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Synthesis, antifungal and antibacterial activity of novel 1,2,4-triazole derivatives

A large number of 1,2,4-triazole-containing ring system have been incorporated into a wide variety of therapeutically interesting drug candidates including anti-inflammatory, central nervous system stimulants, antianxiety, and antimicrobial agents. To overcome the rapid development of drug resistanc...

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Autores principales: Gupta, Deepa, Jain, D. K.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4542402/
https://www.ncbi.nlm.nih.gov/pubmed/26317080
http://dx.doi.org/10.4103/2231-4040.161515
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author Gupta, Deepa
Jain, D. K.
author_facet Gupta, Deepa
Jain, D. K.
author_sort Gupta, Deepa
collection PubMed
description A large number of 1,2,4-triazole-containing ring system have been incorporated into a wide variety of therapeutically interesting drug candidates including anti-inflammatory, central nervous system stimulants, antianxiety, and antimicrobial agents. To overcome the rapid development of drug resistance, new agents should preferably have chemical characteristics that clearly differ from those of existing agents. Thus led to the design and synthesize the new antimicrobial agents. A novel series of Schiff bases based on of 4-(benzylideneamino)-5-phenyl-4H-1,2,4-triazole-3-thiol scaffold was prepared by heating thiocarbohydrazide and substituted benzoic acid and subsequently, treating with substituted benzaldehydes. Seventeen derivatives were synthesized and were biologically screened for antifungal and antibacterial activity. The newly synthesized derivatives of triazole showed antifungal activity against fungal species, Microsporum gypseum; and antibacterial activity against bacterial species, Staphylococcus aureus. It was observed that none of the compounds tested showed positive results for fungi Candida albicans fungi Aspergillus niger, nor against bacterial strain Escherichia coli. Strong antifungal effects were obtained for the synthesized compounds against M. gypseum and were superior or comparable to standard drug ketoconazole. Similarly, all of the synthesized compounds exhibit strong antibacterial activity against S. aureus and were superior or comparable to standard drug streptomycin. It was found that among the triazole derivatives so synthesized, six of them, showed antifungal activity superior to ketoconazole while one of them, showed antibacterial activity superior to streptomycin. Thus, these can be the potential new molecule as an antimicrobial agent.
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spelling pubmed-45424022015-08-27 Synthesis, antifungal and antibacterial activity of novel 1,2,4-triazole derivatives Gupta, Deepa Jain, D. K. J Adv Pharm Technol Res Original Article A large number of 1,2,4-triazole-containing ring system have been incorporated into a wide variety of therapeutically interesting drug candidates including anti-inflammatory, central nervous system stimulants, antianxiety, and antimicrobial agents. To overcome the rapid development of drug resistance, new agents should preferably have chemical characteristics that clearly differ from those of existing agents. Thus led to the design and synthesize the new antimicrobial agents. A novel series of Schiff bases based on of 4-(benzylideneamino)-5-phenyl-4H-1,2,4-triazole-3-thiol scaffold was prepared by heating thiocarbohydrazide and substituted benzoic acid and subsequently, treating with substituted benzaldehydes. Seventeen derivatives were synthesized and were biologically screened for antifungal and antibacterial activity. The newly synthesized derivatives of triazole showed antifungal activity against fungal species, Microsporum gypseum; and antibacterial activity against bacterial species, Staphylococcus aureus. It was observed that none of the compounds tested showed positive results for fungi Candida albicans fungi Aspergillus niger, nor against bacterial strain Escherichia coli. Strong antifungal effects were obtained for the synthesized compounds against M. gypseum and were superior or comparable to standard drug ketoconazole. Similarly, all of the synthesized compounds exhibit strong antibacterial activity against S. aureus and were superior or comparable to standard drug streptomycin. It was found that among the triazole derivatives so synthesized, six of them, showed antifungal activity superior to ketoconazole while one of them, showed antibacterial activity superior to streptomycin. Thus, these can be the potential new molecule as an antimicrobial agent. Medknow Publications & Media Pvt Ltd 2015 /pmc/articles/PMC4542402/ /pubmed/26317080 http://dx.doi.org/10.4103/2231-4040.161515 Text en Copyright: © 2015 Journal of Advanced Pharmaceutical Technology & Research 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-ShareAlike 3.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms.
spellingShingle Original Article
Gupta, Deepa
Jain, D. K.
Synthesis, antifungal and antibacterial activity of novel 1,2,4-triazole derivatives
title Synthesis, antifungal and antibacterial activity of novel 1,2,4-triazole derivatives
title_full Synthesis, antifungal and antibacterial activity of novel 1,2,4-triazole derivatives
title_fullStr Synthesis, antifungal and antibacterial activity of novel 1,2,4-triazole derivatives
title_full_unstemmed Synthesis, antifungal and antibacterial activity of novel 1,2,4-triazole derivatives
title_short Synthesis, antifungal and antibacterial activity of novel 1,2,4-triazole derivatives
title_sort synthesis, antifungal and antibacterial activity of novel 1,2,4-triazole derivatives
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4542402/
https://www.ncbi.nlm.nih.gov/pubmed/26317080
http://dx.doi.org/10.4103/2231-4040.161515
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