Synthesis and biological evaluation of the metabolites of 2-(1-{3-((6-chloronaphthalen-2-yl)sulfonyl)propanoyl}piperidin-4-yl)-5-methyl-1,2 -dihydro-3H-imidazo(1,5-c)imidazol-3-one.

摘要

We have recently discovered imidazo[1,5-c]imidazol-3-one derivative 1 as a potent, selective, and orally bioavailable factor Xa (FXa) inhibitor. In this study, we have synthesized metabolites of 1 and evaluated their biological activities. As a result, we identified the active metabolites S-5 and 6 with a potent FXa inhibitory activity comparable to 1 and a favorable pharmacokinetic profile in monkeys.