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.
出处
《药学学报》
CAS
CSCD
北大核心
1999年第3期197-202,共6页
Acta Pharmaceutica Sinica
基金
国家自然科学基金
关键词
左旋氧氟沙星
氟喹诺酮
合成
抗菌活性
levofloxacin
fluoroquinolone
synthesis
antibacterial activity
