Preparation and antiplatelet activity of glycidic acid derivatives

Jampílek, Josef, Brojerová, Eliška, Doležal, Martin, Kuneš, Jiří and Jun, Daniel Preparation and antiplatelet activity of glycidic acid derivatives Chemical Papers, Vol.62, No. 3, 2008, 281-287

Document type: Článok z časopisu / Journal Article
Collection: Chemical papers  

Author(s) Jampílek, Josef
Brojerová, Eliška
Doležal, Martin
Kuneš, Jiří
Jun, Daniel
Title Preparation and antiplatelet activity of glycidic acid derivatives
Journal name Chemical Papers
Publication date 2008
Year available 2008
Volume number 62
Issue number 3
ISSN 0366-6352
Start page 281
End page 287
Place of publication Poland
Publisher Versita
Collection year 2008
Language english
Subject 250000 Chemical Sciences
250300 Organic Chemistry
Abstract/Summary Arylalkanoic acid derivatives exhibit a variety of biological effects. In the current publication some of new glycidic acid derivatives were prepared via the Darzens condensation. The synthetic approach, analytical and spectroscopic data of all newly synthesized compounds are presented. The prepared compounds were evaluated as potential inhibitors of arachidonic acid-induced platelet aggregation and their activity was compared with that of acetylsalicylic acid as the standard. (±)-Ethyl 3-{4-[(4-methoxyphenyl)sulfanyl]phenyl}-3-methyl-cis-oxirane-2-carboxylate (IC50 = 0.07 mmol L−1) and (±)-3-{4-[(4-methoxyphenyl)sulfanyl]phenyl}-3-methyl-cis-oxirane-2-carboxylic acid (IC50 = 0.06 mmol L−1) showed the highest antiplatelet activity against arachidonic acid-induced platelet aggregation comparable with the standard. Structure-activity relationships between the chemical structure, lipophilicity, and the antiplatelet activity of the evaluated compounds are discussed.
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