IRREVERSIBLE ENZYME INHIBITORS .156. ACTIVE-SITE-DIRECTED IRREVERSIBLE INHIBITORS OF XANTHINE OXIDASE DERIVED FROM 9-(ACYLAMIDOPHENYL)GUANINES SUBSTITUTED WITH A TERMINAL SULFONYL FLUORIDE

被引：16

作者：

BAKER, BR

WOOD, WF

机构：

[1] Department of Chemistry, University of California, Santa Barbara

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1969年 / 12卷 / 02期

关键词：

D O I：

10.1021/jm00302a003

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Twenty candidate active-site-directed irreversible inhibitors of xanthine oxidase have been synthesized and evaluated. These were derived from m-or p-amino-9-phenylguanine attached to benzenesulfonyl fluoride by a sulfonamide, carboxamide, or urea bridge. Three excellent irreversible inhibitors emerged that at a concentration of 10-6 to 10-7 M gave total inactivation of xanthine oxidase with a half-life of 1 min or less; these were 9-phenylguanines substituted by a p-(p-fluorosulfonylbenzamido) (2), p-(m-fluorosulfonylbenzamido) (7), or m-(p-fluorosulfonylbenzenesulfonamido) (21) moiety. © 1969, American Chemical Society. All rights reserved.

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页码：211 / &

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