Design and Synthesis of Some P-Substituted Styrylisoxazole Carboxylic Acid Derivatives as Anti-Inflammatory Agents

Abstract

Egypt electron microscope, after 24 hours of administration of single dose (100 mg/kg) in rats. Significant anti-inflammatory activity was displayed by most of the target derivatives. p-Nitro and p-methoxystyryl isoxazole carboxylic acid derivatives (4e and 4f) revealed 75% inhibition of inflammation after 1 hr reflected the rapid onset of action of these derivatives, which may sustained up to 5 hr as in case of 4e. The anti-inflammatory activity of 5-(p-nitro and pdimethylaminostyryl)-isoxazole-3-carboxylic acid ethyl esters (3e and 3g) being favorably comparable with indomethacin in terms of potency and ulcerogenic liability. The rational behind the synthesis of these compounds and the structure activity relationship are discussed.

Synthesis, Biological Evaluation, and Structure−Activity Relationships for 5-[(E)-2-Arylethenyl]-3-isoxazolecarboxylic Acid Alkyl Ester Derivatives as Valuable Antitubercular Chemotypes

“…The residue was purified by flash chromatography to obtain the product. Analytical data for compounds 8, 26 18, 27 and 32 28 matched the data previously published.…”