吡酮酸类抗菌药物的研究XIV.7,8-双取代-1-环丙基-6-甲基-1,4-二氢-4-氧代喹啉-3-羧酸类化合物的合成与构效关系  

STUDIES ON PYRIDONECARBOXYLIC ACIDS AS ANTIBACTERIALAGENTS XIV. SYNTHESIS AND STRUCTUREACTIVITYRELATIONSHIPS OF 7,8-DISUBSTITUTED-1-CYCLOPROPYL-6-METHYL-1,4-DIHYDRO-4-OXO-3-QUINOLINE CARBOXYLIC ACIDS

作　　者：王洪权[1] 戚建军[1] 孙兰英[1] 余兰香[1] 郭惠元[1] 

机构地区：[1]中国医学科学院中国协和医科大学医药生物技术研究所

出　　处：《药学学报》1998年第9期675-681,共7页Acta Pharmaceutica Sinica

摘　　要：合成了１８个１环丙基６甲基７取代氨基，８位为Ｈ，Ｃｌ，ＮＯ２，ＮＨ２的６位非氟吡酮酸类化合物，测定了它们对１０株革兰氏阳性和革兰氏阴性细菌的ＭＩＣ值，并与环丙沙星、诺氟沙星对照。Eighteen pyridonecarboxylic acids, characterized by a methyl group at the C_6position instead of the usual florine atom, cyclopropyl at the N_1position, substituted amino groups at the C_7position, and some subtituted groups (hydrogen, chlorine, nitro and amino) at the C_8position, were synthesized. The in vitro antibacterial activity of these compounds were tested, and the structureactivity relationships were also discussed. The results of the study showed that the activity of compounds 22 and 24 were less potent than that of ciprofloxacin against S.aureus, S.epidermidis, E.coli and P.aeruginosa, while they were 2～100 times more potent than ciprofloxacin against K.pneumoniae, S.marcescens, A.calcoacetous, E.aerogenes, S.typhi and S.typhimurium.

关 键 词：吡酮酸 喹诺酮衍生物 构效关系 合成 

分 类 号：TQ463.54[化学工程—制药化工]