| 左旋氧氟沙星类似物的合成及其构效关系 |
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| 引用本文： | 杨玉社,嵇汝运,胡增建,陈凯先,武济民.左旋氧氟沙星类似物的合成及其构效关系[J].药学学报,1999,34(3):197-202. |
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| 作者姓名： | 杨玉社 嵇汝运 胡增建 陈凯先 武济民 |
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| 作者单位： | 中国科学院上海药物研究所,上海,200031 |
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| 摘 要： | 目的：发现新型高效的喹诺酮类抗菌药。方法和结果：设计合成了23个左旋氧氟沙星类似物，其中化合物5～23为新化合物，测定了它们对5株革兰阳性菌和5株革兰阴性菌的体外抗菌活性(MIC)，并讨论了构效关系。结论：8-位氨基有利于提高喹诺酮抗阳性菌活性，化合物13，14的抗菌活性优于对照样品左旋氧氟沙星及环丙沙星。
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| 关 键 词： | 左旋氧氟沙星 氟喹诺酮 合成 抗菌活性 |
| 收稿时间： | 1998-04-18 |
| 修稿时间： | : 1998-04- |
SYNTHESIS AND STRUCTURE ACTIVITIES RELATIONSHIP OF LEVOFLOXACIN ANALOGUES |
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| Yang Yushe,Ji Ruyun,Hu zengjian,Chen Kaixian,Wu Jimin.SYNTHESIS AND STRUCTURE ACTIVITIES RELATIONSHIP OF LEVOFLOXACIN ANALOGUES[J].Acta Pharmaceutica Sinica,1999,34(3):197-202. |
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| Authors: | Yang Yushe Ji Ruyun Hu zengjian Chen Kaixian Wu Jimin |
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| Abstract: | AIM: To discover new potent quinolone antibacterial agents. METHODS AND RESULTS: A series of novel analogues of levofloxacin has been prepared. These compounds were evaluated for in vitro activity by determining minimum inhibitory concentrations against a variety of bacteria. The structure activity relationships were also discussed. CONCLUSION: The results showed that the 8 amino group was very favorable for antibacterial activity. Compounds 13 and 14 were superior to the reference compounds levofloxacin and ciprofloxacin and were selected as promising candidates for further studies. |
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| Keywords: | levofloxacin fluoroquinolone synthesis antibacterial activity |
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