左旋氧氟沙星类似物的合成及其构效关系  

SYNTHESIS AND STRUCTURE ACTIVITIES RELATIONSHIP OF LEVOFLOXACIN ANALOGUES

作　　者：杨玉社[1] 嵇汝运[1] 胡增建 陈凯先[1] 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3期197-202,共6页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金

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。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.

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] R914.5[医药卫生—药学]