Author/Authors :
Zuchun (Spring) Zhao، نويسنده , , Damian O. Arnaiz، نويسنده , , Brian Griedel، نويسنده , , Steven Sakata، نويسنده , , Jerry L. Dallas، نويسنده , , Marc Whitlow، نويسنده , , Lan Trinh، نويسنده , , Joseph Post، نويسنده , , Amy Liang، نويسنده , , Michael M. Morrissey، نويسنده , , Kenneth J. Shaw، نويسنده ,
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.
