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Synthesis and Diuretic Activity of Substituted 1,3,4-Thiadiazoles
1,3,4-Thiadiazole nuclease, a 5-membered heterocyclic ring system containing two nitrogen and one sulfur atoms in addition to carbon atoms, is compound that showed promising results in the process of searching new diuretic agents. In this study, seven 5- and 2-thioate derivatives of 1, 3, 4-thiadiaz...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Hindawi
2022
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9012607/ https://www.ncbi.nlm.nih.gov/pubmed/35433072 http://dx.doi.org/10.1155/2022/3011531 |
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author | Ergena, Asrat Rajeshwar, Yerra Solomon, Gebremedhin |
author_facet | Ergena, Asrat Rajeshwar, Yerra Solomon, Gebremedhin |
author_sort | Ergena, Asrat |
collection | PubMed |
description | 1,3,4-Thiadiazole nuclease, a 5-membered heterocyclic ring system containing two nitrogen and one sulfur atoms in addition to carbon atoms, is compound that showed promising results in the process of searching new diuretic agents. In this study, seven 5- and 2-thioate derivatives of 1, 3, 4-thiadiazoles were synthesized by substitution reaction using acetone as solvent and K(2)CO(3) as a base. The compounds ware then characterized by using IR and NMR spectroscopy. The diuretic activity of the compounds was evaluated on Swiss albino mice by measuring urine volume, urinary pH, and urinary Na(+), K(+), and Cl(−). The result showed increase in urinary excretion of both water and electrolytes. 5-Methyl-substituted derivatives of 1, 3, 4-thiadiazoles showed significant increase in excretion of both water and electrolytes when they are compared to both negative control and 5-amino-substituted derivatives. The highest diuretic activity (0.82) was recorded for para-nitro-substituted benzene ring at 2-thioate group of 5-methyl-1, 3, 4-thiadiazole, while the least (0.56) was recorded for propanethioate group at 2(nd) position and amine group at 5(th) position of 1, 3, 4-thiadiazole. The finding of the present study showed that all the compounds have diuretic activity and 5-methyl derivatives of 1, 3, 4-thiadiazoles exhibited significant diuretic activity. |
format | Online Article Text |
id | pubmed-9012607 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Hindawi |
record_format | MEDLINE/PubMed |
spelling | pubmed-90126072022-04-16 Synthesis and Diuretic Activity of Substituted 1,3,4-Thiadiazoles Ergena, Asrat Rajeshwar, Yerra Solomon, Gebremedhin Scientifica (Cairo) Research Article 1,3,4-Thiadiazole nuclease, a 5-membered heterocyclic ring system containing two nitrogen and one sulfur atoms in addition to carbon atoms, is compound that showed promising results in the process of searching new diuretic agents. In this study, seven 5- and 2-thioate derivatives of 1, 3, 4-thiadiazoles were synthesized by substitution reaction using acetone as solvent and K(2)CO(3) as a base. The compounds ware then characterized by using IR and NMR spectroscopy. The diuretic activity of the compounds was evaluated on Swiss albino mice by measuring urine volume, urinary pH, and urinary Na(+), K(+), and Cl(−). The result showed increase in urinary excretion of both water and electrolytes. 5-Methyl-substituted derivatives of 1, 3, 4-thiadiazoles showed significant increase in excretion of both water and electrolytes when they are compared to both negative control and 5-amino-substituted derivatives. The highest diuretic activity (0.82) was recorded for para-nitro-substituted benzene ring at 2-thioate group of 5-methyl-1, 3, 4-thiadiazole, while the least (0.56) was recorded for propanethioate group at 2(nd) position and amine group at 5(th) position of 1, 3, 4-thiadiazole. The finding of the present study showed that all the compounds have diuretic activity and 5-methyl derivatives of 1, 3, 4-thiadiazoles exhibited significant diuretic activity. Hindawi 2022-04-08 /pmc/articles/PMC9012607/ /pubmed/35433072 http://dx.doi.org/10.1155/2022/3011531 Text en Copyright © 2022 Asrat Ergena et al. https://creativecommons.org/licenses/by/4.0/This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Ergena, Asrat Rajeshwar, Yerra Solomon, Gebremedhin Synthesis and Diuretic Activity of Substituted 1,3,4-Thiadiazoles |
title | Synthesis and Diuretic Activity of Substituted 1,3,4-Thiadiazoles |
title_full | Synthesis and Diuretic Activity of Substituted 1,3,4-Thiadiazoles |
title_fullStr | Synthesis and Diuretic Activity of Substituted 1,3,4-Thiadiazoles |
title_full_unstemmed | Synthesis and Diuretic Activity of Substituted 1,3,4-Thiadiazoles |
title_short | Synthesis and Diuretic Activity of Substituted 1,3,4-Thiadiazoles |
title_sort | synthesis and diuretic activity of substituted 1,3,4-thiadiazoles |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9012607/ https://www.ncbi.nlm.nih.gov/pubmed/35433072 http://dx.doi.org/10.1155/2022/3011531 |
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