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

被引:7
|
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
收藏
页码:631 / 638
页数:8
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