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).
Copyright © 2013 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacology
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Caffeic Acids / chemistry
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Dabigatran
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Dose-Response Relationship, Drug
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Drug Design*
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Fibrinolytic Agents / chemical synthesis
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Fibrinolytic Agents / chemistry
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Fibrinolytic Agents / pharmacology*
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Humans
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Molecular Structure
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Platelet Aggregation / drug effects*
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Platelet Aggregation Inhibitors / chemical synthesis
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Platelet Aggregation Inhibitors / chemistry
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Platelet Aggregation Inhibitors / pharmacology*
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Prodrugs / chemical synthesis
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Prodrugs / chemistry
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Prodrugs / pharmacology*
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Pyridines / pharmacology
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Thrombin / metabolism
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Venous Thrombosis / drug therapy
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beta-Alanine / analogs & derivatives
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beta-Alanine / chemistry
Substances
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Benzimidazoles
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Caffeic Acids
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Fibrinolytic Agents
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Platelet Aggregation Inhibitors
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Prodrugs
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Pyridines
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beta-Alanine
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Thrombin
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Dabigatran
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methyl ferulate