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含2-甲基-5-硝基咪唑的吡酮酸类衍生物的合成及其抗菌活性
Synthesis and antibacterial activity of pyridonecarboxylic acid derivatives containing 2-methyl-5-nitroimidazol
【摘要】 目的 研究含N 乙基 2 甲基 5 硝基咪唑的诺氟沙星、环丙沙星和依诺沙星衍生物的合成及其抗菌活性。方法 用含 2 甲基 5 硝基咪唑的诺氟沙星、环丙沙星和依诺沙星等为原料 ,通过亲核取代、酯化合成目的物 ;测定目的物的抗菌活性。结果 设计、合成了 9个新化合物 (IIa~c ,IIIa~f) ,其结构经MS ,1 HNMR和元素分析确证。化合物IIa~c的体内抗菌活性较明显。结论 化合物IIa~c显示了一定的体内抗菌活性 ,值得进一步研究
【Abstract】 Aim To study the synthesis and antibacterial activity of pyridonecarboxylic acid derivatives containing 2 methyl 5 nitroimidazol. Methods Pyridonecarboxylic acid derivatives containing 2 methyl 5 nitroimidazol were synthesized primarily from 2 methyl 5 nitroimidazol, norfloxacin, ciprofloxacin, enoxacin via nucleophilic substitution and esterification. The antibacterial activity of the nine target compounds were tested. Results Nine new compounds were synthesized (IIa~c and IIIa~f). The structure of the title compounds were identified by 1HNMR , MS as well as elementary analysis. Conclusion Compounds IIa, IIb and IIc showed antibacterial activity, and were worth further studying.
【Key words】 pyridonecarboxylic acid; prodrug; imidaxole; antibacterial activity;
- 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,2003年04期
- 【分类号】R914
- 【被引频次】3
- 【下载频次】179