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ED_(50)分别为2.30,8.48,4.28,2.77,4.46,5.68和0.75(mg/kg)。
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.
出处
《药学学报》
CAS
CSCD
北大核心
1991年第2期111-116,共6页
Acta Pharmaceutica Sinica
基金
中国医学科学院科研基金
关键词
吡酮酸
前药
抗菌活性
Pyridonecarboxylic acids
Prodrug
Pivaloyloxymethyl ester
Antibacterial activity
