SYNTHESIS OF ANTIMICROBIAL AGENTS .5. IN-VIVO METABOLISM OF 7-(4-HYDROXYPIPERAZIN-1-YL) QUINOLONES

被引：5

作者：

UNO, T

OKUNO, T

KAWAKAMI, K

SAKAMOTO, F

TSUKAMOTO, G

机构：

[1] Pharmaceuticals Research Center, Kanebo Ltd., Osaka 534, 1-5-90 Tomobuchi-cho, Miyakojima-ku

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 19期

关键词：

D O I：

10.1021/jm00071a001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel pyridone carboxylic acids having a 4-hydroxypiperazin-1-yl, a 4-hydroxy-3-methylpiperazin-1-yl, and a 4-hydroxy-3,5-dimethylpiperazin-1-yl group was prepared, and their metabolism to corresponding piperazinyl derivatives after oral administration to mice and rats was studied. This reductive metabolism appeared to be more extensive in mice than in rats. Moreover, the introduction of a methyl group into the alpha-position of the 4-hydroxy group depressed the metabolism in both species.

引用

页码：2711 / 2715

页数：5

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