Microsomal N-hydroxylation of the glycolamide 2-(glycolylamino)fluorene to give the glycolylhydroxamic acid. A new xenobiotic reaction.
Microsomal N-hydroxylation of the glycolamide 2-(glycolylamino)fluorene to give the glycolylhydroxamic acid. A new xenobiotic reaction.
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乙醇酰胺 2-(乙醇酰氨基)芴的微粒体 N-羟基化得到乙醇酰异羟肟酸。
DOI：
10.1021/tx00016a004
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发表时间：
1990
影响因子：
4.1
通讯作者：
Wei,CI
中科院分区：
文献类型：
--
作者：
Corbett,MD;Corbett,BR;Quintana,SJ;Hannothiaux,MH;Wei,CI
发现乙醇酰胺2-（乙酰氨基）芴部分被诱导的大鼠肝微粒体代谢为异羟肟酸N-羟基-2-（乙酰氨基）芴。这是首次报道微粒体系统进行乙醇酰胺N-羟基化的能力。比较2-氨基芴的乙酰基酰胺和羟乙酰基酰胺的相对代谢速率，发现前者产生的异羟肟酸大约是后者的两倍。另一方面，乙醇酰胺的总体代谢速度略快于乙酰同类物。在NADPH存在下，通过微粒体制剂，羟乙酰基和乙酰基衍生的异羟肟酸均进一步代谢为未知产物。
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.