title: 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 (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).
authors: Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
authors: Xiao-Zhi
authors: XZ
authors: Yang
authors: Xiao-Juan
authors: XJ
authors: Diao
authors: Wen-Hui
authors: WH
authors: Yang
authors: Feng
authors: F
authors: Li
authors: Guang-Wei
authors: GW
authors: He
authors: Guo-Qing
authors: GQ
authors: Gong
authors: Yun-Gen
authors: YG
authors: Xu
mesh_terms: D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology; D002109:Caffeic Acids / Q000737:chemistry; D000069604:Dabigatran; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005343:Fibrinolytic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000494:pharmacology; D013917:Thrombin / Q000378:metabolism; D020246:Venous Thrombosis / Q000188:drug therapy; D015091:beta-Alanine / Q000031:analogs & derivatives / Q000737:chemistry
chemical_list: D001562:Benzimidazoles; D002109:Caffeic Acids; D005343:Fibrinolytic Agents; D010975:Platelet Aggregation Inhibitors; D011355:Prodrugs; D011725:Pyridines; D015091:beta-Alanine; D013917:Thrombin; D000069604:Dabigatran; C530806:methyl ferulate