| 莫西沙星8-二氟甲氧基类似物的合成与体内外抗菌作用 |
| |
| 引用本文： | 刘九雨,吕妍,王玉成,郭慧元. 莫西沙星8-二氟甲氧基类似物的合成与体内外抗菌作用[J]. 中国抗生素杂志, 2006, 31(9): 559-562 |
| |
| 作者姓名： | 刘九雨 吕妍 王玉成 郭慧元 |
| |
| 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,北京,100050 |
| |
| 基金项目： | 致谢：MS和^1H NMR谱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,体内抗菌活性由四川抗菌素工业研究所药理室张淑华、欧真蓉代测. |
| |
| 摘 要： | 1-环丙基-6，7-二氟-8-甲氧基-1，4-二氢．4-氧代喹啉．3-羧酸乙酯依次经醚键断裂、酯化、二氟甲基醚化得1．环丙基-6，7-二氟-8-二氟甲氧基-1，4-二氢-4-氧代喹啉．3-羧酸乙酯，然后经过螫合、与[1S，6S]-2．叔丁氧羰基．2，8．二氮杂双环[4，3，0]壬烷缩合、最后脱除叔丁氧羰基保护得到1-环丙基．8．二氟甲氧基-7-[（1S，6S）．2，8．二氮杂双环[4，3，0]壬烷．8．基]-6-氟．1，4-二氢-4-氧代喹啉-3-羧酸。目标化合物的结构经核磁共振氢谱和质谱（ESI）所确证，并测定了其体内外抗菌作用，结果表明该化合物优于对照药环丙沙星，与莫西沙星相当或略优，尤其对肺炎链球菌29074的体内活性突出，值得深入评价。
|
| 关 键 词： | 喹诺酮 莫西沙星类似物 合成 抗菌作用 |
| 文章编号： | 1001-8689(2006)09-0559-04 |
| 收稿时间： | 2006-01-27 |
| 修稿时间： | 2006-01-27 |
Synthesis and antibacterial activity in vitro and in vivo of 8-diflouromethoxy quinolone: analogue of moxifloxacin |
| |
| Liu Jiu-yu,Lü Yan,Wang Yu-cheng,Guo Hui-yuan. Synthesis and antibacterial activity in vitro and in vivo of 8-diflouromethoxy quinolone: analogue of moxifloxacin[J]. Chinese Journal of Antibiotics, 2006, 31(9): 559-562 |
| |
| Authors: | Liu Jiu-yu Lü Yan Wang Yu-cheng Guo Hui-yuan |
| |
| Affiliation: | Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050 |
| |
| Abstract: | 1-cyclopropyl-7-(S,S)-2,8-diazabicyclo4.3.0non-8-yl-6-fluoro-8-difloro-methoxy-1,4-dihydro-4-oxo-3-quinoline carboxylic acid was prepared and evaluated for antibacterial activity in vitro and in vivo. The compound had better activity than ciprofloxacin in vitro and has similar activity as or better activity than moxifloxacin in vitro and in vivo. Especially against S.pneumoniae 29074, the compound and moxifloxacin have i.v. ED50 of 1.84 and 3.67mg/kg respectively. Consequently, the compound was selected as candidate for further evaluation. |
| |
| Keywords: | Quinolone Analogue of moxifloxacin Synthesis Antibacterial activity |
| 本文献已被 CNKI 维普 万方数据 等数据库收录！ |
