摘要
目的 研究环丙沙星衍生物的合成及其抗菌活性。方法 采用- 2- 甲基- 5- 硝基咪唑、环丙沙星等为原料,通过亲核取代反应合成目的物;测定目的物的抗菌活性。结果 设计、合成了 9个新化合物,其结构经MS, 1HNMR和元素分析确证。化合物II, IVC和IVD的体内抗菌活性较明显。结论 化合物II, IVC和IVD显示了一定的体内抗菌活性,值得进一步研究。
Aim To study the synthesis and antibacterial activity of ciprofloxacin derivatives. Methods Ciprofloxacin derivatives were synthesized primarily from 2-methyl-5-nitroimidazol and ciprofloxacin through nucleophilic substitution. The antibacterial activity of the synthesized compounds were tested. Results Nine new compounds were synthesized. The structure of the title compounds were confirmed by 1H NMR, MS and element analysis. Conclusion Compounds II, IV C and IV D showed appreciable antibacterial activity ,and were worth further studying.
出处
《药学学报》
CAS
CSCD
北大核心
2005年第2期132-135,共4页
Acta Pharmaceutica Sinica
关键词
环丙沙星
前药
咪唑
抗菌活性
合成
ciprofloxacin derivatives
prodrug
imidaxole
antibacterial activity
synthesis