Interdisciplinary Program of Biological Function Molecules, College of Integration Science, Yanbian University, Yanji, 133002, China.
Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, 133002, China.
Chem Biodivers. 2023 May;20(5):e202300105. doi: 10.1002/cbdv.202300105. Epub 2023 Apr 7.
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 μg/mL) and 16d (MIC=0.5 μg/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.
一系列 2-环丙基-5-(5-(6-甲基吡啶-2-基)-2-取代-1H-咪唑并[4,5-b]噻唑-4-基)-6-苯基咪唑并[2,1-b][1,3,4]噻二唑(15a-t 和 16a-f)被合成并评估了它们的抗菌活性。超过一半的化合物表现出中等或强抗菌活性。其中,化合物 15t(MIC=1-2μg/mL)和 16d(MIC=0.5μg/mL)表现出最强的抗菌活性。值得注意的是,化合物 16d 在 HepG2 细胞中没有表现出细胞毒性,也不像阳性对照化合物加替沙星那样发生溶血。结果表明,化合物 16d 应该作为候选抗菌剂进一步研究。