抗支原体喹诺酮的合成及其构效关系

STUDIES ON SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF ANTIMYCOPLASMA QUINOLONES

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。

Abstract: AIM: To develop new antimycoplasma drugs. METHODS and RESULTS: A series of new analogues of (_S)-(-)-ofloxacin with antimycoplasma activities were prepared. Compounds 18～24 were new compounds. Their _{in vitro} susceptibilities to mycoplama were tested. The influences on structure-activity relationships were also discussed. CONCLUSION: The synthesized compounds have good activities against mycoplasma. The electron-withdrawing groups on the 4-position of piperazine or homopiperazine may be favorable for antimycoplasma activity.