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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

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【作者】 叶发青陈莉黄金敏

【Author】 YE Fa qing 1* , CHEN Li 2, HUANG Jin min 2 (1. Department of Chemistry, Wenzhou Medical College, Wenzhou 325027, China; 2. Department of Clinical Pharmacy, Xianning Medical College, Xianning 437100, China)

【机构】 温州医学院化学教研室咸宁医学院临床药学系咸宁医学院临床药学系 浙江温州325027湖北咸宁437100湖北咸宁437100

【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.

【关键词】 吡酮酸前药咪唑抗菌活性
【Key words】 pyridonecarboxylic acidprodrugimidaxoleantibacterial activity
【基金】 湖北省教育厅自然科学类重点课题资助项目(98B0 33)
  • 【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
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