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Synthesis and the Evaluations in vitro Antiplatelet Aggregation Activities of 4-Ethoxyisophthalamides

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In our search for new compounds among the structural analogues of the Picotamide acting on antiplatelet aggregation activities, a new series 2 of 4-ethoxyisophthal-amides were synthesized and their in vitro anti-platelet aggregation activities were evaluated by Born’s test in comparison with their structural analogues of the series 1 of 4-methoxyisophthal-amides. The results revealed, among the series 2, six compounds 200, 2a, 2k, 2n, 2q and 2r displayed good antiplatelet aggregation activities in vitro induced by 5.0 mM ADP with IC50 values ranging over 0.35 μM - 0.77 μM. And of which, compound 2a exhibited the highest in vitro activity superior than two control drugs Picotamide and Aspirin. From a structure-affnity-’Relationship (SAR) pointed of some insight in the view of the role played by 4-ethoxy derivatives.
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Keywords: 4-ethoxyisophthalamide; Antiplatelet aggregation; picotamide; synthesis

Document Type: Research Article

Publication date: August 1, 2015

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  • Cardiovascular & Hematological Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new Cardiovascular & Hematological Agents. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of current topics in Cardiovascular & Hematological medicinal chemistry.

    Cardiovascular & Hematological Agents in Medicinal Chemistry
    is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cardiovascular & hematological drug discovery.
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