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Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.

作者信息

Iwanowicz Edwin J, Kimball S David, Lin James, Lau Wan, Han W-C, Wang Tammy C, Roberts Daniel G M, Schumacher W A, Ogletree Martin L, Seiler Steven M

机构信息

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

出版信息

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3183-6. doi: 10.1016/s0960-894x(02)00651-0.

DOI:10.1016/s0960-894x(02)00651-0
PMID:12372529
Abstract

A series of retro-binding inhibitors of human alpha-thrombin was prepared to elucidate structure-activity relationships (SAR) and optimize in vivo performance. Compounds 9 and 11, orally active inhibitors of thrombin catalytic activity, were identified to be efficacious in a thrombin-induced lethality model in mice.

摘要

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