Thrombin active site inhibitors: Chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues

被引：13

作者：

Das, J ^{[1
]}

Kimball, SD ^{[1
]}

Reid, JA ^{[1
]}

Wang, TC ^{[1
]}

Lau, WF ^{[1
]}

Roberts, DGM ^{[1
]}

Seiler, SM ^{[1
]}

Schumacher, WA ^{[1
]}

Ogletree, ML ^{[1
]}

机构：

[1] Bristol Myers Squibb Pharmaceut Inst, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(01)00664-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of structurally novel small molecule inhibitors of human alpha -thrombin was prepared to elucidate their structure-activity relationships (SAR), selectivity and activity in vivo. BMS-189090 (5) is identified as a potent, selective, and reversible inhibitor of human alpha -thrombin that is efficacious in vivo in a mice lethality model, and in inhibiting both arterial and venous thrombosis in a rat model. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：41 / 44

页数：4

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