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

被引：23

作者：

Yang, Xiao-Zhi ^{[1
]}

Diao, Xiao-Juan ^{[1
]}

Yang, Wen-Hui ^{[2
]}

Li, Feng ^{[3
]}

He, Guang-Wei ^{[3
]}

Gong, Guo-Qing ^{[2
]}

Xu, Yun-Gen ^{[1
]}

机构：

[1] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China

[2] China Pharmaceut Univ, Dept Pharmacol, Nanjing 210009, Peoples R China

[3] Hefei Yi Gong Pharmaceut Co Ltd, Hefei 230088, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 07期

基金：

中国国家自然科学基金;

关键词：

Dabigatran; Ferulic acid; Methyl ferulate; Thrombin inhibitors; Anti-platelet aggregation; Prevention and treatment of thrombosis; DERIVATIVES; THROMBOSIS; ETEXILATE; ASPIRIN;

D O I：

10.1016/j.bmcl.2013.01.126

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

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 antiplatelet aggregation in vitro. In addition, in vivo experiment shows that one of the target compounds, X-2 (ED50 = 3.7 +/- 1.0 mu mol/kg) possesses a more potent activity for inhibiting venous thrombosis than that of dabigatran etexilate (ED50 = 7.8 +/- 1.5 mu mol/kg). (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：2089 / 2092

页数：4

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