Synthesis and antibacterial evaluation of novel Schiff”s base derivatives of nitroimidazole nuclei as potent E.coli FabH inhibitors
Series of novel Schiff”s base derivatives have been synthesized by combining 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl 4-formylbenzoate 5,6 with aromatic/heterocyclic amine 7a-r,8,9a-r in ethanol.All compounds were evaluated for antibacterial assay and inhibition against E.coli FabH.Among the compounds studied,most of the compounds showed effective antibacterial and potential inhibitory activity against E.coli FabH,Compound 10q showed most potent inhibitory activity(IC500= 2.6883 μM)by binding tightly to the active site of the E.coli FabH receptor with minimum binding energy(ΔGb=-55.3117 kcal mol-1),in which molecular docking study indicated the binding mode was stabilized by one hydrogen bond and five π-Π interactions.
Xin Zhang Chetan B Sangani Li-Xin Jia Pi-Xian Gong Fang Wang Jun-Fang Wang Hai-Liang Zhu
State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,Nanjing 210093,People”s Republic of China
国内会议
大连
英文
760-768
2016-09-24（万方平台首次上网日期，不代表论文的发表时间）