| 5-氨基-8-甲氧基-喹诺酮类的合成及其体外抗菌作用 |
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| 引用本文： | 刘明亮,王秀云,郭慧元. 5-氨基-8-甲氧基-喹诺酮类的合成及其体外抗菌作用[J]. 中国抗生素杂志, 2007, 32(2): 81-83 |
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| 作者姓名： | 刘明亮 王秀云 郭慧元 |
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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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| 基金项目： | 致谢：MS、^1H-NMR谱和[α]D由中国医学科学院药物研究所分析室代测;体外抗菌活性由本所药理室代测. |
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| 摘 要： | 以1-环丙基-6，7-二氟-8-甲氧基-1，4-二氢-4-氧代喹啉-3-羧酸乙酯为起始原料依次经过硝化、还原和水解三步反应制得5-氨基-1-环丙基-6，7-二氟-8-甲氧基-1，4-二氢-4-氧代喹啉-3-羧酸，然后分别与2（R）-（-）／2（S）-（＋）或2（R，S）-甲基哌嗪缩合，得到3种目标化合物（5a、5b和5c）。测定它们对20株临床分离和标准革兰阴性菌和标准革兰阳性菌的最低抑菌浓度。结果表明，5a和5b的体外抗菌活性与外消旋体5c基本相当。
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| 关 键 词： | 5-氨基-8-甲氧基喹诺酮 光学异构体 合成 体外抗菌活性 |
| 文章编号： | 1001-8689(2007)02-0081-03 |
| 修稿时间： | 2006-08-11 |
Syntheses and in vitro antibacterial activity of 5-amino-8-methoxyl-quinolones |
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| Liu Ming-liang,Wang Xiu-yun,Guo Hui-yuan. Syntheses and in vitro antibacterial activity of 5-amino-8-methoxyl-quinolones[J]. Chinese Journal of Antibiotics, 2007, 32(2): 81-83 |
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| Authors: | Liu Ming-liang Wang Xiu-yun Guo Hui-yuan |
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| Affiliation: | Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050 |
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| Abstract: | 5-amino-1-cyclopropyl-6-fluoro-8-methoxyl-7-[3(R)/3(S)/3(R,S)-methyl-piperazin-1-yl]-1,4-dihydro-4-oxoquinoline-3-carboxylic acid(5a,5b,5c) were synthesized from ethyl 5-amino-1-cyclopropyl-6,7-difluoro-8-methoxyl-1,4-dihydro-4-oxoquinoline-3-carboxylate(1) via nitration,reduction,hydrolysis,and then condensation with 2(R)-(-)/2(S)-(+) or 2(R,S)-methylpiperazine.The in vitro antibacterial activities of 5a and 5b against 20 Gram-negative and Gram-positive bacteria were comparable to that of racemic compound 5c. |
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| Keywords: | 5-amino-8-methoxylquinolone Optical isomer Synthesis In vitro antibacterial activity |
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