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

作者信息

Das Jagabandhu, Kimball S David, Reid Joyce A, Wang Tammy C, Lau Wan F, Roberts Daniel G M, Seiler Steven M, Schumacher William A, Ogletree Martin L

机构信息

Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA.

出版信息

Bioorg Med Chem Lett. 2002 Jan 7;12(1):41-4. doi: 10.1016/s0960-894x(01)00664-3.

DOI:10.1016/s0960-894x(01)00664-3
PMID:11738569
Abstract

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.

摘要

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