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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...

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Autores principales: Desai, Shobha R., Laddi, U., Bennur, Rajani S., Patil, P. A., Bennur, S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2011
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%).
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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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