Identification and antimicrobial activity of urinary metabolites of a rifamycin derivative in dog

被引：8

作者：

Hosoe, K ^{[1
]}

Mae, T ^{[1
]}

Yamashita, K ^{[1
]}

Fujii, K ^{[1
]}

Yamane, T ^{[1
]}

Hidaka, T ^{[1
]}

Ohashi, T ^{[1
]}

机构：

[1] KANEKA CORP,FINE CHEM RES LABS,TAKASAGO,HYOGO 676,JAPAN

来源：

XENOBIOTICA | 1996年 / 26卷 / 03期

关键词：

D O I：

10.3109/00498259609046711

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. Three metabolites of the antimicrobial agent 3'-hydroxy-5'-(4-isobutyl-1-piperazinyl)benzoxazinorifamycin (KRM-1648) were isolated from dog urine obtained after administration of a single oral dose. These metabolites of KRM-1648 were identified by mass spectrometry and H-1 and C-13-nmr spectrometry. 2. Three metabolites of KRM-1648 were identified as 25-deacetyl KRM-1648, 30-hydroxy KRM-1648 and 25-deacetyl-30-hydroxy KRM-1648. 3. The antimicrobial activities of 25-deacetyl KRM-1648 were comparable with those of the parent compound, whereas 30-hydroxy KRM-1648 was equipotent and 2-8-fold less active than the parent compound against bacteria and mycobacteria, respectively.

引用

页码：321 / 332

页数：12

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