25 (1991)
Research Triangle Institute
Design and synthesis of P2-P1'-linked macrocyclic human renin inhibitors.EBI
J Med Chem 34: 2692-701 (1991)
Merck Sharp And Dohme Research Laboratories
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.EBI
J Med Chem 34: 2685-91 (1991)
UniversitäT Des Saarlandes
Acyclic analogues of 2-(4-phenylpiperidino)cyclohexanol (vesamicol): conformationally mobile inhibitors of vesicular acetylcholine transport.EBI
J Med Chem 34: 2638-43 (1991)
University Of Minnesota
Synthesis, stereochemistry, and biological activity of the 1-(1-phenyl-2-methylcyclohexyl)piperidines and the 1-(1-phenyl-4-methylcyclohexyl)piperidines. Absolute configuration of the potent trans-(-)-1-(1-phenyl-2-methylcyclohexyl)piperidine.EBI
J Med Chem 34: 2615-23 (1991)
Istituto Superiore Di Sanità
Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization.EBI
J Med Chem 34: 2579-88 (1991)
Purdue University
Highly selective adenosine A2 receptor agonists in a series of N-alkylated 2-aminoadenosines.EBI
J Med Chem 34: 2570-9 (1991)
Ciba-Geigy
Nonpeptide angiotensin II receptor antagonists: the discovery of a series of N-(biphenylylmethyl)imidazoles as potent, orally active antihypertensives.EBI
J Med Chem 34: 2525-47 (1991)
E. I. Du Pont De Nemours
Synthesis and biochemical studies of 16- or 19-substituted androst-4-enes as aromatase inhibitors.EBI
J Med Chem 34: 2496-504 (1991)
Tohoku College Of Pharmacy
3-Hydroxy-3-methylglutaryl-coenzyme a reductase inhibitors. 7. Modification of the hexahydronaphthalene moiety of simvastatin: 5-oxygenated and 5-oxa derivatives.EBI
J Med Chem 34: 2489-95 (1991)
Merck Sharp & Dohme Research Laboratories
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 8. Side chain ether analogues of lovastatin.EBI
J Med Chem 34: 2474-7 (1991)
Merck Sharp & Dohme Research Laboratories
Synthesis and evaluation of antiinflammatory activities of a series of corticosteroid 17 alpha-esters containing a functional group.EBI
J Med Chem 34: 2468-73 (1991)
Mitsubishi Kasei
Conformationally restricted polysubstituted biphenyl derivatives with angiotensin II receptors antagonist properties.EBI
J Med Chem 34: 2410-4 (1991)
Searle R & D And Mcr
Synthesis and biological activity of angiotensin II analogues containing a Val-His replacement, Val psi[CH(CONH2)NH]His.EBI
J Med Chem 34: 2402-10 (1991)
Berlex Laboratories
Inhibitors of the protease from human immunodeficiency virus: design and modeling of a compound containing a dihydroxyethylene isostere insert with high binding affinity and effective antiviral activity.EBI
J Med Chem 34: 2344-56 (1991)
Upjohn
Cholinergic activity of acetylenic imidazoles and related compounds.EBI
J Med Chem 34: 2314-27 (1991)
Upjohn
HIV protease: a novel chemotherapeutic target for AIDS.EBI
J Med Chem 34: 2305-14 (1991)
Merck Sharp And Dohme Research Laboratories
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.BDB
J Biol Chem 266: 15771-81 (1991)
Laboratoires Glaxo
Role of the four conserved histidine residues in the amidotransferase domain of carbamoyl phosphate synthetase.BDB
Biochemistry 30: 7901-7 (1991)
Texas A&M University
Cloning and expression of an A1 adenosine receptor from rat brain.BDB
Mol Pharmacol 40: 1-7 (1991)
National Institute Of Mental Health
Imidazo[4,5-b]quinoxaline cyanines as neurokinin antagonists.EBI
J Med Chem 34: 1751-3 (1991)
Rochester
Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.EBI
J Med Chem 34: 1715-20 (1991)
University Of Minnesota
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity.EBI
J Med Chem 34: 1704-7 (1991)
Rhone-Poulenc Rorer Central Research
Synthesis and structure-activity relationships of deltorphin analogues.EBI
J Med Chem 34: 1656-61 (1991)
University Of Ferrara
Function of negative charge in the"address domain" of deltorphins.EBI
J Med Chem 34: 1350-5 (1991)
National Institute Of Environmental Health Sciences
Synthesis and biochemical evaluation of baclofen analogues locked in the baclofen solid-state conformation.EBI
J Med Chem 34: 1307-13 (1991)
Centre De Neurochimie Du Cnrs
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.EBI
J Med Chem 34: 1292-6 (1991)
University Of Minnesota
Peptide leukotrienes: current status of research.EBI
J Med Chem 34: 1235-42 (1991)
Ici Pharmaceuticals Group
gamma-Aminobutyric acidA receptor heterogeneity in rat central nervous system: studies with clonazepam and other benzodiazepine ligands.BDB
J Pharmacol Exp Ther 256: 1154-60 (1991)
Georgetown University
Identification and exploitation of the sigma-opiate pharmacophore.EBI
J Med Chem 34: 1094-8 (1991)
Virginia Commonwealth University
Studies on (H(+)-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl)sulfinyl]benzimidazole proton-pump inhibitors.EBI
J Med Chem 34: 1049-62 (1991)
Upjohn
Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.EBI
J Med Chem 34: 1028-36 (1991)
Ici Pharmaceuticals Group
New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics.EBI
J Med Chem 34: 827-41 (1991)
Anaquest
Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.EBI
J Med Chem 34: 518-25 (1991)
Warner-Lambert
(2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics.EBI
J Med Chem 34: 397-403 (1991)
Zambeletti Research Laboratories
Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity.EBI
J Med Chem 34: 190-4 (1991)
Parke-Davis Research Unit
2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid kappa agonists.EBI
J Med Chem 34: 181-9 (1991)
Ici Pharmaceuticals Group
Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine.BDB
Nature 350: 610-4 (1991)
University Of Toronto
Molecular cloning and characterization of a rat brain cDNA encoding a 5-hydroxytryptamine1B receptor.BDB
EMBO J 10: 4017-23 (1991)
University Of Heidelberg
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands.EBI
J Med Chem 34: 2946-53 (1991)
Abbott Laboratories
Cloning, molecular characterization, and chromosomal assignment of a gene encoding a second D1 dopamine receptor subtype: differential expression pattern in rat brain compared with the D1A receptor.BDB
Proc Natl Acad Sci U S A 88: 7491-5 (1991)
Duke University
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 1. (+/-)-(3-pyridinylbicycloheptyl)alkanoic acids.EBI
J Med Chem 34: 1790-7 (1991)
Ciba-Geigy
Characterization and distribution of [125I]epidepride binding to dopamine D2 receptors in basal ganglia and cortex of human brain.BDB
J Pharmacol Exp Ther 257: 1253-63 (1991)
University Of Pennsylvania
Synthesis and in vitro evaluation of 2,3-dimethoxy-5-(fluoroalkyl)-substituted benzamides: high-affinity ligands for CNS dopamine D2 receptors.EBI
J Med Chem 34: 1612-24 (1991)
University Of California
Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.BDB
Nature 350: 614-9 (1991)
University Of Toronto
Novel synthesis and biochemical properties of an [125I]-labeled photoaffinity probe for thromboxane A2/prostaglandin H2 receptors.EBI
J Med Chem 34: 1511-4 (1991)
Eli Lilly
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.EBI
J Med Chem 34: 725-36 (1991)
Ciba-Geigy
Nicotinamide ethers: novel inhibitors of calcium-independent phosphodiesterase and [3H]rolipram binding.EBI
J Med Chem 34: 86-9 (1991)
Pfizer
Antidopaminergic effects of the stereoisomers of N-[(1-alkyl-2- pyrrolidinyl)methyl]-5-sulfamoylbenzamides and -2,3-dihydrobenzofuran-7-carboxamides.EBI
J Med Chem 34: 261-7 (1991)
Yoshitomi Pharmaceutical Industries
Verbascoside isolated from Lantana camara, an inhibitor of protein kinase C.EBI
J Nat Prod 54: 1595-600
Sanofi Recherche
Methylpendolmycin, an indolactam from a Nocardiopsis sp.EBI
J Nat Prod 54: 1440-3
Sterling Research Group
Delineating the pharmacophoric elements of huperzine A: importance of the unsaturated three-carbon bridge to its AChE inhibitory activity.EBI
J Med Chem 34: 3399-402 (1992)
Mayo Clinic
Examination of HIV-1 protease secondary structure specificity using conformationally constrained inhibitors.EBI
J Med Chem 34: 3395-9 (1992)
University Of Illinois
Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors.EBI
J Med Chem 34: 3388-90 (1992)
University Of South Florida
Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors.EBI
J Med Chem 34: 3350-9 (1992)
Abbott Laboratories
A novel class of enkephalinase inhibitors containing a C-terminal sulfo group.EBI
J Med Chem 35: 602-8 (1992)
Dainippon Pharmaceutical
Conformational analyses and molecular-shape comparisons of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase.EBI
J Med Chem 35: 590-601 (1992)
University Of Illinois
QSAR analyses of the substituted indanone and benzylpiperidine rings of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase.EBI
J Med Chem 35: 584-9 (1992)
University Of Illinois
Renin inhibitory pentols showing improved enteral bioavailability.EBI
J Med Chem 35: 559-67 (1992)
Hoechst
Potent, orally active aldose reductase inhibitors related to zopolrestat: surrogates for benzothiazole side chain.EBI
J Med Chem 35: 457-65 (1992)
Pfizer
alpha-Keto amide inhibitors of aminopeptidases.EBI
J Med Chem 35: 451-6 (1992)
University Of Wisconsin-Madison
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.EBI
J Med Chem 35: 407-22 (1992)
Niddk
Characterization of 5-hydroxytryptamine1B receptors in rat spinal cord via [125I]iodocyanopindolol binding and inhibition of [3H]-5-hydroxytryptamine release.BDB
J Pharmacol Exp Ther 260: 614-26 (1992)
University Of Texas
Improvements in the minimum binding sequence of C5a: examination of His-67.EBI
J Med Chem 35: 402-6 (1992)
Abbott Laboratories
Synthesis and antifolate evaluation of the 10-propargyl derivatives of 5-deazafolic acid, 5-deazaaminopterin, and 5-methyl-5-deazaaminopterin.EBI
J Med Chem 35: 332-7 (1992)
Southern Research Institute
New neplanocin analogues. 1. Synthesis of 6'-modified neplanocin A derivatives as broad-spectrum antiviral agents.EBI
J Med Chem 35: 324-31 (1992)
Toyo Jozo
Synthesis and antifolate properties of 5,10-ethano-5,10-dideazaaminopterin.EBI
J Med Chem 35: 320-4 (1992)
Sri International
Phenyl-substituted analogues of oxotremorine as muscarinic antagonists.EBI
J Med Chem 35: 285-94 (1992)
University Of Uppsala
Nucleosides and nucleotides. 103. 2-Alkynyladenosines: a novel class of selective adenosine A2 receptor agonists with potent antihypertensive effects.EBI
J Med Chem 35: 241-52 (1992)
Hokkaido University
Structure-function studies in a series of carboxyl-terminal octapeptide analogues of anaphylatoxin C5a.EBI
J Med Chem 35: 220-3 (1992)
Abbott Laboratories
Stereoselective LSD-like activity in d-lysergic acid amides of (R)- and (S)-2-aminobutane.EBI
J Med Chem 35: 203-11 (1992)
Purdue University
Total synthesis of uracil analogues of sinefungin.EBI
J Med Chem 35: 63-7 (1992)
Cnrs
Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.EBI
J Med Chem 35: 28-38 (1992)
Rotta Research Laboratorium
Design and synthesis of potent, selective, and orally active fluorine-containing renin inhibitors.EBI
J Med Chem 35: 2-14 (1992)
Warner-Lambert
Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides.BDB
J Med Chem 35: 177-84 (1992)
Roche Products
Heteroatom analogues of bemoradan: chemistry and cardiotonic activity of 1,4-benzothiazinylpyridazinones.EBI
J Med Chem 35: 172-6 (1992)
R. W. Johnson Pharmaceutical Research Institute
Preparation and biological activities of potential vasopressin photoaffinity labels.EBI
J Med Chem 35: 151-7 (1992)
University Of Sherbrooke
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.EBI
J Med Chem 35: 15-27 (1992)
Sandoz Pharma
N-modified analogues of cocaine: synthesis and inhibition of binding to the cocaine receptor.EBI
J Med Chem 35: 141-4 (1992)
Research Triangle Institute
2 beta-substituted analogues of cocaine. Synthesis and inhibition of binding to the cocaine receptor.EBI
J Med Chem 35: 135-40 (1992)
Research Triangle Institute
Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor.EBI
J Med Chem 35: 124-35 (1992)
Sterling Research Group
Synthesis, specificity, and antifungal activity of inhibitors of the Candida albicans delta 24-sterol methyltransferase.EBI
J Med Chem 35: 100-6 (1992)
Smithkline Beecham Pharmaceuticals
Reversal of enzyme regiospecificity with alternative substrates for aspartokinase I from Escherichia coli.BDB
Biochemistry 31: 799-805 (1992)
University Of Akron
Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes.EBI
J Med Chem 34: 3305-9 (1991)
Veterans Affairs Medical Center
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.BDB
J Med Chem 34: 2922-5 (1991)
Merck Sharp And Dohme Research Laboratories
Boc-CCK-4 derivatives containing side-chain ureas as potent and selective CCK-a receptor agonists.EBI
J Med Chem 34: 2837-42 (1991)
Abbott Laboratories
Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity.EBI
J Med Chem 34: 2430-8 (1991)
Hebrew University Of Jerusalem
Novel gonadotropin-releasing hormone antagonists: peptides incorporating modified N omega-cyanoguanidino moieties.EBI
J Med Chem 34: 2395-402 (1991)
Salk Institute
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.BDB
J Med Chem 34: 2231-41 (1991)
Boehringer Ingelheim Pharmaceuticals
Evaluation of natural products as inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase.EBI
J Nat Prod 54: 143-54
University Of Illinois
Molecular cloning and expression of the cDNA for the alpha 1A-adrenergic receptor. The gene for which is located on human chromosome 5.BDB
J Biol Chem 266: 6365-9 (1991)
Duke University
Characterization of two novel cholecystokinin tetrapeptide (30-33) analogues, A-71623 and A-70874, that exhibit high potency and selectivity for cholecystokinin-A receptors.BDB
Mol Pharmacol 39: 346-51 (1991)
Abbott Laboratories
Differential Inhibition of Reverse Transcriptase and Various DNA Polymerases by Digallic Acid and Its DerivativesEBI
J Nat Prod 53: 1234-1240 (1990)
TBA
Pharmacologic comparison of selected agonists for the M1 muscarinic receptor in transfected murine fibroblast cells (B82).BDB
J Pharmacol Exp Ther 256: 689-94 (1991)
University Of Arizona
Boc-Trp-Orn(Z)-Asp-NH2 and derivatives: a new family of CCK antagonists.EBI
J Med Chem 33: 3199-204 (1991)
University Of Paris
Development of CCK-tetrapeptide analogues as potent and selective CCK-A receptor agonists.EBI
J Med Chem 33: 2950-2 (1990)
Abbott Laboratories
5'-O-phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity.EBI
J Med Chem 33: 2481-7 (1990)
Institute For Medical Research
Synthesis of a new class of 2,3-dihydro-2-oxo-1H-benzimidazole-1-carboxylic acid derivatives as highly potent 5-HT3 receptor antagonists.EBI
J Med Chem 33: 2101-8 (1990)
Istituto De Angeli
Structure-activity relationships of 8-cycloalkyl-1,3-dipropylxanthines as antagonists of adenosine receptors.EBI
J Med Chem 33: 1906-10 (1990)
Vanderbilt University
Potent and highly selective neurokinin antagonists.EBI
J Med Chem 33: 1848-51 (1990)
Glaxo Group Research
(+/-)-3-Allyl-6-bromo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3- benzazepin, a new high-affinity D1 dopamine receptor ligand: synthesis and structure-activity relationship.EBI
J Med Chem 34: 3366-71 (1992)
Northeastern University
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.EBI
J Med Chem 34: 3316-28 (1991)
Bristol-Myers Squibb Pharmaceutical Research Institute
Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.EBI
J Med Chem 34: 3085-90 (1991)
Pfizer
Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine.EBI
J Med Chem 34: 2736-46 (1991)
Warner-Lambert
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone.EBI
J Med Chem 34: 2242-7 (1991)
University Of Santiago De Compostela
Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists.EBI
J Med Chem 34: 2023-30 (1991)
H. Lundbeck
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.BDB
J Med Chem 34: 1896-907 (1991)
Hebrew University Of Jerusalem
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents.EBI
J Med Chem 34: 1860-6 (1991)
Pfizer
Structure/activity and molecular modeling studies of the lophotoxin family of irreversible nicotinic receptor antagonists.EBI
J Med Chem 34: 1798-804 (1991)
University Of California San Diego
Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity.EBI
J Med Chem 34: 1707-14 (1991)
Harvard Medical School
Optical isomers of rocastine and close analogues: synthesis and H1 antihistaminic activity of its enantiomers and their structural relationship to the classical antihistamines.EBI
J Med Chem 34: 1314-28 (1991)
A.H. Robins
Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congeners.EBI
J Med Chem 34: 948-55 (1991)
Astra Research Centre
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.EBI
J Med Chem 34: 1068-72 (1991)
Hoechst-Roussel Pharmaceuticals
Effect of fluorine substitution on the adrenergic properties of 3-(tert-butylamino)-1-(3,4-dihydroxyphenoxy)-2-propanol.EBI
J Med Chem 34: 1063-8 (1991)
National Institute Of Diabetes
Structure-affinity relationships of 12-sulfonyl derivatives of 5,8,8a,9,10,11,12,12a,13,13a-decahydro-6H-isoquino[2,1-g][1 ,6] naphthyridines at alpha-adrenoceptors.EBI
J Med Chem 34: 705-17 (1991)
Syntex Research
Dual antagonists of platelet activating factor and histamine. Identification of structural requirements for dual activity of N-Acyl-4-(5,6-dihydro-11H-benzo [5,6]cyclohepta-[1,2-b]pyridin-11-ylidene)piperidines.EBI
J Med Chem 34: 457-61 (1991)
Schering-Plough
Rationally designed"dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.EBI
J Med Chem 34: 404-14 (1991)
Parke-Davis Research Unit
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones.EBI
J Med Chem 34: 248-56 (1991)
Warner-Lambert
R and S enantiomers of 11-hydroxy- and 10,11-dihydroxy-N-allylnoraporphine: synthesis and affinity for dopamine receptors in rat brain tissue.EBI
J Med Chem 34: 24-8 (1991)
Northeastern University
Common stereospecificity of opioid and dopamine systems for N-butyrophenone prodine-like compounds.EBI
J Med Chem 34: 194-7 (1991)
Istituto Superiore Di Sanità
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.EBI
J Med Chem 34: 3360-5 (1992)
Virginia Commonwealth University
Characterization of a guanosine-nucleotide-binding-protein-coupled receptor for pituitary adenylate-cyclase-activating polypeptide on plasma membranes from rat brain.BDB
Eur J Biochem 202: 951-8 (1991)
Georg-August-University
Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the Na+/H+ exchanger, but indicate a common structure on receptor proteins.BDB
J Recept Res 11: 891-907 (1991)
Center For Bio-Pharmaceutical Sciences
Synthesis and pharmacological evaluation of ether and related analogues of delta 8-, delta 9-, and delta 9,11-tetrahydrocannabinol.EBI
J Med Chem 34: 3310-6 (1991)
Virginia Commonwealth University
Structure/activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]acetamides: a novel series of potent and selective kappa-opioid agonists.EBI
J Med Chem 34: 3149-58 (1991)
Ici Pharmaceuticals Group
Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity.EBI
J Med Chem 34: 3125-32 (1991)
Clinical Research Institute Of Montreal
Synthesis and receptor binding of enantiomeric N-substituted cis-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexylamines as high-affinity sigma receptor ligands.EBI
J Med Chem 34: 3058-65 (1991)
National Institute Of Diabetes And Digestive And Kidney Diseases
New 5H-pyridazino[4,5-b]indole derivatives. Synthesis and studies as inhibitors of blood platelet aggregation and inotropics.EBI
J Med Chem 34: 3023-9 (1991)
Universidad De Navarra
Synthesis and biological activity of new HMG-CoA reductase inhibitors. 3. Lactones of 6-phenoxy-3,5-dihydroxyhexanoic acids.EBI
J Med Chem 34: 2962-83 (1991)
Hoechst
Characterization of the alpha-2C adrenergic receptor subtype in the opossum kidney and in the OK cell line.BDB
J Pharmacol Exp Ther 259: 323-9 (1991)
University Of Nebraska
Peripheral-type benzodiazepine receptors in human cerebral cortex, kidney, and colon.BDB
Life Sci 49: 1155-61 (1991)
Technion-Israel Institute Of Technology
1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.EBI
J Med Chem 34: 2906-16 (1991)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of 4-purinylpyrrolidine nucleosides.EBI
J Med Chem 34: 2787-97 (1991)
University Of Minnesota
Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.BDB
Mol Pharmacol 40: 143-8 (1991)
Seattle Veterans Affairs Medical Center
Analogues of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced alpha 1-adrenergic affinity.EBI
J Med Chem 34: 2633-8 (1991)
Virginia Commonwealth University
(1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics.EBI
J Med Chem 34: 2624-33 (1991)
Zambeletti Research Laboratories
Synthesis and anticancer and antiviral activities of various 2'- and 3'-methylidene-substituted nucleoside analogues and crystal structure of 2'-deoxy-2'-methylidenecytidine hydrochloride.EBI
J Med Chem 34: 2607-15 (1991)
Yale University
Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor.EBI
J Med Chem 34: 2561-9 (1991)
Abbott Laboratories
3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.EBI
J Med Chem 34: 2557-60 (1991)
Laboratoire De Pharmacie Chimique, Facult�
Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.EBI
J Med Chem 34: 2438-44 (1991)
University Of Washington
Sulfonylbenzoyl-nitrostyrenes: potential bisubstrate type inhibitors of the EGF-receptor tyrosine protein kinase.EBI
J Med Chem 34: 2328-37 (1991)
Ciba-Geigy
Competition of leukotrienes and ICI-198,615 for [3H]LTD4 binding sites in guinea pig lung membranes suggests the involvement of two LTD4 receptor subtypes.BDB
J Pharmacol Exp Ther 258: 531-6 (1991)
Pfizer
(Methoxyalkyl)thiazoles: a new series of potent, selective, and orally active 5-lipoxygenase inhibitors displaying high enantioselectivity.EBI
J Med Chem 34: 2176-86 (1991)
Ici Pharmaceuticals Group
Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide.EBI
J Med Chem 34: 1891-6 (1991)
University Of Notre Dame
Radiosynthesis of sigma receptor ligands for positron emission tomography: 11C- and 18F-labeled guanidines.EBI
J Med Chem 34: 1867-70 (1991)
Institutions
Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors.EBI
J Med Chem 34: 1855-9 (1991)
Virginia Commonwealth University
Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands.EBI
J Med Chem 34: 1850-4 (1991)
Universitá
Topographically designed analogues of [D-Pen,D-Pen5]enkephalin.EBI
J Med Chem 34: 1823-30 (1991)
University Of Arizona
An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.EBI
J Med Chem 34: 1757-62 (1991)
University Of Minnesota
Pharmacological profiles for rat cortical M1 and M2 muscarinic receptors using selective antagonists: comparison with N1E-115 muscarinic receptors.BDB
J Pharmacol Exp Ther 257: 1121-9 (1991)
Mayo Clinic
Acetazolamide-like carbonic anhydrase inhibitors with topical ocular hypotensive activity.EBI
J Med Chem 35: 2697-703 (1992)
Istituto Chimico Internazionale Dr. G. Rende
Nonpeptide angiotensin II receptor antagonists: synthetic and computational chemistry of N-[[4-[2-(2H-tetrazol-5-yl)-1-cycloalken-1- yl]phenyl]methyl]imidazole derivatives and their in vitro activity.EBI
J Med Chem 35: 2658-67 (1992)
Eli Lilly
N-[4-[[(3,4-dihydro-4-oxo-1,2,3-benzotriazin-6- yl)methyl]amino]benzoyl]-L-glutamic acid, a novel A-ring analogue of 2-desamino-5,8-dideazafolic acid.EBI
J Med Chem 35: 2626-30 (1992)
Harvard Medical School
Rationally designed"dipeptoid" analogues of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist CI-988.EBI
J Med Chem 35: 2573-81 (1992)
Parke-Davis Neuroscience Research Centre
Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.EBI
J Med Chem 35: 2562-72 (1992)
Parke-Davis Pharmaceutical Research Division Of Warner-Lambert
Synthesis and X-ray crystallographic analysis of quinazolinone cholecystokinin/gastrin receptor ligands.EBI
J Med Chem 35: 2534-42 (1992)
Eli Lilly
A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity.EBI
J Med Chem 35: 2525-33 (1992)
Merck Research Laboratories
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.EBI
J Med Chem 35: 2501-24 (1992)
Wyeth-Ayerst Research
SDZ 205-557, a selective, surmountable antagonist for 5-HT4 receptors in the isolated guinea pig ileum.BDB
Naunyn Schmiedebergs Arch Pharmacol 345: 387-93 (1992)
Sandoz Pharma
Isopropyl and phenyl esters of 3 beta-(4-substituted phenyl)tropan-2 beta-carboxylic acids. Potent and selective compounds for the dopamine transporter.EBI
J Med Chem 35: 2497-500 (1992)
Research Triangle Institute
Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands.EBI
J Med Chem 35: 2392-406 (1992)
Smithkline Beecham Pharmaceuticals
2-Alkynyl derivatives of adenosine and adenosine-5'-N-ethyluronamide as selective agonists at A2 adenosine receptors.EBI
J Med Chem 35: 2363-8 (1992)
Universit£
(E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists.EBI
J Med Chem 35: 2342-5 (1992)
Kyowa Hakko Kogyo
Quinazoline antifolate thymidylate synthase inhibitors: difluoro-substituted benzene ring analogues.EBI
J Med Chem 35: 2321-7 (1992)
Institute Of Cancer Research
Novel functional M1 selective muscarinic agonists. Synthesis and structure-activity relationships of 3-(1,2,5-thiadiazolyl)-1,2,5,6-tetrahydro-1-methylpyridines .EBI
J Med Chem 35: 2274-83 (1992)
Novo Nordisk Cns Division
Nucleosides and nucleotides. 107. 2-(cycloalkylalkynyl)adenosines: adenosine A2 receptor agonists with potent antihypertensive effects.EBI
J Med Chem 35: 2253-60 (1992)
Yamasa Shoyu
Iodoaminopotentidine and related compounds: a new class of ligands with high affinity and selectivity for the histamine H2 receptor.EBI
J Med Chem 35: 2231-8 (1992)
Freie Universit£T Berlin
Synthesis and aromatase inhibition of 3-cycloalkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones.EBI
J Med Chem 35: 2210-4 (1992)
UniversitäT Des Saarlandes
Synthesis and muscarinic receptor activity of ester derivatives of 2-substituted 2-azabicyclo[2.2.1]heptan-5-ol and -6-ol.EBI
J Med Chem 35: 2184-91 (1992)
Research Triangle Institute
Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography.EBI
J Med Chem 35: 2178-83 (1992)
Brookhaven National Laboratory
Hydantoin bioisosteres. In vivo active spiro hydroxy acetic acid aldose reductase inhibitors.EBI
J Med Chem 35: 2169-77 (1992)
Pfizer
Orally active aldose reductase inhibitors: indazoleacetic, oxopyridazineacetic, and oxopyridopyridazineacetic acid derivatives.EBI
J Med Chem 35: 2155-62 (1992)
Pfizer
Interaction of flexible analogs of N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine and of N-methyl-4-phenylpyridinium with highly purified monoamine oxidase A and B.BDB
Biochemistry 31: 5611-5 (1992)
University Of California San Francisco
Renin inhibitors containing C-termini derived from mercaptoheterocycles.EBI
J Med Chem 35: 2103-12 (1992)
Merck Sharp & Dohme Research Laboratories
Inhibitors of cholesterol biosynthesis. 6. trans-6-[2-(2-N-heteroaryl-3,5-disubstituted- pyrazol-4-yl)ethyl/ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones.EBI
J Med Chem 35: 2095-103 (1992)
Warner-Lambert
Biological activities and quantitative structure-activity relationships of spiro[imidazolidine-4,4'(1'H)-quinazoline]-2,2',5(3'H)-triones as aldose reductase inhibitors.EBI
J Med Chem 35: 2085-94 (1992)
Tanabe Seiyaku
Cyclic RGD peptide analogues as antiplatelet antithrombotics.EBI
J Med Chem 35: 2040-8 (1992)
Genentech
A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1.EBI
J Med Chem 35: 1978-86 (1992)
National Cancer Institute-Frederick
Metabolism of the Catharanthus Alkaloids: from Streptomyces griseus to Monoamine Oxidase BEBI
J Nat Prod 55: 269-284 (1992)
TBA
Synthesis and pharmacological investigation of the enantiomers of muscarone and allomuscarone.EBI
J Med Chem 35: 1915-20 (1992)
Istituto Chimico-Farmaceutico Dell'Università
Probes for the cocaine receptor. Potentially irreversible ligands for the dopamine transporter.EBI
J Med Chem 35: 1813-7 (1992)
Research Triangle Institute
4'-modified analogues of aristeromycin and neplanocin A: synthesis and inhibitory activity toward S-adenosyl-L-homocysteine hydrolase.EBI
J Med Chem 35: 1782-91 (1992)
University Of Kansas
C-terminal modifications of nonpeptide renin inhibitors: improved oral bioavailability via modification of physicochemical properties.EBI
J Med Chem 35: 1735-46 (1992)
Abbott Laboratories
Nonpeptide renin inhibitors employing a novel 3-aza(or oxa)-2,4-dialkyl glutaric acid moiety as a P2/P3 amide bond replacement.EBI
J Med Chem 35: 1722-34 (1992)
Abbott Laboratories
1,2,3-trisubstituted cyclopropanes as conformationally restricted peptide isosteres: application to the design and synthesis of novel renin inhibitors.EBI
J Med Chem 35: 1710-21 (1992)
University Of Texas
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.BDB
J Med Chem 35: 1702-9 (1992)
Merck Research Laboratories
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.BDB
J Med Chem 35: 1685-701 (1992)
Merck Research Laboratories
Definition and display of steric, hydrophobic, and hydrogen-bonding properties of ligand binding sites in proteins using Lee and Richards accessible surface: validation of a high-resolution graphical tool for drug design.EBI
J Med Chem 35: 1671-84 (1992)
Ciba-Geigy
Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles.EBI
J Med Chem 35: 1663-70 (1992)
Sterling Winthrop Pharmaceuticals Research Division
Localization and function of the D3 dopamine receptor.BDB
Arzneimittelforschung 42: 224-30 (1992)
U. 109
Analogues of platelet activating factor. 6. Mono- and bis-aryl phosphate antagonists of platelet activating factor.EBI
J Med Chem 35: 1650-62 (1992)
American Cyanamid
Inhibitors of acyl-CoA:cholesterol acyltransferase. 1. Identification and structure-activity relationships of a novel series of fatty acid anilide hypocholesterolemic agents.EBI
J Med Chem 35: 1609-17 (1992)
Warner-Lambert
Inhibitors of human purine nucleoside phosphorylase. Synthesis of pyrrolo[3,2-d]pyrimidines, a new class of purine nucleoside phosphorylase inhibitors as potentially T-cell selective immunosuppressive agents. Description of 2,6-diamino-3,5-dihydro-7-(3-thienylmethyl)-4H-pyrrolo[3,2-d] pyrimidin-4-oEBI
J Med Chem 35: 1605-9 (1992)
Warner-Lambert
Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G.EBI
J Med Chem 35: 1597-605 (1992)
Georgia Institute Of Technology
Synthesis and evaluation of a new series of mechanism-based aromatase inhibitors.EBI
J Med Chem 35: 1588-97 (1992)
Centre De Recherches Roussel-Uclaf
Side chain modified 5-deazafolate and 5-deazatetrahydrofolate analogues as mammalian folylpolyglutamate synthetase and glycinamide ribonucleotide formyltransferase inhibitors: synthesis and in vitro biological evaluation.EBI
J Med Chem 35: 1578-88 (1992)
Harvard Medical School
Rationally designed"dipeptoid" analogues of CCK. A Free-Wilson/Fujita-Ban analysis of some alpha-methyltryptophan derivatives as CCK-B antagonists.EBI
J Med Chem 35: 1572-7 (1992)
Parke-Davis Neuroscience Research Centre
Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors.EBI
J Med Chem 35: 1550-7 (1992)
Abbott Laboratories
Analogues of the muscarinic agent 2'-methylspiro[1-azabicyclo[2.2.2]octane-3,4'-[1,3]dioxolane]: synthesis and pharmacology.EBI
J Med Chem 35: 1541-50 (1992)
Uppsala University
SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype.EBI
J Med Chem 35: 1486-9 (1992)
Searle Research And Development
Amide bond replacements incorporated into CCK-B selective"dipeptoids".EBI
J Med Chem 35: 1472-84 (1992)
Parke-Davis Neuroscience Research Center
Inhibitors of human purine nucleoside phosphorylase. Synthesis and biological activities of 8-amino-3-benzylhypoxanthine and related analogues.EBI
J Med Chem 35: 1451-7 (1992)
Warner-Lambert
Syntheses, resolution, and structure-activity relationships of potent acetylcholinesterase inhibitors: 8-carbaphysostigmine analogues.EBI
J Med Chem 35: 1429-34 (1992)
Pfizer
Inhibition of pig kidney L-aromatic amino acid decarboxylase by 2,3-methano-m-tyrosines.EBI
J Med Chem 35: 1410-7 (1992)
University Of Georgia
Synthesis and biological activity of open-chain analogues of 5,6,7,8-tetrahydrofolic acid--potential antitumor agents.EBI
J Med Chem 35: 1399-410 (1992)
Wellcome Research Laboratories
2-substituted 3-(aminooxy)propanamines as inhibitors of ornithine decarboxylase: synthesis and biological activity.EBI
J Med Chem 35: 1339-44 (1992)
Ciba-Geigy
Steady-state kinetic mechanism of Ras farnesyl:protein transferase.BDB
Biochemistry 31: 3800-7 (1992)
Merck Research Laboratories
Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.BDB
Proc Natl Acad Sci U S A 89: 3630-4 (1992)
Synaptic Pharmaceutical
Intriguing structure-activity relations underlie the potent inhibition of HIV protease by norstatine-based peptides.EBI
J Med Chem 35: 1318-20 (1992)
Syntex Research
Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogues).EBI
J Med Chem 35: 1290-5 (1992)
Institute Of Research
Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.EBI
J Med Chem 35: 1280-90 (1992)
Smithkline Beecham Pharmaceuticals
Agonist activity of 2- and 5'-substituted adenosine analogs and their N6-cycloalkyl derivatives at A1- and A2-adenosine receptors coupled to adenylate cyclase.BDB
Biochem Pharmacol 43: 1089-93 (1992)
National Institutes Of Diabetes And Digestive And Kidney Diseases
Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity.BDB
J Med Chem 35: 994-1001 (1992)
Roche Products
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.EBI
J Med Chem 35: 969-81 (1992)
Research Triangle Institute
Selective irreversible inhibitors of aldose reductase.EBI
J Med Chem 35: 1117-20 (1992)
Ohio State University
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.EBI
J Med Chem 35: 1102-8 (1992)
University Of South Carolina
Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions.EBI
J Med Chem 35: 1058-67 (1992)
National Cancer Institute-Bethesda
Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718.EBI
J Med Chem 35: 1042-9 (1992)
Center For Bio-Pharmaceutical Sciences
Renin inhibitors containing alpha-heteroatom amino acids as P2 residues.EBI
J Med Chem 35: 1032-42 (1992)
Warner-Lambert
Novel 5-HT3 antagonists: indol-3-ylspiro(azabicycloalkane-3,5'(4'H)-oxazoles).EBI
J Med Chem 35: 1019-31 (1992)
Merck Sharp And Dohme Research Laboratories
Antiestrogens. 3. Estrogen receptor affinities and antiproliferative effects in MCF-7 cells of phenolic analogues of trioxifene, [3,4-dihydro-2-(4- methoxyphenyl)-1-naphthalenyl][4-[2-(1-pyrrolidinyl)ethoxy]- phenyl]methanone.EBI
J Med Chem 35: 931-8 (1992)
Eli Lilly
8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.EBI
J Med Chem 35: 924-30 (1992)
Kyowa Hakko Kogyo
Synthesis and in vitro biological profile of all four isomers of the potent muscarinic agonist 3-(3-methyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane.EBI
J Med Chem 35: 911-6 (1992)
Merck Sharp And Dohme Research Laboratories
5-(Aminomethyl)-3-aryldihydrofuran-2(3H)-ones, a new class of monoamine oxidase-B inactivators.EBI
J Med Chem 35: 885-9 (1992)
Northwestern University
New nonpeptide angiotensin II receptor antagonists. 1. Synthesis, biological properties, and structure-activity relationships of 2-alkyl benzimidazole derivatives.EBI
J Med Chem 35: 877-85 (1992)
Ici Pharmaceuticals Group
Design and synthesis of novel 6,7-imidazotetrahydroquinoline inhibitors of thymidylate synthase using iterative protein crystal structure analysis.EBI
J Med Chem 35: 847-58 (1992)
Agouron Pharmaceuticals
Synthesis and use of 3-amino-4-phenyl-2-piperidones and 4-amino-2-benzazepin-3-ones as conformationally restricted phenylalanine isosteres in renin inhibitors.EBI
J Med Chem 35: 833-46 (1992)
Merck Sharp And Dohme Research Laboratories
New modified heterocyclic phenylalanine derivatives. Incorporation into potent inhibitors of human renin.EBI
J Med Chem 35: 823-32 (1992)
Wyeth-Ayerst Research
Binding of phenylalkylamine derivatives at 5-HT1C and 5-HT2 serotonin receptors: evidence for a lack of selectivity.EBI
J Med Chem 35: 734-40 (1992)
Virginia Commonwealth University
4-substituted 2-alkoxytetrahydrofurans as potent and long-lasting PAF antagonists.EBI
J Med Chem 35: 676-83 (1992)
J. Uriach & CíA.
Inhibition of human leukocyte elastase (HLE) by N-substituted peptidyl trifluoromethyl ketones.EBI
J Med Chem 35: 641-62 (1992)
Boehringer Ingelheim Pharmaceuticals
A steric and electrostatic comparison of three models for the agonist/antagonist binding site on the adenosine A1 receptor.EBI
J Med Chem 35: 629-35 (1992)
Center For Bio-Pharmaceutical Sciences
Structure-activity relationship studies of central nervous system agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor site.EBI
J Med Chem 35: 2369-74 (1992)
Polish Academy Of Sciences
Conformational analysis of dopamine D-2 receptor antagonists of the benzamide series in relation to a recently proposed D-2 receptor-interaction model.EBI
J Med Chem 35: 2355-63 (1992)
University Of Lund
Synthesis and thromboxane A2/prostaglandin H2 receptor antagonistic activity of phenol derivatives.EBI
J Med Chem 35: 2202-9 (1992)
Takeda Chemical Industries
Benzofuran bioisosteres of hallucinogenic tryptamines.EBI
J Med Chem 35: 2061-4 (1992)
Purdue University
4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor.EBI
J Med Chem 35: 1954-68 (1992)
Merck Sharp And Dohme Research Laboratories
Affinity of human growth hormone-releasing factor (1-29)NH2 analogues for GRF binding sites in rat adenopituitary.EBI
J Med Chem 35: 1864-9 (1992)
Notre-Dame Hospital Research
3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site.EBI
J Med Chem 35: 1791-9 (1992)
Marion Merrell Dow Research Institute
Stereoisomeric probes for the D1 dopamine receptor: synthesis and characterization of R-(+) and S-(-) enantiomers of 3-allyl-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine and its 6-bromo analogue.EBI
J Med Chem 35: 1466-71 (1992)
Research Biochemicals
A study on the contribution of the 1-phenyl substituent to the molecular electrostatic potentials of some benzazepines in relation to selective dopamine D-1 receptor activity.EBI
J Med Chem 35: 502-7 (1992)
University Of Lund
Effect of N-alkylation on the affinities of analogues of spiperone for dopamine D2 and serotonin 5-HT2 receptors.EBI
J Med Chem 35: 423-30 (1992)
University Of Pennsylvania
(+/-)-3-allyl-7-halo-8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines as selective high affinity D1 dopamine receptor antagonists: synthesis and structure-activity relationship.EBI
J Med Chem 35: 67-72 (1992)
Northeastern University
Specific inhibition of HIV-1 protease by boronated porphyrins.EBI
J Med Chem 35: 3426-8 (1992)
University Of California
Synthesis and biological evaluation of dihydroeptastatin, a novel inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase.EBI
J Med Chem 35: 3388-93 (1992)
British Bio-Technology
3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-deoxythymidine.EBI
J Med Chem 35: 3369-72 (1992)
Purdue University
Synthesis and biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors.EBI
J Med Chem 35: 3364-9 (1992)
Thrombosis Research Institute
Synthesis and antibronchospastic activity of 8-alkoxy- and 8-(alkylamino)imidazo[1,2-a]pyrazines.EBI
J Med Chem 35: 3353-8 (1992)
Ura Cnrs 1111
Synthesis of a homologous series of ketomethylene arginyl pseudodipeptides and application to low molecular weight hirudin-like thrombin inhibitors.EBI
J Med Chem 35: 3331-41 (1992)
National Research Council Of Canada
Inhibition of Angiotensin-I-Converting Enzyme by Tetrahydroxyxanthones Isolated from Tripterospermum lanceolatumEBI
J Nat Prod 55: 691-695 (1992)
TBA
Human gene S31 encodes the pharmacologically defined serotonin 5-hydroxytryptamine1E receptor.BDB
Mol Pharmacol 42: 180-5 (1992)
Synaptic Pharmaceutical
Urea and 2-imidazolidone derivatives of the muscarinic agents oxotremorine and N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.EBI
J Med Chem 35: 3270-9 (1992)
University Of Uppsala
Conformationally restrained, chiral (phenylisopropyl)amino-substituted pyrazolo[3,4-d]pyrimidines and purines with selectivity for adenosine A1 and A2 receptors.EBI
J Med Chem 35: 3263-9 (1992)
Marion Merrell Dow Research Institute
Histamine H2-receptor agonists. Synthesis, in vitro pharmacology, and qualitative structure-activity relationships of substituted 4- and 5-(2-aminoethyl)thiazoles.EBI
J Med Chem 35: 3239-46 (1992)
Vrije Universiteit
Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity.EBI
J Med Chem 35: 3148-55 (1992)
Dupont Pharmaceuticals
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.EBI
J Med Chem 35: 3141-7 (1992)
University Of South Carolina
1,4-Dihydropyridines as antagonists of platelet activating factor. 1. Synthesis and structure-activity relationships of 2-(4-heterocyclyl)phenyl derivatives.EBI
J Med Chem 35: 3115-29 (1992)
Pfizer
Synthesis and pharmacological evaluation of enantiomerically pure 4-deoxy-4-fluoromuscarines.EBI
J Med Chem 35: 3102-10 (1992)
C.N.R.-Centro Studio Sostanze Organiche Naturali
Mapping the binding site of tissue kallikrein: preparation and testing of all possible substrate analog inhibitors homologous with the sequence of kininogen between Ser386 and Gln392.EBI
J Med Chem 35: 3094-102 (1992)
University Hospital
Penicillin derived C2-symmetric dimers as novel inhibitors of HIV-1 proteinase.EBI
J Med Chem 35: 3080-1 (1992)
Glaxo Group Research
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.EBI
J Med Chem 35: 3066-75 (1992)
Kyowa Hakko Kogyo
PgH2 analogs as potential antiplatelet derivatives.EBI
J Med Chem 35: 3033-9 (1992)
University Of Illinois
Thieno[2,3-b]furan-2-sulfonamides as topical carbonic anhydrase inhibitors.EBI
J Med Chem 35: 3027-33 (1992)
Merck Research Laboratories
Synthesis and antifolate evaluation of 10-ethyl-5-methyl-5,10- dideazaaminopterin and an alternative synthesis of 10-ethyl-10- deazaaminopterin (edatrexate).EBI
J Med Chem 35: 3002-6 (1992)
Southern Research Institute
Design and synthesis of some substrate analogue inhibitors of phospholipase A2 and investigations by NMR and molecular modeling into the binding interactions in the enzyme-inhibitor complex.EBI
J Med Chem 35: 2939-51 (1992)
Fisons
Synthesis and biological activity of CCK heptapeptide analogues. Effects of conformational constraints and standard modifications on receptor subtype selectivity, functional activity in vitro, and appetite suppression in vivo.EBI
J Med Chem 35: 2919-28 (1992)
Abbott Laboratories
Biochemical and pharmacological properties of SR 46349B, a new potent and selective 5-hydroxytryptamine2 receptor antagonist.BDB
J Pharmacol Exp Ther 262: 759-68 (1992)
Sanofi Recherche
Probing the molecular basis of resistance to pyrimethamine by site-directed mutagenesis.EBI
J Med Chem 35: 2912-5 (1992)
Pennsylvania State University
Nucleosides and nucleotides. 112. 2-(1-Hexyn-1-yl)adenosine-5'-uronamides: a new entry of selective A2 adenosine receptor agonists with potent antihypertensive activity.EBI
J Med Chem 35: 2881-90 (1992)
Hokkaido University
2-Substituted 1-azabicycloalkanes, a new class of non-opiate antinociceptive agents.EBI
J Med Chem 35: 2855-63 (1992)
R. W. Johnson Pharmaceutical Research Institute
Stereoisomers of ketoconazole: preparation and biological activity.EBI
J Med Chem 35: 2818-25 (1992)
Syntex Research
N-methylated analogs of Ac[Nle28,31]CCK(26-33): synthesis, activity, and receptor selectivity.EBI
J Med Chem 35: 2806-11 (1992)
Hadassah-University Hospital
Inhibitors of human renin with C-termini derived from amides and esters of alpha-mercaptoalkanoic acids.EBI
J Med Chem 35: 2772-81 (1992)
Merck Research Laboratories
Quinoline antifolate thymidylate synthase inhibitors: variation of the C2- and C4-substituents.EBI
J Med Chem 35: 2761-8 (1992)
Ici Pharmaceuticals Group
Potent inhibitors of platelet aggregation based upon the Arg-Gly-Asp-Phe sequence of fibrinogen. A proposal on the nature of the binding interaction between the Asp-carboxylate of RGDX mimetics and the platelet GP IIb-IIIa receptor.EBI
J Med Chem 35: 4914-7 (1993)
Searle Research & Development
Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding.EBI
J Med Chem 35: 4903-10 (1993)
Virginia Commonwealth University
5-HT3 receptor antagonists. 1. New quinoline derivatives.EBI
J Med Chem 35: 4893-902 (1992)
Kyowa Hakko Kogyo
ATP-citrate lyase as a target for hypolipidemic intervention. Sulfoximine and 3-hydroxy-beta-lactam containing analogues of citric acid as potential tight-binding inhibitors.EBI
J Med Chem 35: 4875-84 (1992)
Smithkline Beecham Pharmaceuticals
New bronchodilators. 3. Imidazo[4,5-c][1,8]naphthyridin-4(5H)-ones.EBI
J Med Chem 35: 4866-74 (1992)
Kyowa Hakko Kogyo
Inhibition of human leukocyte elastase by N-substituted peptides containing alpha,alpha-difluorostatone residues at P1.EBI
J Med Chem 35: 4795-808 (1993)
Boehringer Ingelheim Pharmaceuticals
Synthesis and physicochemical properties of sulfamate derivatives as topical antiglaucoma agents.EBI
J Med Chem 35: 4790-4 (1992)
A.H. Robins
Protein-Tyrosine Kinase Inhibition: Mechanism-Based Discovery of Antitumor AgentsEBI
J Nat Prod 55: 1529-1560 (1992)
TBA
Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue.EBI
J Med Chem 35: 4764-6 (1993)
Mayo Foundation
Dihydropyrimidine angiotensin II receptor antagonists.EBI
J Med Chem 35: 4751-63 (1993)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis, configuration, and activity of isomeric 2-phenyl-2-(N-piperidinyl)bicyclo[3.1.0]hexanes at phencyclidine and sigma binding sites.EBI
J Med Chem 35: 4704-12 (1993)
National Institute Of Diabetes And Digestive And Kidney Diseases
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.EBI
J Med Chem 35: 4683-9 (1993)
National Institute On Drug Abuse
Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors.EBI
J Med Chem 35: 4640-2 (1993)
Merck Research Laboratories
Dihydroxynitrobenzaldehydes and hydroxymethoxynitrobenzaldehydes: synthesis and biological activity as catechol-O-methyltransferase inhibitors.EBI
J Med Chem 35: 4584-8 (1993)
Instituto De QuíMica OrgáNica General (Csic)
2-(N'-aralkylidenehydrazino)adenosines: potent and selective coronary vasodilators.EBI
J Med Chem 35: 4562-6 (1993)
University Of South Florida
2-(N'-alkylidenehydrazino)adenosines: potent and selective coronary vasodilators.EBI
J Med Chem 35: 4557-61 (1993)
University Of South Florida
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-(2-phthalimidoethyl)piperidine and related derivatives.EBI
J Med Chem 35: 4542-8 (1993)
Eisai
The mouse 5HT5 receptor reveals a remarkable heterogeneity within the 5HT1D receptor family.BDB
EMBO J 11: 4779-86 (1992)
Cnrs
Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin.EBI
J Med Chem 35: 4503-5 (1992)
Pfizer
A dideazatetrahydrofolate analogue lacking a chiral center at C-6, N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5- yl)ethyl]benzoyl]-L-glutamic acid, is an inhibitor of thymidylate synthase.EBI
J Med Chem 35: 4450-4 (1992)
Princeton University
Synthesis and biological activity of 4-(diphenylmethyl)-alpha-[(4-quinolinyloxy)methyl]-1-piperazineethanol and related compounds.EBI
J Med Chem 35: 4442-9 (1992)
Warner-Lambert
Acyl-CoA:cholesterol O-acyl transferase (ACAT) inhibitors. 1. 2-(Alkylthio)-4,5-diphenyl-1H-imidazoles as potent inhibitors of ACAT.EBI
J Med Chem 35: 4384-92 (1992)
Rhone-Poulenc Rorer
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.EBI
J Med Chem 35: 4373-83 (1992)
Ciba-Geigy
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 3. Pyridinylalkyl-substituted 8-[(arylsulfonyl)amino]octanoic acids.EBI
J Med Chem 35: 4366-72 (1992)
Ciba-Geigy
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 2. Synthesis and biological activity of 8-(benzenesulfonamido)-7-(3-pyridinyl)octaonic acid and related compounds.EBI
J Med Chem 35: 4362-5 (1992)
Ciba-Geigy
Synthesis and biological evaluation of conformationally restricted 2-(1-pyrrolidinyl)-N-[2-(3,4-dichlorophenyl)ethyl]-N-methylethylenediam ines as sigma receptor ligands. 1. Pyrrolidine, piperidine, homopiperidine, and tetrahydroisoquinoline classes.EBI
J Med Chem 35: 4334-43 (1992)
National Institute Of Diabetes And Digestive And Kidney Diseases
Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.EBI
J Med Chem 35: 4297-305 (1992)
University Of Illinois
Analogs of CCK incorporating conformationally constrained replacements for Asp32.EBI
J Med Chem 35: 4249-52 (1992)
Roche Research Center
Structure-activity studies on benzhydrol-containing nipecotic acid and guvacine derivatives as potent, orally-active inhibitors of GABA uptake.EBI
J Med Chem 35: 4238-48 (1992)
Warner-Lambert
Adenosine deaminase inhibitors. Synthesis and biological evaluation of C1' and nor-C1' derivatives of (+)-erythro-9-(2(S)-hydroxy-3(R)-nonyl)adenine.EBI
J Med Chem 35: 4180-4 (1992)
University Of Rhode Island
Synthesis of novel MPTP analogs as potential monoamine oxidase B (MAO-B) inhibitors.EBI
J Med Chem 35: 4165-74 (1992)
Virginia Polytechnic Institute And State University
Guanidinophenyl-substituted enol lactones as selective, mechanism-based inhibitors of trypsin-like serine proteases.EBI
J Med Chem 35: 4150-9 (1992)
University Of Illinois
Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective adenosine agonists.EBI
J Med Chem 35: 4143-9 (1992)
National Institute Of Diabetes
(Pyridylcyanomethyl)piperazines as orally active PAF antagonists.EBI
J Med Chem 35: 4118-34 (1992)
J. Uriach & C£A.S.A.
Inhibition of hog liver folylpolyglutamate synthetase by 5-substituted 5,8-dideaza analogues of folic acid bearing a terminal L-ornithine residue.EBI
J Med Chem 35: 4078-85 (1992)
Medical University Of South Carolina
Synthesis, chemical, and biological properties of vinylogous hydroxamic acids: dual inhibitors of 5-lipoxygenase and IL-1 biosynthesis.EBI
J Med Chem 35: 4061-8 (1992)
Dupont Pharmaceuticals
New nonpeptide angiotensin II receptor antagonists. 2. Synthesis, biological properties, and structure-activity relationships of 2-alkyl-4-(biphenylylmethoxy)quinoline derivatives.EBI
J Med Chem 35: 4027-38 (1992)
Ici Pharmaceuticals Group
Novel functional M1 selective muscarinic agonists. 2. Synthesis and structure-activity relationships of 3-pyrazinyl-1,2,5,6-tetrahydro-1-methylpyridines. Construction of a molecular model for the M1 pharmacophore.EBI
J Med Chem 35: 4011-9 (1992)
Eli Lilly
6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists.EBI
J Med Chem 35: 3984-90 (1992)
University Of GöTeborg
4-Oxospiro[benzopyran-2,4'-piperidines] as class III antiarrhythmic agents. Pharmacological studies on 3,4-dihydro-1'-[2-(benzofurazan-5-yl)- ethyl]-6-methanesulfonamidospiro[(2H)-1-benzopyran-2,4'-piperidin]-4-on e (L-691,121).EBI
J Med Chem 35: 3973-6 (1992)
Merck Research Laboratories
Design and synthesis of a C7 mimetic for the predicted gamma-turn conformation found in several constrained RGD antagonists.EBI
J Med Chem 35: 3970-2 (1992)
Smithkline Beecham Pharmaceuticals
Investigation of conformational specificity at GPIIb/IIIa: evaluation of conformationally constrained RGD peptides.EBI
J Med Chem 35: 3962-9 (1992)
Smithkline Beecham Pharmaceuticals
Stabilization of the N-terminal residues of luteinizing hormone-releasing hormone agonists and the effect on pharmacokinetics.EBI
J Med Chem 35: 3890-4 (1992)
Abbott Laboratories
Imidazole-5-acrylic acids: potent nonpeptide angiotensin II receptor antagonists designed using a novel peptide pharmacophore model.EBI
J Med Chem 35: 3858-72 (1992)
Smithkline Beecham Pharmaceuticals
4-substituted thiophene- and furan-2-sulfonamides as topical carbonic anhydrase inhibitors.EBI
J Med Chem 35: 3822-31 (1992)
Merck Research Laboratories
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 9. The synthesis and biological evaluation of novel simvastatin analogs.EBI
J Med Chem 35: 3813-21 (1992)
Merck Research Laboratories
New hydroxyethylamine HIV protease inhibitors that suppress viral replication.EBI
J Med Chem 35: 3803-12 (1992)
University Of Wisconsin-Madison
Analogs of Ac-CCK-7 incorporating dipeptide mimics in place of Met28-Gly29.EBI
J Med Chem 35: 3774-83 (1992)
Roche Research Center
Highly potent, orally active diester macrocyclic human renin inhibitors.EBI
J Med Chem 35: 3755-73 (1992)
Merck Research Laboratories
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.EBI
J Med Chem 35: 3731-44 (1992)
Merck Research Laboratories
Discovery of a novel class of orally active, non-peptide angiotensin II antagonists.EBI
J Med Chem 35: 3714-7 (1992)
Abbott Laboratories
Aliphatic propargylamines: potent, selective, irreversible monoamine oxidase B inhibitors.EBI
J Med Chem 35: 3705-13 (1992)
University Of Saskatchewan
Conformational analysis of the aromatase inhibitor 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione (rogletimide) and discovery of potent 5-alkyl derivatives.EBI
J Med Chem 35: 3699-704 (1992)
Institute Of Cancer Research
Novel 1,2,4-oxadiazoles and 1,2,4-thiadiazoles as dual 5-lipoxygenase and cyclooxygenase inhibitors.EBI
J Med Chem 35: 3691-8 (1992)
Warner-Lambert
5,10-Methylenetetrahydro-5-deazafolic acid and analogues: synthesis and biological activities.EBI
J Med Chem 35: 3678-85 (1992)
Duquesne University
Truncated, branched, and/or cyclic analogues of neuropeptide Y: importance of the pancreatic peptide fold in the design of specific Y2 receptor ligands.EBI
J Med Chem 35: 3653-9 (1992)
Salk Institute
Prodrugs of nitroxyl as inhibitors of aldehyde dehydrogenase.EBI
J Med Chem 35: 3648-52 (1992)
University Of Minnesota
1-(2-Aminoethyl)-3-methyl-8,9-dihydropyrano[3,2-e]indole: a rotationally restricted phenolic analog of the neurotransmitter serotonin and agonist selective for serotonin (5-HT2-type) receptors.EBI
J Med Chem 35: 3625-32 (1992)
Pfizer
Displacement Activity of Bisbenzylisoquinoline Alkaloids at Striatal 3H-SCH 23390 and 3H-Raclopride Binding SitesEBI
J Nat Prod 55: 1281-1286 (1992)
TBA
Brominated polyacetylenic acids from the marine sponge Xestospongia muta: inhibitors of HIV protease.EBI
J Nat Prod 55: 1170-7 (1992)
Smithkline Beecham Pharmaceuticals
N-(1-oxododecyl)-4 alpha,10-dimethyl-8-aza-trans-decal-3 beta-ol: a potent competitive inhibitor of 2,3-oxidosqualene cyclase.EBI
J Med Chem 35: 3581-3 (1992)
Marion Merrell Dow Research Institute
7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.EBI
J Med Chem 35: 3578-81 (1992)
Kyowa Hakko Kogyo
Renin inhibitors containing new P1-P1' dipeptide mimetics with heterocycles in P1'.EBI
J Med Chem 35: 3525-36 (1992)
E. Merck Darmstadt
Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran, a potent orally active platelet-activating factor (PAF) antagonist and its water-soluble prodrug phosphate ester.EBI
J Med Chem 35: 3474-82 (1992)
Merck Research Laboratories
NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists.BDB
Eur J Pharmacol 219: 45-52 (1992)
Novo Nordisk
Inhibition of protein kinase C by cationic amphiphiles.BDB
Biochemistry 31: 9025-30 (1992)
Mcmaster University
Non-prostanoid thromboxane A2 receptor antagonists with a dibenzoxepin ring system. 2.EBI
J Med Chem 35: 3402-13 (1992)
Kyowa Hakko Kogyo
Non-prostanoid thromboxane A2 receptor antagonists with a dibenzoxepin ring system. 1.EBI
J Med Chem 35: 3394-402 (1992)
Kyowa Hakko Kogyo
Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinones.EBI
J Med Chem 35: 3319-24 (1992)
Eli Lilly
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.EBI
J Med Chem 35: 2591-600 (1992)
Pfizer
Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators.EBI
J Med Chem 35: 2407-14 (1992)
Alter
Studies on neurokinin antagonists. 1. The design of novel tripeptides possessing the glutaminyl-D-tryptophylphenylalanine sequence as substance P antagonists.EBI
J Med Chem 35: 2015-25 (1992)
Fujisawa Pharmaceutical
Development of potent and selective CCK-A receptor agonists from Boc-CCK-4: tetrapeptides containing Lys(N epsilon)-amide residues.EBI
J Med Chem 35: 2007-14 (1992)
Abbott Laboratories
Synthesis and biological evaluation of N alpha-(5-deaza-5,6,7,8-tetrahydropteroyl)-L-ornithine.EBI
J Med Chem 35: 2002-6 (1992)
Medical University Of South Carolina
New thymidine triphosphate analogue inhibitors of human immunodeficiency virus-1 reverse transcriptase.EBI
J Med Chem 35: 1938-41 (1992)
University Of California
Anti-aids agents, 6. Salaspermic acid, an anti-HIV principle from Tripterygium wilfordii, and the structure-activity correlation with its related compounds.EBI
J Nat Prod 55: 340-6 (1992)
University Of North Carolina
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 2. Tricyclic pyridobenzoxazepinones and dibenzoxazepinones.BDB
J Med Chem 35: 1887-97 (1992)
Boehringer Ingelheim Pharmaceuticals
Synthesis and substance P antagonist activity of naphthimidazolium derivatives.EBI
J Med Chem 35: 1273-9 (1992)
Rochester
Novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles as potential antiallergy agents.EBI
J Med Chem 35: 958-65 (1992)
Warner-Lambert
Syntheses and thymidylate synthase inhibitory activity of the poly-gamma-glutamyl conjugates of N-[5-[N-(3,4-dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl)-N-methylamino ]-2-thenoyl]-L-glutamic acid (ICI D1694) and other quinazoline antifolates.EBI
J Med Chem 35: 859-66 (1992)
Institute Of Cancer Research
Structure-activity relationships associated with 3,4,5-triphenyl-1H-pyrazole-1-nonanoic acid, a nonprostanoid prostacyclin mimetic.EBI
J Med Chem 35: 389-97 (1992)
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and substance P receptor binding activity of androstano[3,2-b]pyrimido[1,2-a]benzimidazoles.EBI
J Med Chem 35: 374-8 (1992)
Rochester
Molecular cloning and expression of a pituitary somatostatin receptor with preferential affinity for somatostatin-28.BDB
Mol Pharmacol 42: 939-46 (1992)
National Institute Of Mental Health
N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.EBI
J Med Chem 35: 4638-9 (1993)
Oregon State University
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.EBI
J Med Chem 35: 4516-25 (1993)
Bristol-Myers Squibb
Synthesis and pharmacological characterization of 2-(4-chloro-3-hydroxyphenyl)ethylamine and N,N-dialkyl derivatives as dopamine receptor ligands.EBI
J Med Chem 35: 4408-14 (1992)
University Of Camerino
Novel piperidine sigma receptor ligands as potential antipsychotic drugs.EBI
J Med Chem 35: 4344-61 (1992)
Dupont Pharmaceuticals
Effect of modification of the basic residues of dynorphin A-(1-13) amide on kappa opioid receptor selectivity and opioid activity.EBI
J Med Chem 35: 4330-3 (1992)
Oregon State University
Synthesis and dopaminergic activity of some 3-(1,2,3,6-tetrahydro-1-pyridylalkyl)indoles. A novel conformational model to explain structure-activity relationships.EBI
J Med Chem 35: 4020-6 (1992)
E. Merck Darmstadt
Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines.EBI
J Med Chem 35: 3845-57 (1992)
Merck Sharp And Dohme Research Laboratories
Characterization of [3H]quinpirole binding to D2-like dopamine receptors in rat brain.BDB
J Pharmacol Exp Ther 262: 929-35 (1992)
Dupont Pharmaceuticals
Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent.EBI
J Med Chem 35: 3081-4 (1992)
American Cyanamid
Oxygen isosteric derivatives of 3-(3-hydroxyphenyl)-N-n-propylpiperidine.EBI
J Med Chem 35: 3045-9 (1992)
Universit£
Synthesis and antihistaminic activity of some thiazolidin-4-ones.EBI
J Med Chem 35: 2910-2 (1992)
Universit£
Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.BDB
Mol Pharmacol 42: 1-5 (1992)
University Of Nebraska
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.EBI
J Med Chem 35: 2712-5 (1992)
Hoechst-Roussel Pharmaceuticals
Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist.BDB
J Pharmacol Exp Ther 262: 383-93 (1992)
University Of North Carolina
Synthesis and antiallergic activity of 11-(aminoalkylidene)-6,11-dihydrodibenz[b,e]oxepin derivatives.EBI
J Med Chem 35: 2074-84 (1992)
Kyowa Hakko Kogyo
Potent and systemically active aminopeptidase N inhibitors designed from active-site investigation.EBI
J Med Chem 35: 1259-66 (1992)
University Of Paris
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.EBI
J Med Chem 35: 1092-101 (1992)
H. Lundbeck
Dopaminergic and serotonergic activities of imidazoquinolinones and related compounds.EBI
J Med Chem 35: 1076-92 (1992)
Upjohn Laboratories
Analgesic dipeptide derivatives. 7. 3,7-Diamino-2-hydroxyheptanoic acid (DAHHA) containing dipeptide analogues of the analgesic compound H-Lys-Trp(Nps)-OMe.EBI
J Med Chem 35: 889-95 (1992)
Instituto De Qu£Mica M£Dica
Binding of typical and atypical antipsychotic agents to transiently expressed 5-HT1C receptors.BDB
J Pharmacol Exp Ther 260: 1361-5 (1992)
Stanford University
Synthesis and alpha-adrenergic activities of 2- and 4-substituted imidazoline and imidazole analogues.EBI
J Med Chem 35: 750-5 (1992)
Ohio State University
Synthesis, cardiac electrophysiology, and beta-blocking activity of novel arylpiperazines with potential as class II/III antiarrhythmic agents.EBI
J Med Chem 35: 743-50 (1992)
Berlex Laboratories
Pyrrole mannich bases as potential antipsychotic agents.EBI
J Med Chem 35: 552-8 (1992)
R. W. Johnson Pharmaceutical Research Institute
Synthesis of halogenated trimetoquinol derivatives and evaluation of their beta-agonist and thromboxane A2 (TXA2) antagonist activities.EBI
J Med Chem 35: 466-79 (1992)
Ohio State University
Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells.BDB
J Pharmacol Exp Ther 260: 576-80 (1992)
Mayo Clinic
Preparation and opioid activity of analogues of the analgesic dipeptide 2,6-dimethyl-L-tyrosyl-N-(3-phenylpropyl)-D-alaninamide.EBI
J Med Chem 35: 223-33 (1992)
G.D. Searle And
Novel cAMP PDE III inhibitors: 1,6-naphthyridin-2(1H)-ones.EBI
J Med Chem 35: 4858-65 (1992)
Sterling Winthrop Pharmaceuticals Research Division
Selective, centrally acting serotonin 5-HT2 antagonists. 2. Substituted 3-(4-fluorophenyl)-1H-indoles.EBI
J Med Chem 35: 4823-31 (1993)
H. Lundbeck
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.EBI
J Med Chem 35: 4813-22 (1993)
H. Lundbeck
Para-substituted Phe3 deltorphin analogues: enhanced selectivity of halogenated derivatives for delta opioid receptor sites.EBI
J Med Chem 35: 4651-7 (1993)
University Of Ferrara
O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay.EBI
J Med Chem 35: 4589-94 (1993)
University Of Washington
Incorporation of a novel conformationally restricted tyrosine analog into a cyclic, delta opioid receptor selective tetrapeptide (JOM-13) enhances delta receptor binding affinity and selectivity.EBI
J Med Chem 35: 4498-500 (1992)
University Of Michigan
Opioid agonist and antagonist activities of morphindoles related to naltrindole.EBI
J Med Chem 35: 4325-9 (1992)
University Of Minnesota
omega-[(4,6-Diphenyl-2-pyridyl)oxy]alkanoic acid derivatives: a new family of potent and orally active LTB4 antagonists.EBI
J Med Chem 35: 4315-24 (1992)
Centre De Recherche De Vitry-Alfortville
omega-[(4-Phenyl-2-quinolyl)oxy]alkanoic acid derivatives: a new family of potent LTB4 antagonists.EBI
J Med Chem 35: 4306-14 (1992)
Centre De Recherche De Vitry-Alfortville
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.EBI
J Med Chem 35: 4253-5 (1992)
Rhone-Poulenc Rorer Central Research
L-thymidine is phosphorylated by herpes simplex virus type 1 thymidine kinase and inhibits viral growth.EBI
J Med Chem 35: 4214-20 (1992)
Istituto Di Genetica Biochimica Ed Evoluzionistica
Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists.EBI
J Med Chem 35: 4195-204 (1992)
Glaxo Group Research
The first mechanism-based inactivators for angiotensin-converting enzyme.EBI
J Med Chem 35: 4175-9 (1992)
Baxter Diagnostics
Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists.EBI
J Med Chem 35: 4092-7 (1992)
Centre De Neurochimie Du Cnrs
Delta opioid antagonist activity and binding studies of regioisomeric isothiocyanate derivatives of naltrindole: evidence for delta receptor subtypes.EBI
J Med Chem 35: 4086-91 (1992)
University Of Minnesota
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.EBI
J Med Chem 35: 4039-44 (1992)
Hokuriku University
Conformationally restricted deltorphin analogues.EBI
J Med Chem 35: 3956-61 (1992)
Clinical Research Institute Of Montreal
A new class of high affinity ligands for the neurokinin A NK2 receptor: psi (CH2NR) reduced peptide bond analogues of neurokinin A4-10.EBI
J Med Chem 35: 3949-55 (1992)
Marion Merrell Dow Research Institute
Orally active, nonpeptide oxytocin antagonists.EBI
J Med Chem 35: 3919-27 (1992)
Merck Research Laboratories
Development of a novel class of cyclic hexapeptide oxytocin antagonists based on a natural product.EBI
J Med Chem 35: 3905-18 (1992)
Merck Research Laboratories
Development of a novel series of styrylquinoline compounds as high-affinity leukotriene D4 receptor antagonists: synthetic and structure-activity studies leading to the discovery of (+-)-3-[[[3-[2-(7-chloro-2-quinolinyl)-(E)-ethenyl]phenyl][[3- (dimethylamino)-3-oxopropyl]thio]methyl]thio]propionicEBI
J Med Chem 35: 3832-44 (1992)
Merck Frosst Centre For Therapeutic Research
Cloning of a novel somatostatin receptor, SSTR3, coupled to adenylylcyclase.BDB
J Biol Chem 267: 20422-8 (1992)
University Of Chicago
Antagonistic properties are shifted back to agonistic properties by further N-terminal shortening of pituitary adenylate-cyclase-activating peptides in human neuroblastoma NB-OK-1 cell membranes.BDB
Eur J Biochem 208: 815-9 (1992)
UniversitÉ
3-Phenyl-4-hydroxyquinolin-2(1H)-ones: potent and selective antagonists at the strychnine-insensitive glycine site on the N-methyl-D-aspartate receptor complex.EBI
J Med Chem 35: 3423-5 (1992)
Eli Lilly
Reversible inhibitors of the gastric (H+/K+)-ATPase. 3. 3-substituted-4-(phenylamino)quinolines.EBI
J Med Chem 35: 3413-22 (1992)
Smithkline Beecham Pharmaceuticals R&D
Receptor occupancy and adenylate cyclase activation in AR 4-2J rat pancreatic acinar cell membranes by analogs of pituitary adenylate cyclase-activating peptides amino-terminally shortened or modified at position 1, 2, 3, 20, or 21.BDB
Mol Pharmacol 42: 347-55 (1992)
Universit&Acute
A Strategy for Identifying Novel, Mechanistically Unique Inhibitors of Topoisomerase IEBI
J Nat Prod 55: 401-413 (1992)
TBA
Design of a functional hexapeptide antagonist of endothelin.EBI
J Med Chem 35: 3301-3 (1992)
Warner-Lambert
Benzothiazole hydroxy ureas as inhibitors of 5-lipoxygenase: use of the hydroxyurea moiety as a replacement for hydroxamic acid.EBI
J Med Chem 35: 3180-3 (1992)
R. W. Johnson Pharmaceutical Research Institute
Omega-[(omega-arylalkyl)thienyl]alkanoic acids: from specific LTA4 hydrolase inhibitors to LTB4 receptor antagonists.EBI
J Med Chem 35: 3170-9 (1992)
Centre De Recherche De Vitry-Alfortville
Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor.EBI
J Med Chem 35: 3058-66 (1992)
Upjohn
Quantitative structure-activity relationships of N2-phenylguanines as inhibitors of herpes simplex virus thymidine kinases.EBI
J Med Chem 35: 2979-83 (1992)
University Of Massachusetts Medical School
Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors.EBI
J Med Chem 35: 2970-8 (1992)
Zambeletti Research Laboratories
Analogs of the delta opioid receptor selective cyclic peptide [2-D-penicillamine,5-D-penicillamine]-enkephalin: 2',6'-dimethyltyrosine and Gly3-Phe4 amide bond isostere substitutions.EBI
J Med Chem 35: 2928-38 (1992)
G.D. Searle And
Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluation, and radiochemistry of [125I]-6 beta-iodoEBI
J Med Chem 35: 2826-35 (1992)
National Institute Of Diabetes And Digestive And Kidney Diseases
Enantiomeric N-substituted N-normetazocines: a comparative study of affinities at sigma, PCP, and mu opioid receptors.EBI
J Med Chem 35: 2812-8 (1992)
Research Triangle Institute
Inhibition of collagenase by aranciamycin and aranciamycin derivatives.EBI
J Med Chem 35: 2768-71 (1992)
Technical University Of Denmark
Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility.EBI
J Med Chem 35: 2688-96 (1992)
Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains.EBI
J Med Chem 35: 2672-87 (1992)
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel inhibitors of prolyl 4-hydroxylase. 3. Inhibition by the substrate analogue N-oxaloglycine and its derivatives.EBI
J Med Chem 35: 2652-8 (1992)
Ici Pharmaceuticals Group
Methoxytetrahydropyrans. A new series of selective and orally potent 5-lipoxygenase inhibitors.EBI
J Med Chem 35: 2600-9 (1992)
Ici Pharmaceuticals Group
Multiple histamine receptors: properties and functional characteristics.BDB
Biochem Soc Trans 20: 122-5 (1992)
Queen'S Medical Centre
Structural requirements for the occupancy of pituitary adenylate-cyclase-activating-peptide (PACAP) receptors and adenylate cyclase activation in human neuroblastoma NB-OK-1 cell membranes. Discovery of PACAP(6-38) as a potent antagonist.BDB
Eur J Biochem 207: 239-46 (1992)
UniversitÉ
Comparison of antagonist and agonist binding to the leukotriene B4 receptor intact human polymorphonuclear neutrophils (PMN).BDB
J Pharmacol Exp Ther 262: 80-9 (1992)
Ciba-Geigy
Characterization of a novel 5-HT4 receptor antagonist of the azabicycloalkyl benzimidazolone class: DAU 6285.BDB
Naunyn Schmiedebergs Arch Pharmacol 345: 264-9 (1992)
Centre De Pharmacologie-Endocrinologie (Montpellier, France)
Ring substituted and other conformationally constrained tyrosine analogues of [D-Pen2,D-Pen5]enkephalin with delta opioid receptor selectivity.EBI
J Med Chem 35: 2384-91 (1992)
University Of Arizona
Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.EBI
J Med Chem 35: 2374-84 (1992)
University Of Washington
Selective reversible and irreversible ligands for the kappa opioid receptor.EBI
J Med Chem 35: 2243-7 (1992)
National Taiwan University
Synthesis and receptor binding properties of fluoro- and iodo-substituted high affinity sigma receptor ligands: identification of potential PET and SPECT sigma receptor imaging agents.EBI
J Med Chem 35: 2221-30 (1992)
National Institute Of Diabetes And Digestive And Kidney Diseases
Structure-activity study of hCGRP8-37, a calcitonin gene-related peptide receptor antagonist.EBI
J Med Chem 35: 2163-8 (1992)
Université
Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency- and solubility-enhancing modifications.EBI
J Med Chem 35: 2139-42 (1992)
TBA
A novel probe for the cannabinoid receptor.EBI
J Med Chem 35: 2065-9 (1992)
Hebrew University
Synthesis and structure-activity relationships of a series of novel benzopyran-containing platelet activating factor antagonists.EBI
J Med Chem 35: 2055-61 (1992)
Abbott Laboratories
Spiropiperidines as high-affinity, selective sigma ligands.EBI
J Med Chem 35: 2033-9 (1992)
Merck Sharp And Dohme Research Laboratories
Benz[f]isoquinoline analogues as high-affinity sigma ligands.EBI
J Med Chem 35: 2025-33 (1992)
Merck Sharp And Dohme Research Laboratories
Akuammine and Dihydroakuammine, Two Indolomonoterpene Alkaloids Displaying Affinity for Opioid ReceptorsEBI
J Nat Prod 55: 380-384 (1992)
TBA
Reversible inhibitors of the gastric (H+/K+)-ATPase. 2. 1-Arylpyrrolo[3,2-c]quinolines: effect of the 4-substituent.EBI
J Med Chem 35: 1845-52 (1992)
Smithkline Beecham Pharmaceuticals R&D
Substitution on the Phe3 aromatic ring in cyclic delta opioid receptor-selective dermorphin/deltorphin tetrapeptide analogues: electronic and lipophilic requirements for receptor affinity.EBI
J Med Chem 35: 1535-41 (1992)
University Of Michigan
(Aminoalkoxy)chromones. Selective sigma receptor ligands.EBI
J Med Chem 35: 1526-35 (1992)
Nova Pharmaceutical
Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity.EBI
J Med Chem 35: 1521-5 (1992)
Harvard Medical School
Endothelin: a new challenge.EBI
J Med Chem 35: 1493-508 (1992)
Warner-Lambert
Molecular cloning and functional characterization of a human 5-HT1B serotonin receptor: a homologue of the rat 5-HT1B receptor with 5-HT1D-like pharmacological specificity.BDB
Biochem Biophys Res Commun 184: 752-9 (1992)
Veterans Affairs Medical Center
Development of 2,3-dihydro-6-(3-phenoxypropyl)-2-(2-phenylethyl)-5-benzofuranol (L-670,630) as a potent and orally active inhibitor of 5-lipoxygenase.EBI
J Med Chem 35: 1299-318 (1992)
Merck Frosst Centre For Therapeutic Research
Stereospecificity of amino acid side chains in deltorphin defines binding to opioid receptors.EBI
J Med Chem 35: 1222-7 (1992)
National Institute Of Environmental Health Sciences
(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate.EBI
J Med Chem 35: 1049-57 (1992)
Byk Gulden Pharmaceuticals
Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors.EBI
J Med Chem 35: 1009-18 (1992)
Universit£
Development of high-affinity 5-HT3 receptor antagonists. 1. Initial structure-activity relationship of novel benzamides.EBI
J Med Chem 35: 895-903 (1992)
Rh£Ne-Poulenc Rorer Central Research
Novel inhibitors of prolyl 4-hydroxylase. 2. 5-Amide substituted pyridine-2-carboxylic acids.EBI
J Med Chem 35: 804-7 (1992)
Ici Pharmaceuticals Group
Novel inhibitors of prolyl 4-hydroxylase.EBI
J Med Chem 35: 800-4 (1992)
Ici Pharmaceuticals Group
Benzazepinone calcium channel blockers. 4. Structure-activity overview and intracellular binding site.EBI
J Med Chem 35: 780-93 (1992)
Bristol-Myers Squibb Pharmaceutical Research Institute
Systemic analgesic activity and delta-opioid selectivity in [2,6-dimethyl-Tyr1,D-Pen2,D-Pen5]enkephalin.EBI
J Med Chem 35: 684-7 (1992)
Searle Research And Development
3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.EBI
J Med Chem 35: 620-8 (1992)
Syntex Research
New kappa-receptor agonists based upon a 2-[(alkylamino)methyl]piperidine nucleus.EBI
J Med Chem 35: 490-501 (1992)
Glaxo Group Research
2-[(2-pyridylmethyl)sulfinyl]-1H-thieno[3,4-d]imidazoles. A novel class of gastric H+/K(+)-ATPase inhibitors.EBI
J Med Chem 35: 438-50 (1992)
Hoechst
Pharmacological characterization of a novel muscarinic partial agonist, YM796, in transfected cells expressing the m1 or m2 muscarinic receptor gene.BDB
Life Sci 50: 355-63 (1992)
University Of Arizona
Structure-function studies of peptides inhibiting the ribonucleotide reductase activity of herpes simplex virus type I.EBI
J Med Chem 35: 346-50 (1992)
Notre-Dame Hospital Research
Substituted 4,6-diaminoquinolines as inhibitors of C5a receptor binding.EBI
J Med Chem 35: 252-8 (1992)
Merck Sharp And Dohme Research Laboratories
Beta-proline analogues as agonists at the strychnine-sensitive glycine receptor.EBI
J Med Chem 35: 233-41 (1992)
Warner-Lambert
Synthesis and antibacterial activity of new tetracyclic quinolone antibacterials.EBI
J Med Chem 35: 94-9 (1992)
Kanebo
Synthesis, antinociceptive activity, and opioid receptor profiles of substituted trans-3-(decahydro- and octahydro-4a-isoquinolinyl)phenols.EBI
J Med Chem 35: 48-56 (1992)
Glaxo Group Research
Synthesis, characterization, and biological evaluation of a novel class of N-(arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamines: structural requirements and binding affinity at the sigma receptor.EBI
J Med Chem 35: 38-47 (1992)
National Institute Of Diabetes And Digestive And Kidney Diseases
Scoparic acid A, a beta-glucuronidase inhibitor from Scoparia dulcis.EBI
J Nat Prod 55: 1748-55 (1992)
Toyama Medical And Pharmaceutical University
Phospholipase A2 inhibitors from marine organisms.EBI
J Nat Prod 55: 1701-17 (1992)
University Of California-San Diego
Discovery of a potent substance P antagonist: recognition of the key molecular determinant.EBI
J Med Chem 35: 4911-3 (1993)
Pfizer
Potential anti-AIDS naphthalenesulfonic acid derivatives. Synthesis and inhibition of HIV-1 induced cytopathogenesis and HIV-1 and HIV-2 reverse transcriptase activities.EBI
J Med Chem 35: 4846-53 (1992)
University Of Illinois At Chicago
Gonadotropin-releasing hormone antagonists with N omega-triazolylornithine, -lysine, or -p-aminophenylalanine residues at positions 5 and 6.EBI
J Med Chem 35: 4270-8 (1992)
Salk Institute
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.BDB
J Med Chem 35: 3792-802 (1992)
Merck Research Laboratories
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1 specific reverse transcriptase inhibitors. 1. Phthalimidoalkyl and -alkylamino analogues.BDB
J Med Chem 35: 3784-91 (1992)
Merck Research Laboratories
Conformationally rigid amphetamine analogs as inhibitors of monoamine uptake by brain synaptosomes.EBI
J Med Chem 19: 725-7 (1976)
TBA
Novel bis(benzamidino) compounds with an aromatic central link. Inhibitors of thrombin, pancreatic kallikrein, trypsin, and complement.EBI
J Med Chem 19: 634-9 (1976)
TBA

BDB Curated by BindingDB
EBI Curated by ChEMBL