Substituted N-phenylisothioureas: Potent inhibitors of human nitric oxide synthase with neuronal isoform selectivity

Journal of Medicinal Chemistry

Volumn 40, Issue 12, 1997, Pages 1901-1905

  Shearer, Barry G ^a,b   Lee, Shuliang ^a,b   Oplinger, Jeffrey A ^a,b   Frick, Lloyd W ^a,c   Garvey, Edward P ^a,b   Furfine, Eric S ^a,b  

^a GLAXOSMITHKLINE   (United States)

^b Glaxo Wellcome R and D ^*

^c Div of Bioanalysis and Drug Metab

Author keywords

[No Author keywords available]

Indexed keywords

ANTIOXIDANT; NITRIC OXIDE SYNTHASE INHIBITOR; S ETHYL N [4 (TRIFLUOROMETHYL)PHENYL]ISOTHIOUREA; S ETHYL N PHENYLISOTHIOUREA; UNCLASSIFIED DRUG;

ANTIOXIDANT ACTIVITY; ARTICLE; BINDING COMPETITION; COMPETITIVE INHIBITION; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; STRUCTURE ACTIVITY RELATION;

ANIMALS; ARGININE; BINDING, COMPETITIVE; BRAIN; CITRULLINE; ENZYME INHIBITORS; HUMANS; ISOENZYMES; MOLECULAR STRUCTURE; NEURONS; NITRIC OXIDE SYNTHASE; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; THIOUREA;

EID: 0030979486     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm960785c     Document Type: Article

References (25)

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17. The weak inhibition of rat iNOS by S-methyl N-phenylisothiourea was reported during the course of this work: Southan, G. J.; Szabo, C.; Thiemermann, C. Isothioureas: Potent Inhibitors of Nitric Oxide Synthases with Variable Isoform Selectivity. Br. J. Pharmacol. 1995, 111, 510-516.
18. (18) The following patents describing other classes of substitututed N-phenyl derived NOS inhibitors appeared after completion of this work: Cowart, M.; Kerwin, J. F. 2-Nitroaryl and 2-Cyanoaryl Compounds as Regulators of Nitric Oxide Synthase. WO 9412163. MacDonald, J. E.; Gentile, R. J.; Murray, R. J. Guanidine Derivatives Useful in Therapy. WO 9421621. Gentile, R. J.; Murray, R. J.; MacDonald, J. E. Amidine Derivatives with Nitric Oxide Synthetase Activities. WO 9505363.
19. The following patents describing other classes of substitututed N-phenyl derived NOS inhibitors appeared after completion of this work: Cowart, M.; Kerwin, J. F. 2-Nitroaryl and 2-Cyanoaryl Compounds as Regulators of Nitric Oxide Synthase. WO 9412163. MacDonald, J. E.; Gentile, R. J.; Murray, R. J. Guanidine Derivatives Useful in Therapy. WO 9421621. Gentile, R. J.; Murray, R. J.; MacDonald, J. E. Amidine Derivatives with Nitric Oxide Synthetase Activities. WO 9505363.
20. The following patents describing other classes of substitututed N-phenyl derived NOS inhibitors appeared after completion of this work: Cowart, M.; Kerwin, J. F. 2-Nitroaryl and 2-Cyanoaryl Compounds as Regulators of Nitric Oxide Synthase. WO 9412163. MacDonald, J. E.; Gentile, R. J.; Murray, R. J. Guanidine Derivatives Useful in Therapy. WO 9421621. Gentile, R. J.; Murray, R. J.; MacDonald, J. E. Amidine Derivatives with Nitric Oxide Synthetase Activities. WO 9505363.
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