Substituted 2-iminopiperidines as inhibitors of human nitric oxide synthase isoforms

…, JR Connor, MG Currie, KF Fok, TJ Hagen…

文献索引：Webber, R. Keith; Metz, Suzanne; Moore, William M.; Connor, Jane R.; Currie, Mark G.; Fok, Kam F.; Hagen, Timothy J.; Hansen Jr., Donald W.; Jerome, Gina M.; Manning, Pamela T.; Pitzele, Barnett S.; Toth, Mihaly V.; Trivedi, Mahima; Zupec, Mark E.; Siong Tjoeng Journal of Medicinal Chemistry, 1998 , vol. 41, # 1 p. 96 - 101

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被引用次数: 61

摘要

A series of analogues of 2-iminopiperidine have been prepared and shown to be potent inhibitors of the human nitric oxide synthase (NOS) isoforms. Methyl substitutions on the 4- position (3) or 4-and 6-positions (8) afforded the most potent analogues. These compounds exibited IC50 values of 0.1 and 0.08 μM, respectively, for hiNOS inhibition. Substitution with cyclohexylmethyl at the 6-position (13) afforded an inhibitor that showed the best ...