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抗支原体喹诺酮的合成及其构效关系
引用本文:杨玉社,嵇汝运,陈凯先,叶辉,武济民.抗支原体喹诺酮的合成及其构效关系[J].药学学报,1999,34(5):349-352.
作者姓名:杨玉社  嵇汝运  陈凯先  叶辉  武济民
作者单位:中国科学院上海药物研究所,上海,200031
摘    要:目的:开发新型抗支原体药物。方法与结果:设计合成了一系列新型左旋氧氟沙星类似物(18~24),测试其体外抗支原体活性(MIC值),并讨论了他们的构效关系。结论:所合成的化合物有较好的抗支原体活性。哌嗪环或高哌嗪环4位氮原子有吸电子基团时,可能有利于提高喹诺酮的抗支原体活性。

关 键 词:左旋氧氟沙星  氟喹诺酮  合成  抗菌活性
收稿时间:1998-04-17
修稿时间:: 1998-04-

STUDIES ON SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF ANTIMYCOPLASMA QUINOLONES
Yang Yushe,Ji Ruyun,Chen Kaixian,Ye Hui,Wu Jimin.STUDIES ON SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF ANTIMYCOPLASMA QUINOLONES[J].Acta Pharmaceutica Sinica,1999,34(5):349-352.
Authors:Yang Yushe  Ji Ruyun  Chen Kaixian  Ye Hui  Wu Jimin
Abstract:AIM: To develop new antimycoplasma drugs. METHODS and RESULTS: A series of new analogues of (S)(-)ofloxacin with antimycoplasma activities were prepared. Compounds 1824 were new compounds. Their in vitro susceptibilities to mycoplama were tested. The influences on structureactivity relationships were also discussed. CONCLUSION: The synthesized compounds have good activities against mycoplasma. The electronwithdrawing groups on the 4position of piperazine or homopiperazine may be favorable for antimycoplasma activity.
Keywords:antitmycoplamasa quinolone  mycoplasma  (S)(-)ofloxacin  synthesis  
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