Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors

被引：13

作者：

Arnaiz, DO ^{[1
]}

Zhao, ZS ^{[1
]}

Liang, A ^{[1
]}

Trinh, L ^{[1
]}

Whitlow, M ^{[1
]}

Koovakkat, SK ^{[1
]}

Shaw, KJ ^{[1
]}

机构：

[1] Berlex Biosci, Discovery Res, Richmond, CA 94804 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(00)00138-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of indole and carbazole based inhibitors of factor Xa (FXa) has been investigated. The most potent compound inhibits FXa with a K-i of 0.2 nM and has 900- and 750-fold selectivity over thrombin and trypsin, respectively. (C) 2000 Elsevier Science Ltd. All rights reserved.

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页码：957 / 961

页数：5

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