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.
Cardiovascular & Hematological Agents in Medicinal Chemistry
Title:Synthesis and the Evaluations in vitro Antiplatelet Aggregation Activities of 4-Ethoxyisophthalamides
Volume: 13 Issue: 2
Author(s): Xiu J. Liu, Tian En Shi, Xiao Wang, Ting T. Wei and Xia Meng
Affiliation:
Keywords: Antiplatelet aggregation, 4-ethoxyisophthalamide, picotamide, synthesis.
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.
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Cite this article as:
Liu J. Xiu, Shi En Tian, Wang Xiao, Wei T. Ting and Meng Xia, Synthesis and the Evaluations in vitro Antiplatelet Aggregation Activities of 4-Ethoxyisophthalamides, Cardiovascular & Hematological Agents in Medicinal Chemistry 2015; 13 (2) . https://dx.doi.org/10.2174/187152571302151217142711
DOI https://dx.doi.org/10.2174/187152571302151217142711 |
Print ISSN 1871-5257 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6182 |
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