Novel 5-azaindole factor VIIa inhibitors

…, D Vijaykumar, TA Wahl, Z Tong, PA Sprengeler…

文献索引：Riggs, Jennifer R.; Hu, Huiyong; Kolesnikov, Aleksandr; Leahy, Ellen M.; Wesson, Kieron E.; Shrader, William D.; Vijaykumar, Dange; Wahl, Troy A.; Tong, Zhiwei; Sprengeler, Paul A.; Green, Michael J.; Yu, Christine; Katz, Brad A.; Sanford, Ellen; Nguyen, Margaret; Cabuslay, Ronnel; Young, Wendy B. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 12 p. 3197 - 3200

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被引用次数: 20

摘要

We have developed a series of potent and selective factor VIIa inhibitors based on the 2-[5-(5 -carbamimidoyl-1H-benzoimidazol-2-yl)-6-hydroxy-biphenyl-3-yl]- succinic acid scaffold. These biaryl amidine-containing compounds suffer from low oral bioavailability. In an attempt to apply the knowledge we have gained from our amidine fVIIa inhibitor parenteral program to an oral program, we began with our 5-amidinobenzimidazole scaffold and replaced the amidine ...