Synthesis, intramolecular cyclization, and antinociceptive activity of 4-(het)aryl-2-{[4-(4-chlorophenyl)-3-(ethoxycarbonyl)thiophen-2-yl]amino}-4-oxobut-2-enoic acids

I. A. Gorbunova, I. P. Nikonov, R. R. Makhmudov,D. A. Shipilovskikh, P. S. Silaichev,S. A. Shipilovskikh

Russian Chemical Bulletin(2023)

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摘要
Synthesis and intramolecular cyclization of the substituted 4-(het)aryl-2-{[4-(4-chlorophenyl)-3-(ethoxycarbonyl)thiophen-2-yl]amino}-4-oxobut-2-enoic acids were studied. It was found that the synthesized compounds underwent the intramolecular cyclization to give the substituted ethyl 4-(4-chlorophenyl)-2-{[2-oxofuran-3(2 H )-ylidene]-amino}thiophene-3-carboxylates. Evaluation of the biological activity of the synthesized compounds showed that they have pronounced antinociceptive activity along with low toxicity.
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关键词
Gewald thiophenes,2,4-dioxobutanoic acids,3-iminofuran-2-ones,antinociceptive activity,toxicity,medications
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