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有机化学 ›› 2005, Vol. 25 ›› Issue (10): 1221-1226. 上一篇    下一篇

研究论文

1-环丙基-6-氟-7-(4-酰基-1-哌嗪基)-1,4-二氢-4-氧代喹啉-3-羧酸的合成及其抗菌活性研究

李英俊*,1，刘素娜1，许永廷1，靳焜2
彭勤纪2，王营1，张治广1   

  1. (1辽宁师范大学化学化工学院 大连 116029)
    (2大连理工大学精细化学化工重点实验室 大连 116012)
  • 收稿日期:2005-01-17 修回日期:2005-04-15 发布日期:2005-10-08
  • 通讯作者: 李英俊

Synthesis and Antibacterial Activity of 1-Cyclopropyl-6-fluoro-7-(4-acyl-1-piperazinyl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic Acid

LI Ying-Jun*,1,LIU Su-Na1,XU Yong-Ting1,JIN Kun2
PENG Qin-Ji2,WANG Ying1,ZHANG Zhi-Guang1   

  1. (1School of Chemical Engineering, Liaoning Normal University, Dalian 1160290)
    (2State Key Laboratory of Fine Chemicals, Dalian University of Technol-ogy, Dalian 116012)
  • Received:2005-01-17 Revised:2005-04-15 Published:2005-10-08
  • Contact: LI Ying-Jun

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以1-环丙基-6-氟-7-氯-1, 4-二氢-4-氧代喹啉-3-羧酸为原料经过两步反应合成出了16个新的1-环丙基-6-氟-7-(4-酰基-1-哌嗪基)-1, 4-二氢-4-氧代喹啉-3-羧酸, 并利用IR, 1H NMR, 13C NMR, MS谱及元素分析对其结构进行了表征. 初步体外抗菌活性研究表明, 大部分目标化合物对大肠杆菌有一定的抑菌活性, MIC值在0.312～20 g/mL之间, 但活性低于对照物环丙沙星和氧氟沙星; 目标化合物对绿脓杆菌无抑菌活性, 最低抑菌浓度(MIC)均大于20 g/mL.

关键词: 氟喹诺酮, 环丙沙星, 合成, 抗菌活性

Sixteen new 1-cyclopropyl-6-fluoro-7-(4-acyl-1-piperazinyl)-1,4-dihydro-4-oxo-quinoline-3- carboxylic acids were synthesized from 1-cyclopropyl-6-fluoro-7-chloro-1,4-dihydro-4-oxo-quinoline-3- carboxylic acid. The structures of the new compounds were characterized by IR, 1H NMR, 13C NMR, MS spectra and elemental analysis. Antibacterial activity tests in vitro indicated that most of the target compounds possessed relatively high inhibiting activity against Escherichia coli, but lower than ciprofloxacin and ofloxacin. The target compounds had no inhibiting activity against Pseudomonas aeruginosa.

Key words: ciprofloxacin, fluoroquinolone, synthesis, antibacterial activity