李向红, 田治明, 苗华, 余兰香, 郭惠元. 吡酮酸类抗菌药物的研究 XII.6-氯-1-环丙基-7-(1-哌嗪基)-1,4-二氢-4-氧代喹啉-3-羧酸及其类似物的合成与抗菌作用J. 药学学报, 1997, 32(11): 844-851.
引用本文: 李向红, 田治明, 苗华, 余兰香, 郭惠元. 吡酮酸类抗菌药物的研究 XII.6-氯-1-环丙基-7-(1-哌嗪基)-1,4-二氢-4-氧代喹啉-3-羧酸及其类似物的合成与抗菌作用J. 药学学报, 1997, 32(11): 844-851.
XH Li, ZM Tian, H Miao, LX Yu , HY Guo, . STUDIES ON PYRIDONECARBOXYLIC ACIDS AS ANTIBACTERIAL AGENTS XII. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF 6-CHLORO-1-CYCLOPROPYL-7-(1-PIPERAZINYL)-1,4-DIHYDRO-4-OXO-QUINOLINE-3-CARBOXYLIC ACID AND ANALOGUESJ. Acta Pharmaceutica Sinica, 1997, 32(11): 844-851.
Citation: XH Li, ZM Tian, H Miao, LX Yu , HY Guo, . STUDIES ON PYRIDONECARBOXYLIC ACIDS AS ANTIBACTERIAL AGENTS XII. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF 6-CHLORO-1-CYCLOPROPYL-7-(1-PIPERAZINYL)-1,4-DIHYDRO-4-OXO-QUINOLINE-3-CARBOXYLIC ACID AND ANALOGUESJ. Acta Pharmaceutica Sinica, 1997, 32(11): 844-851.

吡酮酸类抗菌药物的研究 XII.6-氯-1-环丙基-7-(1-哌嗪基)-1,4-二氢-4-氧代喹啉-3-羧酸及其类似物的合成与抗菌作用

STUDIES ON PYRIDONECARBOXYLIC ACIDS AS ANTIBACTERIAL AGENTS XII. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF 6-CHLORO-1-CYCLOPROPYL-7-(1-PIPERAZINYL)-1,4-DIHYDRO-4-OXO-QUINOLINE-3-CARBOXYLIC ACID AND ANALOGUES

  • 摘要: 合成了16个6-氯-1-环丙基-7-(1-哌嗪基)-1,4-二氢-4-氧代喹啉-3-羧酸及其类似物,并测定了抗菌活性,结果表明,化合物11Ca及11Cc对金葡菌-15的活性是环丙沙星的4倍,对大肠杆菌-22和绿脓杆菌-29的活性与环丙沙星相当。

     

    Abstract: Sixteen pyridonecarboxylic acids, characterized by having a chlorine atom and a cyclopropyl group at the 6- and 1-position respectively, substituted amino groups at the 7-position, and some substituted groups (chloro, nitro, amino, dimethylamino) at the 8-position, were synthesized. In vitro antibacterial activities of these compounds were tested. The fluoroquinolones ciprofloxacin and norfloxacin were included for comparative purposes. The results showed that both 11Ca and 11Cc were 4-8 times more active than ciprofloxacin and norfloxacin against S. aureus-15 in vitro, but with the same activity as ciprofloxacin against E. coli-22 and P.aeruginosa-29.

     

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