Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase

被引：36

作者：

Shankaran, K

Donnelly, KL

Shah, SK

Guthikonda, RN

MacCoss, M

Humes, JL

Pacholok, SG

Grant, SK

Kelly, TM

Wong, KK

机构：

[1] Merck Res Lab, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Lab, Dept Immunol & Inflammat, Rahway, NJ 07065 USA

[3] Merck Res Lab, Dept Enzymol, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 17期

关键词：

NOS; pyrrolidin-2-imine; 1,3-thiazolidin-2-imine;

D O I：

10.1016/j.bmcl.2004.06.033

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Syntheses and evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase (NOS) are discussed. An extensive SAR was established for pyrrolidin-2-imines class of compounds. The amidines came out as the most potent inhibitors in addition to displaying selectivity. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：4539 / 4544

页数：6

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