期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 90, 期 5, 页码 943-952出版社
WILEY
DOI: 10.1111/cbdd.13020
关键词
5-phenyl-1,3,4-oxadiazole-2-thiol; antibacterial agents; non-toxicity; quaternary ammonium salt; SEM and TEM
资金
- National Natural Science Foundation of China [21402010]
- Foundation of Shandong province [ZR2013BM022, 2014CGZH1316, 2015GGX102013]
- Foundation of Yantai city [2016ZH078, 2014ZH092]
Twenty-one novel 5-phenyl-1,3,4-oxadiazole-2-thiol (POT) substituted N-hydroxyethyl quaternary ammonium salts (6a-g, 7a-g, 8a-g) were prepared and characterized by FTIR, NMR, and elemental analysis. Compounds 6a, 6c, and 8a were confirmed by X-ray single-crystal diffraction. They display the unsurpassed antibacterial activity against Staphylococcus aureus, -H-tococcus, Escherichia coli, P.aeruginosa, Proteus vulgaris, Canidia Albicans, especially 6g, 7g, 8g with dodecyl group. Compounds 8a-d with N,N-dihydroxyethyl and POT groups display unsurpassed antibacterial activity and non-toxicity. The structure-activity relationships indicate that POT and flexible dihydroxyethyl group in QAS are necessary for antibacterial activity and cytotoxicity. SEM and TEM images of E.coli morphologies of 8d show the antibacterial agents can adhere to membrane surfaces to inhibit bacterial growth by disrupting peptidoglycan formation and releasing bacterial cytoplasm from cell membranes.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据