Design of potential antiplatelet agents based on modifications of the 3-pyridylisoxazole scaffold

Abstract

Based on two modifications of the main scaffold, 3-(3-pyridyl)isoxazole, two series of compounds were prepared, namely, positional isomers (5-substituted 3-phenylisoxazoles) and bioisosteres (5-substituted 3-(3-pyridyl)-1,2,4-oxadiazoles). Both series of compounds showed anti-aggregatory activity in the study of human platelet aggregation initiated by arachidonic acid and the selective thromboxane A₂ receptor agonist U46619. According to the results of the biological studies, all three scaffolds can be used for further development of prototypes of anti-aggregatory agents.