1415901-85-7Relevant articles and documents
Design, synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing methyl ferulate
Yang, Xiao-Zhi,Diao, Xiao-Juan,Yang, Wen-Hui,Li, Feng,He, Guang-Wei,Gong, Guo-Qing,Xu, Yun-Gen
, p. 2089 - 2092 (2013/04/24)
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 (ED50 = 3.7 ± 1.0 μmol/kg) possesses a more potent activity for inhibiting venous thrombosis than that of dabigatran etexilate (ED50 = 7.8 ± 1.5 μmol/kg).
Synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing a cleavable moiety with anti-platelet activity
Yang, Xiao-Zhi,Yang, Wen-Hui,Xu, Yun-Gen,Diao, Xiao-Juan,He, Guang-Wei,Gong, Guo-Qing
, p. 21 - 28 (2013/01/15)
A novel series of prodrugs consisting of dabigatran and 2-hydroxymethyl-3,5,6-trimethylpyrazine (HTMP) were synthesized. The pharmacological results show that all of them possess the effect of anti-platelet aggregation induced by thrombin in vitro. Moreover, one of those compounds, Y-2 (ED50 = 2.1 ± 1.3 mg/kg) shows more potent activity for inhibiting thrombosis in vivo than that of dabigatran etexilate (ED50 = 4.4 ± 2.2 mg/kg).