中文摘要：

目的评价氟喹诺酮C-3位羧基被酰腙替代对其抗菌活性影响,为进一步扩大结构修饰提供新的途径。方法第三代氟喹诺酮类药物氧氟沙星及环丙沙星为起始原料,经肼解成其相应的酰肼,然后分别与芳香醛进行缩合得系列C-3酰腙目标化合物。用琼脂稀释法研究了目标化合物体外对标准菌株金黄色葡萄球菌（S.aureusATCC29213）、大肠埃希氏菌（E.coliATCC25922）、铜绿假单孢菌（P.aeruginosaATCC2785）的生长抑制活性。结果合成了12个新的目标酰腙化合物,体外活性结果表明,氧氟沙星类酰腙化合物表现出较弱的体外抗菌活性（其MIC〉128μg·mL^-1）,而多数环丙沙星类酰腙化合物却表现出较强的体外抗菌活性（其MIC〉8μg·mL^-1）,尤其是香草醛环丙酰腙（5d）对S.aureus及E.coli的MIC≥0.5μg·mL^-1,对P.aeruginosa的MIC≥1.0μg·mL^-1,其抗菌活性与对照环丙沙星相当（MIC≥0.5μg·mL^-1）,而优于氧氟沙星（MIC≥2.0μg·mL^-1）。结论抗菌药氟喹诺酮C-3位羧基被其他取代基替代值得进一步研究。

英文摘要：

OBJECTIVE To evaluate an influence for the placement of C-3 fluoro quinolone carboxylic group with acylhydrazone on the antibacterial activity.METHODS A series of C-3 acylhydrazones derived ciprofloxacin and ofloxacin were synthesized by a condensation the corresponding C-3 hydrazides with aromatic aldehydes,and the in vitro antibacterial activities of newly synthesized compounds were tested against Gram positive bacteria and Gram negative bacteria with the standard 2-fold agar dilution method.RESULTS Twelve title compunds were synthesized,and their structures were characterized by their spectral data.Some ciprofloxacin derivatives showed potential antibacterial activity but ofloxacin derivatives had poor activity.CONCLUSION The C-3 carboxyl-based substituted antibacterial fluoroquinolones are valuable for further study.