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ID: ALA1133358
Journal: Bioorg Med Chem Lett
Title: Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.
Authors: Zhao Z, Arnaiz DO, Griedel B, Sakata S, Dallas JL, Whitlow M, Trinh L, Post J, Liang A, Morrissey MM, Shaw KJ.
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.
CiteXplore: 10853669