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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2021
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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) |
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alr2 compound synthesis hybrid diabetes cataract Organic chemistry QD241-441 |
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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 |
work_keys_str_mv |
AT yinliang designanddevelopmentofnovelthiazolesulfonamidederivativesasaprotectiveagentagainstdiabeticcataractinwistarratsviainhibitionofaldosereductase AT zhangmingxue designanddevelopmentofnovelthiazolesulfonamidederivativesasaprotectiveagentagainstdiabeticcataractinwistarratsviainhibitionofaldosereductase AT hetiangeng designanddevelopmentofnovelthiazolesulfonamidederivativesasaprotectiveagentagainstdiabeticcataractinwistarratsviainhibitionofaldosereductase |
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1718371698328207360 |