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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).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Yang XZ,Diao XJ,Yang WH,Li F,He GW,Gong GQ,Xu YG

doi

10.1016/j.bmcl.2013.01.126

subject

Has Abstract

pub_date

2013-04-01 00:00:00

pages

2089-92

issue

7

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00159-5

journal_volume

23

pub_type

杂志文章

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