NAPHTHALENYLSULFONYL-HYDANTOINS AS ALDOSE REDUCTASE INHIBITORS

被引：6

作者：

MALAMAS, MS ^{[1
]}

SESTANJ, K ^{[1
]}

MILLEN, J ^{[1
]}

机构：

[1] WYETH AYERST RES,SUBDIV METAB DISORDERS,PRINCETON,NJ 08543

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 26卷 / 04期

关键词：

ALDOSE REDUCTASE INHIBITOR; DIABETIC COMPLICATIONS; ANTICONVULSANT ACTIVITY; GALACTOSEMIC RAT MODEL;

D O I：

10.1016/0223-5234(91)90096-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Accumulation of intracellular sorbitol, formed from glucose by aldose reductase, is believed to play an important role in the development of certain chronic complications of diabetes mellitus. Several 1-(naphthalenylsulfonyl)hydantoins inhibit aldose reductase isolated from bovine lens in vitro, and decrease galactitol formation in sciatic nerves of galactosemic rats in vivo. The 5-bromo analogue (entry 12, table I) was found to be the most orally active aldose reductase inhibitor of this series with an ED50 value of 8.1 mg/kg po. The 1-(naphthalenylsulfonyl)-2-thiohydantoin analogues with the exception of entry 11 (table I) which showed good in vivo activity, were either inactive or had only marginal activity.

引用

页码：369 / 374

页数：6

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