| 莫西沙星前药的合成及其体内外抗菌活性 |
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| 引用本文： | 刘明亮,魏永刚,孙兰英,张淑华,郭慧元.莫西沙星前药的合成及其体内外抗菌活性[J].中国抗生素杂志,2003,28(11):647-652. |
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| 作者姓名： | 刘明亮 魏永刚 孙兰英 张淑华 郭慧元 |
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| 作者单位： | 1. 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
2. 中国医药集团四川抗菌素工业研究所,成都,610051 |
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| 摘 要： | 分别以N-叔丁氧羰基氨基酸和莫西沙星为原料，经缩合、脱氨基保护基、中和得到8种含有氨基酰基的前药，按同样程序，还得到了2种含有二肽的前药。测定了10种莫西沙星前药及对照药对20株临床分离的革兰氏阳性菌的最小抑菌浓度以及对小鼠腹腔感染金黄色葡萄球菌01193和肺炎链球菌01182的体内保护疗效，结果表明，10种前药的体内外抗菌活性均低于左氧氟沙星和盐酸莫西沙星。
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| 关 键 词： | 氟喹诺酮 莫西沙星前药 合成 体内外活性 |
| 文章编号： | 1001-8689(2003)11-647-06 |
| 修稿时间： | 2002年12月18 |
Synthesis and the in vivo and in vitro antibacterial activity of moxifloxacin prodrugs |
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| Liu Ming liang,Wei Yong gang,Sun Lan ying,Zhang Shu Hua and Guo Hui yuan.Synthesis and the in vivo and in vitro antibacterial activity of moxifloxacin prodrugs[J].Chinese Journal of Antibiotics,2003,28(11):647-652. |
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| Authors: | Liu Ming liang Wei Yong gang Sun Lan ying Zhang Shu Hua and Guo Hui yuan |
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| Institution: | Liu Ming liang1,Wei Yong gang1,Sun Lan ying1,Zhang Shu Hua2 and Guo Hui yuan1 |
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| Abstract: | Ten prodrugs of moxifloxacin were synthesized via condensation of N tert butoxycarbnyl amino acids and moxifloxacin,hydrolysis to remove the N protecting groups and neutrolization. The in vitro antibacterial activity against 20 Gram positive bacteria and in vivo antibacterial activity against S.aureus 01193 and S.pneumoniae 01182 of these compounds are lower than that of moxifloxacin hydrochloride and levofloxacin. |
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| Keywords: | Fluoroquinolone Moxifloxacin prodrugs Synthesis In vitro and in vivo activity |
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