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

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.

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

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 com-pounds possessed relatively high inhibiting activity against Escherichia coli, but lower than ciprofloxacin and ofloxacin. The target compounds had no inhibiting activity against Pseudomonas aeruginosa.