Syntheses of 5-substituted oxazole-4-carboxylic acid derivatives with inhibitory activity on blood platelet aggregation.

doi:10.1248/CPB.31.4417

Paper

Syntheses of 5-substituted oxazole-4-carboxylic acid derivatives with inhibitory activity on blood platelet aggregation.

Published Dec 25, 1983 · Y. Ozaki, S. Maeda, T. Iwasaki

Chemical & pharmaceutical bulletin

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12

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Abstract

Methyl 5-substituted oxazole-4-carboxylates were synthesized by the reaction of methyl α-isocyanoacetate with acylating reagents in the presence of bases. The oxazole methyl esters were converted into the carboxylic acids and the carboxamides. Then, N-alkyl-oxazole-4-carboxamides were prepared through the oxazole-4-carboxylic acid chloride. Furthermore, 2-substituted oxazoles were synthesized by cyclization of N-acyl-α-benzoylglycine methyl esters. which were obtained by acylation of α-benzoylglycine methyl ester followed by ammonolysis of the resulting oxazole methyl esters. These oxazole compounds were evaluated for inhibitory activity on blood platelet aggregation in vitro and ex vivo. Some of these compounds showed the inhibitory activity comparable to that of aspirin. Of these, 5-(3, 4, 5-trimethoxyphenyl) oxazole-4-carboxamide was the most active compound in the ex vivo test.

In Vitro Study

Study Snapshot

5-substituted oxazole-4-carboxylic acid derivatives show inhibitory activity on blood platelet aggregation, with 5-(3, 4, 5-trimethoxyphenyl) oxazole-4-carboxamide being the most active compound in ex vivo tests.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Syntheses of 5-substituted oxazole-4-carboxylic acid derivatives with inhibitory activity on blood platelet aggregation.

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References

Citations

Protecting-Group-Free Synthesis of 1-Phenylisoquinolin-4-ols: Thermal Cyclization of Methyl 2-[(Diphenylmethylidene)amino]acetates.

This study developed a protecting-group-free synthetic approach to 1-phenylisoquinolin-4-ols by thermal cyclization of methyl 2-[(diphenylmethylidene)amino]acetates, with R1 and R2 substituents affecting reaction temperatures, time

Regioselective palladium-catalyzed phenylation of ethyl 4-oxazolecarboxylate

Palladium-catalyzed C-2 arylation of ethyl 4-oxazolecarboxylate with phenyliodide is efficient and regioselective, with optimal conditions determined by optimizing solvent, base, ligand, and catalyst parameters.

N–H Insertion reactions of rhodium carbenoids. Part 5: A convenient route to 1,3-azoles☆

This study presents a convenient route to 1,3-azoles through N-H insertion reactions of rhodium carbenoids, leading to diverse oxazoles, thiazoles, and imidazoles.