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

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 molec...

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Autores principales: Yin Liang, Zhang Mingxue, He Tiangeng
Formato: article
Lenguaje:EN
Publicado: De Gruyter 2021
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Acceso en línea:https://doaj.org/article/fcbbfce5d0d446fd9f55f238464cbc99
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spelling oai:doaj.org-article:fcbbfce5d0d446fd9f55f238464cbc992021-12-05T14:10:50ZDesign and development of novel thiazole-sulfonamide derivatives as a protective agent against diabetic cataract in Wistar rats via inhibition of aldose reductase2191-019710.1515/hc-2020-0124https://doaj.org/article/fcbbfce5d0d446fd9f55f238464cbc992021-09-01T00:00:00Zhttps://doi.org/10.1515/hc-2020-0124https://doaj.org/toc/2191-0197In 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.Yin LiangZhang MingxueHe TiangengDe Gruyterarticlealr2compound synthesishybriddiabetescataractOrganic chemistryQD241-441ENHeterocyclic Communications, Vol 27, Iss 1, Pp 63-70 (2021)
institution DOAJ
collection DOAJ
language EN
topic alr2
compound synthesis
hybrid
diabetes
cataract
Organic chemistry
QD241-441
spellingShingle alr2
compound synthesis
hybrid
diabetes
cataract
Organic chemistry
QD241-441
Yin Liang
Zhang Mingxue
He Tiangeng
Design and development of novel thiazole-sulfonamide derivatives as a protective agent against diabetic cataract in Wistar rats via inhibition of aldose reductase
description 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.
format article
author Yin Liang
Zhang Mingxue
He Tiangeng
author_facet Yin Liang
Zhang Mingxue
He Tiangeng
author_sort Yin Liang
title Design and development of novel thiazole-sulfonamide derivatives as a protective agent against diabetic cataract in Wistar rats via inhibition of aldose reductase
title_short Design and development of novel thiazole-sulfonamide derivatives as a protective agent against diabetic cataract in Wistar rats via inhibition of aldose reductase
title_full Design and development of novel thiazole-sulfonamide derivatives as a protective agent against diabetic cataract in Wistar rats via inhibition of aldose reductase
title_fullStr Design and development of novel thiazole-sulfonamide derivatives as a protective agent against diabetic cataract in Wistar rats via inhibition of aldose reductase
title_full_unstemmed Design and development of novel thiazole-sulfonamide derivatives as a protective agent against diabetic cataract in Wistar rats via inhibition of aldose reductase
title_sort design and development of novel thiazole-sulfonamide derivatives as a protective agent against diabetic cataract in wistar rats via inhibition of aldose reductase
publisher De Gruyter
publishDate 2021
url https://doaj.org/article/fcbbfce5d0d446fd9f55f238464cbc99
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AT zhangmingxue designanddevelopmentofnovelthiazolesulfonamidederivativesasaprotectiveagentagainstdiabeticcataractinwistarratsviainhibitionofaldosereductase
AT hetiangeng designanddevelopmentofnovelthiazolesulfonamidederivativesasaprotectiveagentagainstdiabeticcataractinwistarratsviainhibitionofaldosereductase
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