Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties

…, M Hadden, D Orton, AR Rendina, JM Luettgen…

文献索引：Corte, James R.; Fang, Tianan; Pinto, Donald J.P.; Han, Wei; Hu, Zilun; Jiang, Xiang-Jun; Li, Yun-Long; Gauuan, Jolicia F.; Hadden, Mark; Orton, Darren; Rendina, Alan R.; Luettgen, Joseph M.; Wong, Pancras C.; He, Kan; Morin, Paul E.; Chang, Chong-Hwan; Cheney, Daniel L.; Knabb, Robert M.; Wexler, Ruth R.; Lam, Patrick Y.S. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 9 p. 2845 - 2849

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被引用次数: 22

摘要

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.