Design, synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing methyl ferulate

Abstract A novel series of prodrugs containing dabigatran and methyl ( E )-3-(4-hydroxy-2-methoxyphenyl)propenoate (methyl ferulate) were synthesized. All of them reveal the effect of thrombin-induced anti-platelet aggregation in vitro. In addition, in vivo experiment shows that one of the target compounds, X - 2 (ED 50  = 3.7 ± 1.0 μmol/kg) possesses a more potent activity for inhibiting venous thrombosis than that of dabigatran etexilate (ED 50  = 7.8 ± 1.5 μmol/kg).