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目的 :研究 7-取代 - 1- ( 2 -氟乙基 ) - 6 ,8-二氟 - 1,4-二氢 - 4-氧 - 3-喹啉羧酸的合成及其抗菌活性。 方法 :通过高温下缩合、环化、亲核取代得到关键中间体 ,然后通过反应制得目标化合物。选用临床常见的 6株致病菌的标准菌株进行体外抗菌活性测定。 结果 :设计合成 11个化合物 ,均为首次报道。通过 IR,1 HNMR和元素分析来确证化合物的结构。体外抗菌活性实验以氟罗沙星为对照品 ,其中化合物 1 , 2 , 4的抗菌活性较强。 结论 :合成的 11个化合物中有一些化合物显示较好的抗菌活性 ,值得进一步深入研究。
Objective: To study the synthesis and antibacterial activity of 7-substituted-1- (2-fluoroethyl) -6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid. Methods: The key intermediate was obtained through condensation, cyclization and nucleophilic substitution at high temperature, and then the target compound was obtained through the reaction. Selection of clinical common 6 strains of pathogenic bacteria in vitro antibacterial activity determination. Results: The design and synthesis of 11 compounds were the first reported. The structure of the compound was confirmed by IR, 1 HNMR and elemental analysis. In vitro antibacterial activity test with fleroxacin as a reference substance, of which compounds 1, 2, 4 antibacterial activity. Conclusion: Some of the 11 compounds synthesized show good antibacterial activity and deserve further study.