左旋氧氟沙星类似物的合成及其抗菌抗肿瘤活性研究  

STUDIES ON SYNTHESIS ANTIBACTERIAL AND ANTITUMOR ACTIVITY OF (S) (-) OFLOXACIN ANALOGUES

作　　者：杨玉社[1] 嵇汝运[1] 陈凯先[1] 丁健[1] 

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2期119-124,共6页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金;上海市科技启明星计划资助项目

摘　　要：目的：设计合成有抗菌抗肿瘤活性的喹诺酮药物。方法和结果：根据推理药物设计原理，设计并合成了１６个新型抗菌抗肿瘤喹诺酮类化合物，并研究其构效关系。结论：用９株细菌及４株肿瘤细胞评价了它们的体外抗菌活性（ＭＩＣ值）及抗肿瘤活性（抑瘤率％）。其中。AIM: To design and prepare quinolone compounds with antibacterial and antitumor activities. METHODS AND RESULTS: According to rational drug design principle, a series of novel analogues of (S) (-) ofloxacin has been prepared and the influences on structure activity relationships was also discussed. CONCLUSION: Their in vitro antitumor and antibacterial activities were evaluated. The results showed that compound 16～20 have good antitumor and antibacterial activities.

关 键 词：左旋氧氟沙星 合成 抗肿瘤活性 抗菌活性 

分 类 号：R978.19[医药卫生—药品] R914.5[医药卫生—药学]