| 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 |
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| 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 |
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| 作者姓名： | 李向红 田治明 苗华 余兰香 郭惠元 |
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| 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,北京100050 |
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| 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。
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| 关 键 词： | 吡酮酸 喹诺酮衍生物 抗菌活性 |
| 收稿时间： | 1996-12-06 |
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 |
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| X H Li,Z M Tian,H Miao,L X Yu,H Y 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, 32(11): 844-851 |
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| Authors: | X H Li Z M Tian H Miao L X Yu H Y Guo |
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| Affiliation: | Institute of Medicinal Biotechnology, Chinese Acadeny of Medical Sciences, Peking Union Medical College, Beijing 100050. |
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| 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 11 Ca and 11 Cc 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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| Keywords: | Quinolone derivatives Antibacterial activity Pyridonecarboxylic acid |
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