Design and development of novel thiazole-sulfonamide derivatives as a protective agent against diabetic cataract in Wistar rats via inhibition of aldose reductase

IF 1.3 3区化学 Q3 CHEMISTRY, ORGANIC

Heterocyclic Communications Pub Date : 2021-01-01 DOI:10.1515/hc-2020-0124

L. Yin, Mingxue Zhang, Tian-geng He

引用次数: 1

Abstract

Abstract In recent years, ALR2 (aldose reductase) inhibitors have attracted attention for their effective ability to reduce the progression of diabetes-associated cataracts. Therefore, in the present article, we intended to develop novel thiazole-sulfonamide hybrids as a potent inhibitor of ALR2. These molecules significantly inhibited the ALR2 level in the rat lenses homogenate, where the most potent compound 7b showed activity comparable to sorbinil as standard. In Wistar rats, compound 7b improved the insulin level and body weight of the experimental animal together with a reduction in the glucose output. Compound 7b showed a significant reduction in the expression of ALR2 in rat lenses in western blot analysis.

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新型噻唑-磺酰胺衍生物通过抑制醛糖还原酶对Wistar大鼠糖尿病性白内障的保护作用的设计与研制

近年来，醛糖还原酶(ALR2)抑制剂因其能有效降低糖尿病相关性白内障的进展而备受关注。因此，在本文中，我们打算开发新的噻唑-磺胺杂交体作为ALR2的有效抑制剂。这些分子显著抑制了大鼠晶状体匀浆中ALR2的水平，其中最有效的化合物7b显示出与山梨醇相当的活性。在Wistar大鼠中，化合物7b改善了实验动物的胰岛素水平和体重，同时减少了葡萄糖输出。western blot结果显示，化合物7b显著降低了大鼠晶状体中ALR2的表达。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Heterocyclic Communications 化学-有机化学

CiteScore

3.80

自引率

4.30%

发文量

审稿时长

1.4 months

期刊介绍： Heterocyclic Communications (HC) is a bimonthly, peer-reviewed journal publishing preliminary communications, research articles, and reviews on significant developments in all phases of heterocyclic chemistry, including general synthesis, natural products, computational analysis, considerable biological activity and inorganic ring systems. Clear presentation of experimental and computational data is strongly emphasized. Heterocyclic chemistry is a rapidly growing field. By some estimates original research papers in heterocyclic chemistry have increased to more than 60% of the current organic chemistry literature published. This explosive growth is even greater when considering heterocyclic research published in materials science, physical, biophysical, analytical, bioorganic, pharmaceutical, medicinal and natural products journals. There is a need, therefore, for a journal dedicated explicitly to heterocyclic chemistry and the properties of heterocyclic compounds.