Highly selective aldose reductase inhibitors .2. Optimization of the aryl part of 3-(arylmethyl)-2,4,5-trioxoimidazolidine-1-acetic acids

被引：0

作者：

Kotani, T ^{[1
]}

Ishii, A ^{[1
]}

Nagaki, Y ^{[1
]}

Toyomaki, Y ^{[1
]}

Yago, H ^{[1
]}

Suehiro, S ^{[1
]}

Okukado, N ^{[1
]}

Okamoto, K ^{[1
]}

机构：

[1] NIPPON ZOKI PHARMACEUT CO LTD, INST BIOACT SCI, YASHIRO, HYOGO 67314, JAPAN

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 1997年 / 45卷 / 02期

关键词：

diabetic complication; aldose reductase inhibitor; aldose reductase; aldehyde reductase; selectivity; 2,4,5-trioxoimidazolidine-1-acetic acid;

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Accumulation of intracellular sorbitol, the product of glucose reduction catalyzed by aldose reductase (AR) [EC 1.1.1.21], is thought to be the main culprit in the development of diabetic complications, A series of 3-arylalkyl-2,4,5-trioxoimidazolidine-1-acetic acids was prepared and tested for inhibitory activities towards AR and aldehyde reductase (ALR) [EC 1.1.1.2]. These derivatives showed strong inhibitory activity against AR without markedly inhibiting ALR, In particular, the compounds with 3-nitrophenyl, 4-chloro-3-nitrophenyl, and chloro-substituted benzothiazolyl groups as the aryl part showed powerful AR-inhibitory activity, The chlorosubstituted benzothiazolyl compound showed an AR selectivity of more than 5000 fold.

引用

页码：297 / 304

页数：8

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