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<p>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 A<sub>2</sub> 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.</p>

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

  • 期刊论文

  • 发表日期：

    2025年4月1日

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  • O. V. Demina,
  • N. E. Belikov,
  • A. Yu. Lukin,
  • N. A. Podoplelova,
  • M. A. Panteleev,
  • A. A. Khodonov,
  • S. D. Varfolomeev

摘要

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.