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

被引：8

作者：

Rasras, Anas J. ^{[1
]}

El-Naggar, Mohamed ^{[2
]}

Safwat, Nesreen A. ^{[3
]}

Al-Qawasmeh, Raed A. ^{[2
,4
]}

机构：

[1] Al Balqa Appl Univ, Fac Sci, Dept Chem, POB 19117, Al Salt, Jordan

[2] Univ Sharjah, Coll Sci, Dept Chem, Pure & Appl Chem Res Grp, POB 27272, Sharjah, U Arab Emirates

[3] Al Azhar Univ, Reg Ctr Mycol & Biotechnol, Cairo 11371, Egypt

[4] Univ Jordan, Dept Chem, Amman 11942, Jordan

来源：

BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY | 2022年 / 18卷

关键词：

antibacterial; cholic acid; heterocyclic; Mannich reaction; oxadiazole; BIOLOGICAL EVALUATION; DOCKING; INDOLE;

D O I：

10.3762/bjoc.18.63

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

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.

引用

页码：631 / 638

页数：8

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