OXIDATION OF AZAHETEROCYCLES WITH MAMMALIAN LIVER ALDEHYDE OXIDASE

被引：51

作者：

STUBLEY, C

STELL, JGP

MATHIESON, DW

机构：

[1] Department of Pharmaceutical Chemistry, University of Bradford, Bradford, West Yorkshire

来源：

XENOBIOTICA | 1979年 / 9卷 / 08期

关键词：

D O I：

10.3109/00498257909087261

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. Isoquinoline, cinnoline, quinoxaline, quinazoline and phthalazine were incubated with preparations of rabbit liver aldehyde oxidase. 2. The oxidation products, 1-hydroxyisoquinoline, 4-hydroxycinnoline, 2-hydroxy-and 2,3-dihydroxy-quinoxaline, 4-hydroxy- and 2,4-dihydroxy-quinazoline, and 1 -hydroxyphthalazine were identified by comparison of their spectral and chromatographic characteristics with those of authentic compounds. 3. Michaelis-Menten constants are reported for the action of the parent heterocycles with aldehyde oxidase. The compounds reported in this study are among the most efficient substrates yet described for rabbit liver aldehyde oxidase. 4. The compounds in 1 above were incubated with bovine milk xanthine oxidase: only quinazoline and phthalazine yielded significant amounts of metabolites. Km values were calculated for these compounds. 5. Incubation of the heterocycles with rat liver preparations gave qualitatively the same results as those obtained using rabbit liver, but smaller amounts of the oxidation products were detected from rat liver incubations. © 1979 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted.

引用

页码：475 / 484

页数：10

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