期刊
CHEMISTRY & BIODIVERSITY
卷 -, 期 -, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbdv.202300105
关键词
imidazole; thiadiazole; cytotoxicity; antibacterial activity; hemolyisis
A series of novel 2-cyclopropyl-5-(5-(6-methylpyridin-2-yl)-2-substituted-1H-imidazol-4-yl)-6-phenylimidazo[2,1-b][1,3,4]thiadiazoles were synthesized and evaluated for their antibacterial activities. Most of the compounds exhibited moderate to strong antibacterial activities, with compounds 15t (MIC=1-2 mu g/mL) and 16d (MIC=0.5 mu g/mL) showing the highest potency. Interestingly, compound 16d showed no cytotoxicity in HepG2 cells and no hemolysis, suggesting its potential as a candidate antibacterial agent.
A series of 2-cyclopropyl-5-(5-(6-methylpyridin-2-yl)-2-substituted-1H-imidazol-4-yl)-6-phenylimidazo[2,1-b][1,3,4]thiadiazoles (15a-t and 16a-f) were synthesized and their antibacterial activities were evaluated. More than half of the compounds showed moderate or strong antibacterial activity. Among them, compounds 15t (MIC=1-2 mu g/mL) and 16d (MIC=0.5 mu g/mL) showed the strongest antibacterial activities. Notably, compound 16d did not exhibit cytotoxicity in HepG2 cells and did not show hemolysis like the positive control compound Gatifloxacin. The results suggest that compound 16d should be further investigated as a candidate antibacterial agent.
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