胆酰基1,3,4-恶二唑杂化化合物：设计、合成与抗菌评估
Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment.
作者信息
Rasras Anas J, El-Naggar Mohamed, Safwat Nesreen A, Al-Qawasmeh Raed A
机构信息
Faculty of Science, Department of Chemistry, Al-Balqa Applied University, PO Box 19117, Al-Salt, Jordan.
College of Sciences, Department of Chemistry, University of Sharjah, Pure and Applied, Chemistry Research Group, PO Box 27272, Sharjah, United Arab Emirates.
出版信息
Beilstein J Org Chem. 2022 May 31;18:631-638. doi: 10.3762/bjoc.18.63. eCollection 2022.
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 were , , , and with MIC values between 31 and 70 µg/mL, while compound was the most active one against with a MIC value of 70 µg/mL. Interestingly, compounds and exerted selective activity against Gram-positive bacteria. The synthesized compounds showed good activity against and and compound exhibited selective activity against fungi only.
合成了一种基于胆酸与杂环部分1,3,4-恶二唑杂化的新型化学文库，并对其针对革兰氏阳性菌、革兰氏阴性菌和真菌的抗菌活性进行了测试。在合成的化合物中，对[具体细菌名称未给出]最有效的衍生物是[具体化合物名称未给出]，其MIC值在31至70 µg/mL之间，而化合物[具体化合物名称未给出]对[具体细菌名称未给出]最具活性，MIC值为70 µg/mL。有趣的是，化合物[具体化合物名称未给出]和[具体化合物名称未给出]对革兰氏阳性菌具有选择性活性。合成的化合物对[具体细菌名称未给出]和[具体细菌名称未给出]显示出良好的活性，并且化合物[具体化合物名称未给出]仅对真菌表现出选择性活性。
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