ALDOSE REDUCTASE INHIBITION BY 2,4-OXO AND THIOXO DERIVATIVES OF 1,2,3,4-TETRAHYDROQUINAZOLINE

被引：9

作者：

BILLON, F ^{[1
]}

DELCHAMBRE, C ^{[1
]}

CLOAREC, A ^{[1
]}

SARTORI, E ^{[1
]}

TEULON, JM ^{[1
]}

机构：

[1] UNION PHARMACOL SCI APPL LAB,F-92506 RUEIL MALMAISON,FRANCE

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 25卷 / 02期

关键词：

aldose reductase; diabetic complications; quinazoline;

D O I：

10.1016/0223-5234(90)90019-Y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibitors of aldose reductase are believed to be useful for the treatment of diabetic complications. Original [(2,4-dioxo-1,2,3,4-tetrahydro)quinazolin-1-yl] acetic acids and their thioxo derivatives have been synthesized and examined for their ability to inhibit aldose reductase in vitro and in vivo. Most were active in vitro on rat lens aldose reductase in the 10-7 molar range. Compound V16, which has a (2′-fluoro-4′-bromo)benzyl substituent on nitrogen N-3 was found in hypergalactosemic rats to be a good inhibitor of galactitol accumulation in sciatic nerves and to prevent cataract formation. © 1990.

引用

页码：121 / 126

页数：6

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