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

BG Shearer, S Lee, JA Oplinger, LW Frick…

文献索引：Shearer, Barry G.; Lee, Shuliang; Oplinger, Jeffrey A.; Frick, Lloyd W.; Garvey, Edward P.; Furfine, Eric S. Journal of Medicinal Chemistry, 1997 , vol. 40, # 12 p. 1901 - 1905

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被引用次数: 70

摘要

S-Ethyl N-phenylisothiourea (4) has been found to be a potent inhibitor of both the human constitutive and inducible isoforms of nitric oxide synthase. A series of substituted N- phenylisothiourea analogues was synthesized to investigate the structure-activity relationship of this class of inhibitor. Each analogue was evaluated for human isoform selectivity. One analogue, S-ethyl N-[4-(trifluoromethyl) phenyl] isothiourea (39), exhibited ...