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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
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Document type:
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Článok z časopisu / Journal Article |
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Collection:
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Chemical papers
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| Author(s) |
Jampílek, Josef
Brojerová, Eliška
Doležal, Martin
Kuneš, Jiří
Jun, Daniel
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| Title |
Preparation and antiplatelet activity of glycidic acid derivatives
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| Journal name |
Chemical Papers
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| Publication date |
2008
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| Year available |
2008
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| Volume number |
62
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| Issue number |
3
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| ISSN |
0366-6352
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| Start page |
281
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| End page |
287
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| Place of publication |
Poland
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| Publisher |
Versita
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| Collection year |
2008
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| Language |
english
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| Subject |
250000 Chemical Sciences
250300 Organic Chemistry
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| 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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