Factor VIIa inhibitors: gaining selectivity within the trypsin family

WD Shrader, A Kolesnikov, J Burgess-Henry…

文献索引：Shrader, William D.; Kolesnikov, Aleksandr; Burgess-Henry, Jana; Rai, Roopa; Hendrix, John; Hu, Huiyong; Torkelson, Steve; Ton, Tony; Young, Wendy B.; Katz, Bradley A.; Yu, Christine; Tang, Jie; Cabuslay, Ronnel; Sanford, Ellen; Janc, James W.; Sprengeler, Paul A. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 6 p. 1596 - 1600

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被引用次数: 19

摘要

Within the trypsin family of coagulation proteases, obtaining highly selective inhibitors of factor VIIa has been challenging. We report a series of factor VIIa (fVIIa) inhibitors based on the 5-amidino-2-(2-hydroxy-biphenyl-3-yl)-benzimidazole (1) scaffold with potency for fVIIa and high selectivity against factors IIa, Xa, and trypsin. With this scaffold class, we propose that a unique hydrogen bond interaction between a hydroxyl on the distal ring of the biaryl ...