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Synthesis and Pharmacological Activities of Some New 3-Substituted-4-Amino-5-Mercapto-1,2,4-Triazoles
In this study, various 3-β-[(N-benzenesulphonyl/tosyl)-4-(un) substituted anilino]ethyl-4-amino-5-mercapto-4(H)-1,2,4-triazoles (5a–f), with biologically active ‘sulphonamide’ moiety as the side chain have been prepared. The structures of the newly synthesised compounds have been established on the...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Medknow Publications & Media Pvt Ltd
2011
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3224403/ https://www.ncbi.nlm.nih.gov/pubmed/22131636 http://dx.doi.org/10.4103/0250-474X.89771 |
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author | Desai, Shobha R. Laddi, U. Bennur, Rajani S. Patil, P. A. Bennur, S. |
author_facet | Desai, Shobha R. Laddi, U. Bennur, Rajani S. Patil, P. A. Bennur, S. |
author_sort | Desai, Shobha R. |
collection | PubMed |
description | In this study, various 3-β-[(N-benzenesulphonyl/tosyl)-4-(un) substituted anilino]ethyl-4-amino-5-mercapto-4(H)-1,2,4-triazoles (5a–f), with biologically active ‘sulphonamide’ moiety as the side chain have been prepared. The structures of the newly synthesised compounds have been established on the basis of their spectral data and elemental analysis. All the compounds were evaluated for antimicrobial activities against Escherichia coli, Bacillus cirroflagellosus, Aspergillus niger and Colletotrichum capsici. Most of the compounds investigated exhibited significant antifungal activity against Colletotrichum capsici, even greater than fluconazole, the standard used. Only two compounds 3f (59%) and 5e (67%), have shown moderate antituberculosis activity. All the triazoles exhibited moderate degree of antiinflammatory activity and least ulcerogenecity. Most of the compounds have shown significant analgesic activity (81.02–120.72%) in comparison with aspirin (49.39%). In the MES method, only compound 3e exhibited a protection of 66.66%, whereas others exhibited minimum protection of (33.33%). |
format | Online Article Text |
id | pubmed-3224403 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2011 |
publisher | Medknow Publications & Media Pvt Ltd |
record_format | MEDLINE/PubMed |
spelling | pubmed-32244032011-11-30 Synthesis and Pharmacological Activities of Some New 3-Substituted-4-Amino-5-Mercapto-1,2,4-Triazoles Desai, Shobha R. Laddi, U. Bennur, Rajani S. Patil, P. A. Bennur, S. Indian J Pharm Sci Short Communications In this study, various 3-β-[(N-benzenesulphonyl/tosyl)-4-(un) substituted anilino]ethyl-4-amino-5-mercapto-4(H)-1,2,4-triazoles (5a–f), with biologically active ‘sulphonamide’ moiety as the side chain have been prepared. The structures of the newly synthesised compounds have been established on the basis of their spectral data and elemental analysis. All the compounds were evaluated for antimicrobial activities against Escherichia coli, Bacillus cirroflagellosus, Aspergillus niger and Colletotrichum capsici. Most of the compounds investigated exhibited significant antifungal activity against Colletotrichum capsici, even greater than fluconazole, the standard used. Only two compounds 3f (59%) and 5e (67%), have shown moderate antituberculosis activity. All the triazoles exhibited moderate degree of antiinflammatory activity and least ulcerogenecity. Most of the compounds have shown significant analgesic activity (81.02–120.72%) in comparison with aspirin (49.39%). In the MES method, only compound 3e exhibited a protection of 66.66%, whereas others exhibited minimum protection of (33.33%). Medknow Publications & Media Pvt Ltd 2011 /pmc/articles/PMC3224403/ /pubmed/22131636 http://dx.doi.org/10.4103/0250-474X.89771 Text en Copyright: © Indian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Short Communications Desai, Shobha R. Laddi, U. Bennur, Rajani S. Patil, P. A. Bennur, S. Synthesis and Pharmacological Activities of Some New 3-Substituted-4-Amino-5-Mercapto-1,2,4-Triazoles |
title | Synthesis and Pharmacological Activities of Some New 3-Substituted-4-Amino-5-Mercapto-1,2,4-Triazoles |
title_full | Synthesis and Pharmacological Activities of Some New 3-Substituted-4-Amino-5-Mercapto-1,2,4-Triazoles |
title_fullStr | Synthesis and Pharmacological Activities of Some New 3-Substituted-4-Amino-5-Mercapto-1,2,4-Triazoles |
title_full_unstemmed | Synthesis and Pharmacological Activities of Some New 3-Substituted-4-Amino-5-Mercapto-1,2,4-Triazoles |
title_short | Synthesis and Pharmacological Activities of Some New 3-Substituted-4-Amino-5-Mercapto-1,2,4-Triazoles |
title_sort | synthesis and pharmacological activities of some new 3-substituted-4-amino-5-mercapto-1,2,4-triazoles |
topic | Short Communications |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3224403/ https://www.ncbi.nlm.nih.gov/pubmed/22131636 http://dx.doi.org/10.4103/0250-474X.89771 |
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