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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
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(11).
作者姓名:李向红  田治明  苗华  余兰香  郭惠元
作者单位:中国医学科学院、中国协和医科大学医药生物技术研究所
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

关 键 词:吡酮酸  喹诺酮衍生物  抗菌活性

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
XH Li,ZM Tian,H Miao,LX Yu and 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 ANALOGUES[J].Acta Pharmaceutica Sinica,1997(11).
Authors:XH Li  ZM Tian  H Miao  LX Yu and HY Guo
Institution:XH Li,ZM Tian,H Miao,LX Yu and HY Guo *
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.
Keywords:Pyridonecarboxylic acid  Quinolone derivatives  Antibacterial activity
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