Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties
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- 作者：James R. Corte ; Tianan Fang ; Donald J.P. Pinto ; Wei Han ; Zilun Hu ; Xiang-Jun Jiang ; Yun-Long Li ; Jolicia F. Gauuan ; Mark Hadden ; Darren Orton ; Alan R. Rendina ; Joseph M. Luettgen ; Pancras C. Wong ; Kan
- 关键词：Factor Xa ; Anthranilamide
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：1 May 2008
- 年：2008
- 卷：18
- 期：9
- 页码：2845-2849
- 全文大小：266 K
文摘
Introduction of the phenyl piperidinone and phenyl pyridinone P4 moieties in the anthranilamide scaffold led to potent, selective, and orally bioavailable inhibitors of factor Xa. Anthranilamide 28 displayed comparable efficacy to apixaban in the rabbit arteriovenous-shunt (AV) thrombosis model.