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Properties of [3H]haloperidol and [3H]dopamine binding associated with dopamine receptors in calf brain membranes.

Mol Pharmacol 12: 800-12 (1976)

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Synthesis and properties of 2-S-(N,N-dialkylamino)ethyl)thio-1,3,2-dioxaphosphorinane 2-oxide and of the corresponding quaternary derivatives as potential nontoxic antiglaucoma agents.

J Med Chem 19: 810-3 (1976)

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Synthesis and biological action of two glucocorticoid alkylating agents.

J Med Chem 20: 1134-9 (1978)

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Proteinase inhibitors. I. Inhibitors of elastase.

J Med Chem 20: 1464-8 (1977)

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Synthesis and evaluation of alpha-hydroxythiol esters as antitumor agents and glyoxalase I inhibitors.

J Med Chem 20: 1239-42 (1977)

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Stereochemical studies on medicinal agents. 23. Synthesis and biological evaluation of 6-amino derivatives of naloxone and naltrexone.

J Med Chem 20: 1100-2 (1977)

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New inhibitors of steroid 11beta-hydroxylase. Structure--activity relationship studies of metyrapone-like compounds.

J Med Chem 20: 762-6 (1977)

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Synthesis and structure-activity relationships of bestatin analogues, inhibitors of aminopeptidase B.

J Med Chem 20: 510-5 (1977)

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Inhibition of histidine decarboxylase. Derivatives of histidine.

J Med Chem 20: 506-9 (1977)

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Influence of side-chain structure of aliphatic amino acids on binding to isoleucyl-tRNA synthetase from Escherichia coli MRE 600.

Eur J Biochem 66: 147-55 (1976)

Gesellschaft Fur Molekularbiolische Forschung Mbh

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Effects of thiophene analogues of chloroamphetamines on central serotonergic mechanisms.

J Med Chem 21: 978-81 (1979)

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Prodrugs of 9-beta-D-arabinofuranosyladenine. 1. Synthesis and evaluation of some 5'-(O-acyl) derivatives.

J Med Chem 21: 1218-21 (1979)

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Use of adenine nucleotide derivatives to assess the potential of exo-active-site-directed reagents as species- or isozyme-specific enzyme inactivators. 2. Isozyme-specific inactivation of a mammalian enzyme and its significance in the possible design of fetal isozyme targeted antineoplastic agents.

J Med Chem 21: 1137-40 (1979)

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Structure-activity relationships for the inhibition of acrosin by benzamidine derivatives.

J Med Chem 21: 1132-6 (1979)

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Synthesis and biochemical evaluation of inhibitors of estrogen biosynthesis.

J Med Chem 21: 1007-11 (1979)

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Diarylamidine derivatives with one or both of the aryl moieties consisting of an indole or indole-like ring. Inhibitors of arginine-specific esteroproteases.

J Med Chem 21: 613-23 (1978)

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Inactivation of trypsin-like proteases by sulfonylation. Variation of positively charged group and inhibitor length.

J Med Chem 21: 456-9 (1978)

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Analogues of ornithine as inhibitors of ornithine decarboxylase. New deductions concerning the topography of the enzyme's active site.

J Med Chem 21: 50-5 (1978)

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Hypolipidemic activity of 5-aryl-3-methylvaleric acid derivatives.

J Med Chem 20: 1705-8 (1978)

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Potent reversible anticholinesterase agents. Bis- and mono-N-substituted benzoquinolinium halides.

J Med Chem 20: 1617-23 (1978)

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Vitamin B6 antagonists obtained by replacing or modifying the 2-methyl group.

J Med Chem 20: 745-9 (1977)

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4-Halovinyl- and 4-ethynyl-4-deformylpyridoxal derivatives and related analogues as potentially irreversible antagonists of vitamin B6.

J Med Chem 20: 567-72 (1977)

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Inhibition of acetylcholinesterase by thiamine. A structure-function study.

J Med Chem 20: 161-4 (1977)

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Antagonists of vitamin B6. Simultaneous and stepwise modification of the 2 and 4 positions.

J Med Chem 20: 1-5 (1977)

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Synthesis and biological evaluation of 9,11-azo-13-oxa-15-hydroxyprostanoic acid, a potent inhibitor of platelet aggregation.

J Med Chem 22: 1402-8 (1980)

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Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 5. Conformationally mobile analogues derived by furan ring opening.

J Med Chem 22: 1347-54 (1980)

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4-(p-Bromophenyl)-4-(dimethylamino)-1-phenethylcyclohexanol, an extremely potent respresentative of a new analgesic series.

J Med Chem 22: 1157-8 (1979)

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Synthesis and biological properties of N2-substituted spin-labeled analogues of actinomycin D.

J Med Chem 22: 1051-5 (1979)

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Synthesis and antiestrogenic activity of [3,4-dihydro-2-(4-methoxyphenyl)-1-naphthalenyl][4-[2-(1-pyrrolidinyl)ethoxy]-phenyl]methanone, methanesulfonic acid salt.

J Med Chem 22: 962-6 (1979)

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Evidence for two types of binding of 3H-gaba and 3H-muscimol in rat cerebral cortex and cerebellum.

Life Sci 24: 1849-54 (1979)

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Design of species- or isozyme-specific enzyme inhibitors. 1. Effect of thymidine substituents on affinity for the thymidine site of hamster cytoplasmic thymidine kinase.

J Med Chem 22: 621-31 (1979)

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trans-5-(3,3,3-Trifluoro-1-propenyl-)-2'-deoxyuridylate: a mechanism-based inhibitor of thymidylate synthetase.

J Med Chem 22: 339-40 (1979)

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Characterization of the binding of [3H]muscimol, a potent gamma-aminobutyric acid agonist, to rat brain synaptosomal membranes using a filtration assay.

J Neurochem 32: 713-8 (1979)

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Inhibition of gastric acid secretion by 1,8-naphthyridin-2(1H)-ones.

J Med Chem 22: 301-6 (1979)

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Cyclic amidine inhibitors of indolamine N-methyltransferase.

J Med Chem 22: 237-47 (1979)

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Coenzyme--substrate adducts as inhibitors of mouse liver 3,4-dihydroxyphenylalanine decarboxylase.

J Med Chem 22: 233-7 (1979)

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Phosphonate analogue of 2'-deoxy-5-fluorouridylic acid.

J Med Chem 22: 109-11 (1979)

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Inhibition of Lactobacillus casei thymidylate synthetase by 5-substituted 2'-deoxyuridylates. Preliminary quantitative structure-activity relationship.

J Med Chem 20: 1469-73 (1977)

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Methotrexate analogues. 9. Synthesis and biological properties of some 8-alkyl-7,8-dihydro analogues.

J Med Chem 20: 1323-7 (1977)

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Thymidylate synthetase inhibitors. Synthesis of N-substituted 5-aminomethyl-2'-deoxyuridine 5'-phosphates.

J Med Chem 20: 669-73 (1977)

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A manual method for applying the Hansch approach to drug design.

J Med Chem 20: 463-9 (1977)

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Quantitative structure-activity relationships of antimalarial and dihydrofolate reductase inhibition by quinazolines and 5-substituted benzyl-2,4-diaminopyrimidines.

J Med Chem 20: 96-102 (1977)

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Histamine H1 receptors identified in mammalian brain membranes with [3H]mepyramine.

Proc Natl Acad Sci U S A 75: 6290-4 (1978)

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Design of species- or isozyme-specific enzyme inhibitors. 3. Species and isozymic differences between mammalian and bacterial adenylate kinases in substituent tolerance in an enzyme-substrate complex.

J Med Chem 22: 1529-32 (1980)

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Synthesis and biological properties of 2-, 5-, and 6-fluoronorepinephrines.

J Med Chem 22: 1493-7 (1979)

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3-Substituted pyrazole derivatives as inhibitors and inactivators of liver alcohol dehydrogenase.

J Med Chem 22: 356-9 (1979)

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Paradoxical effects of N-cyanoalkyl substituents upon the activities of several classes of opioids.

J Med Chem 22: 328-31 (1979)

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Deoxymorphines: role of the phenolic hydroxyl in antinociception and opiate receptor interactions.

J Med Chem 22: 256-9 (1979)

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Conformation of 2,9-dimethyl-3'-hydroxy-5-phenyl-6,7-genzomorphan and its relation to other analgetics and enkephalin.

J Med Chem 21: 600-6 (1978)

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Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.

J Med Chem 21: 415-22 (1978)

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Studies in the (+)-morphinan series. 5. Synthesis and biological properties of (+)-naloxone.

J Med Chem 21: 398-400 (1978)

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Synthesis of beta-spiro[pyrrolidinoindolines], their binding to the glycine receptor, and in vivo biological acitivity.

J Med Chem 20: 1448-51 (1977)

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3-Hydroxy-17-aralkylmorphinans as potential opiate receptor-site-directed alkylating agents.

J Med Chem 20: 1020-4 (1977)

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Inhibition of squalene synthetase by farnesyl pyrophosphate analogues.

J Med Chem 20: 243-9 (1977)

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Synthesis and biological properties of some spin-labeled 9-aminoacridines.

J Med Chem 19: 994-8 (1976)

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Inhibition of four human serine proteases by substituted benzamidines.

J Med Chem 21: 1202-7 (1979)

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Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.

J Med Chem 22: 1247-57 (1979)

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5-Cyano-2'-deoxyuridine 5'-phosphate: a potent competitive inhibitor of thymidylate synthetase.

J Med Chem 22: 1137-9 (1979)

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Synthesis and biological activity of 8-oxadihydropteridines.

J Med Chem 22: 741-3 (1979)

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Synthesis of 5-selenium-substituted uracil derivatives. Inhibition of thymidylate synthetase by 5-hydroseleno-2'-deoxyuridylate.

J Med Chem 22: 618-21 (1979)

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N-(2-Cyanoethyl) derivatives of meperidine, ketobemidone, and a potent 6,7-benzomorphan.

J Med Chem 22: 889-90 (1979)

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Methotrexate analogues. 12. Synthesis and biological properties of some aza homologues.

J Med Chem 22: 869-74 (1979)

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Enzyme affinity of the 5,6-dihydro derivatives of the substrate and product of thymidylate synthetase catalysis.

J Med Chem 22: 319-21 (1979)

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Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.

J Med Chem 21: 101-6 (1978)

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Ultraviolet photoelectron spectroscopy of cyclic amidines. 1. Electronic structure of some alpha-adrenergic benzylimidazolines.

J Med Chem 22: 1290-5 (1979)

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Absolute configuration of glycerol derivatives. 7. Enantiomers of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]methyl]-1,4-benzodioxane (WB-4101), a potent competitive alpha-adrenergic antagonist.

J Med Chem 22: 1125-7 (1979)

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Nicotinamide adenine dinucleotide phosphate-decanaldehyde adduct as an inhibitor of beef brain NADP-linked aldehyde reductase.

J Med Chem 22: 1011-4 (1979)

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Binding characteristics of 3H-prazosin to rat brain alpha-adrenergic receptors.

Eur J Pharmacol 55: 323-6 (1979)

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Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine.

J Med Chem 21: 952-7 (1978)

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Nondepressant beta-adrenergic blocking agents. 1. Substituted 3-amino-1-(5,6,7,8-tetrahydro-1-naphthoxy)-2-propanols.

J Med Chem 21: 913-22 (1978)

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Stereoelectronic factors in the binding of substrate analogues and inhibitors to purine nucleoside phosphorylase isolated from human erythrocytes.

J Med Chem 21: 877-82 (1979)

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Antidepressant agents. 9. 3,3-Diphenylcyclobutylamines, a new class of central stimulants.

J Med Chem 21: 78-82 (1978)

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Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding.

Proc Natl Acad Sci U S A 74: 3805-9 (1977)

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Binding characteristics of a radiolabeled agonist and antagonist at central nervous system alpha noradrenergic receptors.

Mol Pharmacol 13: 454-73 (1977)

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Absolute configuration of glycerol derivatives. 4. Synthesis and pharmacological activity of chiral 2-alkylaminomethylbenzodioxans, competitive alpha-adrenergic antagonists.

J Med Chem 20: 880-5 (1977)

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Beta adrenergic receptor binding in membrane preparations from mammalian brain.

Mol Pharmacol 12: 568-80 (1976)

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Alpha-noradrenergic receptor binding in mammalian brain: differential labeling of agonist and antagonist states.

Life Sci 19: 69-76 (1976)

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Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines.

J Med Chem 19: 291-6 (1976)

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Conformationally restricted analogs of histamine H1 receptor antagonists: trans and cis-1-benzyl-3-dimethylamino-6-phenylpiperidine.

J Med Chem 19: 117-22 (1976)

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