抗支原体喹诺酮的合成及其构效关系  

STUDIES ON SYNTHESIS AND STRUCTUREACTIVITY RELATIONSHIPS OF ANTIMYCOPLASMA QUINOLONES

作　　者：杨玉社[1] 嵇汝运[1] 陈凯先[1] 叶辉 武济民 

机构地区：[1]中国科学院上海药物研究所

出　　处：《药学学报》1999年第5期349-352,共4页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金

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。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.

关 键 词：左旋氧氟沙星 氟喹诺酮 合成 抗菌活性 

分 类 号：R978.19[医药卫生—药品]