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

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.

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