王洪权, 戚建军, 孙兰英, 余兰香, 郭惠元. 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J. 药学学报, 1998, 33(9): 675-681.
引用本文: 王洪权, 戚建军, 孙兰英, 余兰香, 郭惠元. 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J. 药学学报, 1998, 33(9): 675-681.
Wang Hongquan, Qi Jianjun, Sun Lanying, Yu Lanxiang , Guo Huiyuan, . 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 ACIDSJ. Acta Pharmaceutica Sinica, 1998, 33(9): 675-681.
Citation: Wang Hongquan, Qi Jianjun, Sun Lanying, Yu Lanxiang , Guo Huiyuan, . 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 ACIDSJ. Acta Pharmaceutica Sinica, 1998, 33(9): 675-681.

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

  • 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,讨论了它们的构效关系。

     

    Abstract: Eighteen pyridonecarboxylic acids, characterized by a methyl group at the C6-position instead of the usual florine atom, cyclopropyl at the N1-position, substituted amino groups at the C7-position, and some subtituted groups (hydrogen, chlorine, nitro and amino) at the C8-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.

     

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