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本文介绍一系列新的芳基氟喹诺酮类的合成及抗菌作用。这些衍生物的特点是在6-位有氟原子,在7-位有取代氨基,在1-位有取代苯基。构效关系研究指出,当1-取代基是对-氟苯基或对-羟基苯基及7-取代基是1-哌嗪基、4-甲基-1-哌嗪基或3-氨基-1-吡略烷基时,体外抗菌活力最大。其中A-56620(1)和A-56619(2)(分别为norfloxacin及pefloxacin的N-乙基被对-氟苯基所置换)以及3体外试验具有广谱和强效的抗菌作
This article describes a series of new aryl fluoroquinolones synthesis and antibacterial activity. These derivatives are characterized by having a fluorine atom at the 6-position, a substituted amino group at the 7-position and a substituted phenyl group at the 1-position. The structure-activity relationship study indicates that when the 1-substituent is p-fluorophenyl or p-hydroxyphenyl and the 7-substituent is 1-piperazinyl, 4-methyl-1-piperazinyl or 3-amino- 1-pyrrolidinyl, the largest antibacterial activity in vitro. Among them, A-56620 (1) and A-56619 (2) (N-ethyl groups of norfloxacin and pefloxacin, respectively, substituted by p-fluorophenyl groups) and 3 in vitro test have broad spectrum and potent antibacterial activity