化学
抗菌活性
氮杂环丁烷
DNA旋转酶
金黄色葡萄球菌
大肠杆菌
对接(动物)
三唑
最小抑制浓度
体外
组合化学
铜绿假单胞菌
头孢噻肟
立体化学
1,2,4-三唑
细菌
有机化学
生物化学
抗生素
护理部
基因
生物
医学
遗传学
作者
Esha Dhall,Sonika Jain,Achal Mishra,Jaya Dwivedi,Swapnil Sharma
摘要
A novel series of phenyl substituted azetidine containing 1, 2, 4‐triazole derivatives 7 ( a – j ) were synthesized and characterized by IR, 1HNMR, 13CNMR, and mass spectroscopy. Synthesized 1, 2, 4‐triazole derivatives were subsequently assayed in vitro to investigate their antibacterial activity against Staphylococcus aureus , Pseudomonas aeruginosa , and Escherichia coli using broth dilution method. Compounds 7c , 7d , and 7e exhibited potent inhibitory activities as compared to standard cefotaxime. Further, fluorescence spectral studies were also carried out to ascertain the antibacterial potential of compound 7c against two bacterial strains, that is, P. aeruginosa and S. aureus . In docking studies, all the compounds exhibited good docking scores between −12.04 and −11.36 kcal/mol and indicated that compounds could act through inhibition of bacterial DNA gyrase (PDB ID 3U2D). Among all, 7c has shown the maximum docking score and found in agreement to in vitro studies. In conclusion, synthesized 1, 2, 4‐triazole derivatives holds substantial caliber to be categorized as antibacterial agents.
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