7-取代-1-(2-氟乙基)-6,8-二氟-1,4-二氢-4-氧-3-喹啉羧酸化合物的合成及其抗菌活性

Synthesis and antibacterial activity of 7-substituted-1-(2-fluoroethyl)-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolone carboxylic acid compounds

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 quinolone carboxylic acid compounds. Methods: The title compounds were synthesized by condensation,cyclization, nucleophilic substitution. Antibacterial activity in vitro was determined with 6 kinds of common pathogenic bacteria. Results: Eleven compounds of 7 substituted 1 (2 fluoroethyl) 6,8 difluoro 1,4 dihydro 4 oxo 3 quinolone carboxylic acid were designed and synthesized. These compounds were firstly reported. The chemical structures of all compounds were determined by IR, 1HNMR and elementary analysis. CompoundⅠ 1,Ⅰ 2,Ⅱ 4 showed better antibacterial activities than that of fleroxacin. Conclusion: Some of the title compounds show potent antibacterial activities and should be further studied. [