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

Author(s): Xiu J. Liu, Tian En Shi, Xiao Wang, Ting T. Wei, Xia Meng.

Journal Name: Cardiovascular & Hematological Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Cardiovascular & Hematological Agents)

Volume 13 , Issue 2 , 2015

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Graphical Abstract:


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.

Keywords: Antiplatelet aggregation, 4-ethoxyisophthalamide, picotamide, synthesis.

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Article Details

Year: 2015
Page: [124 - 128]
Pages: 5
DOI: 10.2174/187152571302151217142711
Price: $58

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