Design,synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing methyl ferulate |
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| Authors: | Xiao-Zhi Yang Xiao-Juan Diao Wen-Hui Yang Feng Li Guang-Wei He Guo-Qing Gong Yun-Gen Xu |
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| Institution: | 1. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;2. Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, China;3. Hefei Yi Gong Pharmaceutical Co., Ltd, Hefei 230088, China |
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| 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 (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). |
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