Rational design and synthesis of a novel, selective class of thrombin inhibitors: P-1-argininal derivatives incorporating P-3-P-4 quaternary lactam dipeptide surrogates

被引：21

作者：

Semple, JE

Minami, NK

Tamura, SY

Brunck, TK

Nutt, RF

Ripka, WC

机构：

[1] Department of Medicinal Chemistry, Corvas International, Inc., San Diego, CA 92121

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(97)00446-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

SAR and molecular modeling investigations on the potent and selective thrombin inhibitor 1b (CVS 1578) and related serine protease inhibitors led to the design of series 2a-g, featuring quaternary alpha-amino-alpha-benzyl-lactam scaffolds that serve as novel P-3-P-4 dipeptide mimics. The design, synthesis, and biological activity of these targets are presented. (C) 1997 Elsevier Science Ltd.

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页码：2421 / 2426

页数：6

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