将甘醇酰胺2-（甘氨酰氨基）芴进行微粒体N-羟基化反应生成甘醇酰异羟肟酸。一种新的外源化合物反应。

Microsomal N-hydroxylation of the glycolamide 2-(glycolylamino)fluorene to give the glycolylhydroxamic acid. A new xenobiotic reaction.

作者信息

Corbett M D, Corbett B R, Quintana S J, Hannothiaux M H, Wei C I

机构信息

Food Science and Human Nutrition Department, University of Florida, Gainesville 32611.

出版信息

Chem Res Toxicol. 1990 Jul-Aug;3(4):296-300. doi: 10.1021/tx00016a004.

DOI:10.1021/tx00016a004

PMID:2133075

Abstract

The glycolamide 2-(glycolylamino)fluorene was found to be metabolized in part by induced rat liver microsomes to the hydroxamic acid N-hydroxy-2-(glycolylamino)fluorene. This is the first report of the ability of a microsomal system to carry out the N-hydroxylation of a glycolamide. A comparison of the relative rates of metabolism of the acetyl and glycolyl amides of 2-aminofluorene showed that the former gave about twice as much of the hydroxamic acid as did the latter. On the other hand, the overall metabolism of the glycolamide was slightly more rapid than that of the acetyl congener. Both the glycolyl- and acetyl-derived hydroxamic acids were further metabolized to unknown products by microsomal preparations in the presence of NADPH.

摘要

发现乙醇酰胺2 -（乙醇酰氨基）芴在部分诱导的大鼠肝微粒体中代谢为异羟肟酸N -羟基- 2 -（乙醇酰氨基）芴。这是关于微粒体系统进行乙醇酰胺N -羟基化能力的首次报道。对2 -氨基芴的乙酰酰胺和乙醇酰胺的相对代谢速率进行比较，结果表明前者产生的异羟肟酸量约为后者的两倍。另一方面，乙醇酰胺的整体代谢比乙酰同类物略快。在NADPH存在的情况下，微粒体制剂将乙醇酰基和乙酰基衍生的异羟肟酸进一步代谢为未知产物。