李卓荣, 郭惠元, 张致平. 吡酮酸类抗菌药物的研究——Ⅸ.若干吡酮酸类化合物前药的研究J. 药学学报, 1991, 26(2): 111-116.
引用本文: 李卓荣, 郭惠元, 张致平. 吡酮酸类抗菌药物的研究——Ⅸ.若干吡酮酸类化合物前药的研究J. 药学学报, 1991, 26(2): 111-116.
ZR Li, HY Guo , ZP Zhang, . STUDIES ON PYRIDONECARBOXYLIC ACIDS AS ANTIBACTERIAL AGENTS Ⅸ. STUDY ON PRODRUGS OF SOME PYRIDONECARBOXYLIC ACIDSJ. Acta Pharmaceutica Sinica, 1991, 26(2): 111-116.
Citation: ZR Li, HY Guo , ZP Zhang, . STUDIES ON PYRIDONECARBOXYLIC ACIDS AS ANTIBACTERIAL AGENTS Ⅸ. STUDY ON PRODRUGS OF SOME PYRIDONECARBOXYLIC ACIDSJ. Acta Pharmaceutica Sinica, 1991, 26(2): 111-116.

吡酮酸类抗菌药物的研究——Ⅸ.若干吡酮酸类化合物前药的研究

STUDIES ON PYRIDONECARBOXYLIC ACIDS AS ANTIBACTERIAL AGENTS Ⅸ. STUDY ON PRODRUGS OF SOME PYRIDONECARBOXYLIC ACIDS

  • 摘要: 合成了氟哌酸、环丙氟哌酸和氟啶酸的N-烷基化、羧基酯化或既烷基化又酯化的衍生物22个,并对其体内活性进行了研究。化合物ⅢAa,b,e;ⅢBa,e;ⅣA和ⅣB的ED50分别为2.30,8.48,4.28,2.77,4.46,5.68和0.75(mg/kg)。

     

    Abstract: Synthesis and antibacterial activity of pivaloyloxymethyl esters of norfloxacin, ciprofloxacin and their N-substituted derivatives are reported. In vivo antibacterial activities (EDso) of ⅢAa, b, e; ⅢBa, e; ⅣA and ⅣB were 2.30, 8.48, 4.28, 2.77, 4.46, 5.68 and 0.75 (mg/kg)respectively.

     

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