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Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors
Z Zhao1, D O Arnaiz, B Griedel
1Discovery Research, Berlex Biosciences, Richmond, CA 94804-0099, USA. Spring_Zhao@berlex.com
Bioorganic & Medicinal Chemistry Letters
|June 15, 2000
Abstract:
Inhibitors based on the benzimidazole scaffold showed subnanomolar potency against Factor Xa with 500-1000-fold selectivity against thrombin and 50-100-fold selectivity against trypsin. The 2-substituent on the benzimidazole ring had a strong impact on the FXa inhibitory activity. Crystallography studies suggest that the 2-substituent may have a conformational effect favoring the extended binding conformation.