诺氟沙星衍生物的合成及其抗菌活性研究

Synthesis and antibacterial activity of norfloxacin derivatives

目的设计合成具有抗菌活性的诺氟沙星衍生物。方法采用 2 甲基 5 硝基咪唑、诺氟沙星等为原料 ,通过亲核取代反应合成目的物 ;测定目的物的体内抗菌活性。结果合成的 9个化合物的结构经MS、1H NMR和元素分析所确证。结论合成了 9个未见报道的新化合物 ,体内活性测试结果表明 :其中的 3个化合物具有较高的抗菌活性。

Aim To study the synthesis and antibacterial activity of norfloxacin derivatives.Method Norfloxacin derivatives were synthesized primarily from 2-methyl-5-nitroimidazol,norfloxacin via nucleophilic substitution.The antibacterial activities of the nine target compounds were tested.Result Their structures were confirmed by 1H-NMR,MS and elemental analysis.Conclusion The nine compounds prepared were new compounds and three of them showed higher activity than those of the compared compounds.