210963-32-9Relevant academic research and scientific papers
Benzimidazole-Based fXa inhibitors with improved thrombin and trypsin selectivity
Shaw, Kenneth J.,Guilford, William J.,Griedel, Brian D.,Sakata, Steve,Trinh, Lan,Wu, Shung,Xu, Wei,Zhao, Zuchun,Morrissey, Michael M.
, p. 1311 - 1314 (2002)
Optimization of the benzimidazole-based fXa inhibitors for selectivity versus thrombin and trypsin was achieved by substitution on the benzimidazole ring and replacement of the naphthylamidine group. Substitution of a nitro group at the 4-position on the benzimidazole improves both potency against fXa and selectivity versus thrombin. Alternatively, replacement of the naphthylamidine with either a biphenylamidine or propenylbenzamidine not only improves fXa potency and selectivity versus thrombin, but selectivity versus trypsin as well.
