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,¹HNMR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.