Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment

BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY(2022)

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摘要
A new chemical library based on the hybridization of cholic acid with the heterocyclic moiety 1,3,4-oxadizole was synthesized, and tested for antimicrobial activity against Gram-positive, Gram-negative bacteria, and fungi. Among the synthesized compounds, the most potent derivatives against S. aureus were 4t, 4i, 4p, and 4c with MIC values between 31 and 70 ??g/mL, while compound 4p was the most active one against Bacillus subtilis with a MIC value of 70 ??g/mL. Interestingly, compounds 4a and 4u exerted selective activity against Gram-positive bacteria. The synthesized compounds showed good activity against A. fumigatus and C. albicans and compound 4v exhibited selective activity against fungi only.
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关键词
antibacterial, cholic acid, heterocyclic, Mannich reaction, oxadiazole
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