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Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents
Emerging yeasts are among the most prevalent causes of systemic infections with high mortality rates and there is an urgent need to develop specific, effective and non-toxic antifungal agents to respond to this issue. In this study 35 aldehydes, hydrazones and hydrazines were obtained and their anti...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2015
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272182/ https://www.ncbi.nlm.nih.gov/pubmed/26007181 http://dx.doi.org/10.3390/molecules20059229 |
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author | Casanova, Bruna B. Muniz, Mauro N. de Oliveira, Thayse de Oliveira, Luís Flavio Machado, Michel M. Fuentefria, Alexandre M. Gosmann, Grace Gnoatto, Simone C. B. |
author_facet | Casanova, Bruna B. Muniz, Mauro N. de Oliveira, Thayse de Oliveira, Luís Flavio Machado, Michel M. Fuentefria, Alexandre M. Gosmann, Grace Gnoatto, Simone C. B. |
author_sort | Casanova, Bruna B. |
collection | PubMed |
description | Emerging yeasts are among the most prevalent causes of systemic infections with high mortality rates and there is an urgent need to develop specific, effective and non-toxic antifungal agents to respond to this issue. In this study 35 aldehydes, hydrazones and hydrazines were obtained and their antifungal activity was evaluated against Candida species (C. parapsilosis, C. tropicalis, C. krusei, C. albicans, C. glabrata and C. lusitaneae) and Trichosporon asahii, in an in vitro screening. The minimum inhibitory concentrations (MICs) of the active compounds in the screening was determined against 10 clinical isolates of C. parapsilosis and 10 of T. asahii. The compounds 4-pyridin-2-ylbenzaldehyde] (13a) and tert-butyl-(2Z)-2-(3,4,5-trihydroxybenzylidine)hydrazine carboxylate (7b) showed the most promising MIC values in the range of 16–32 μg/mL and 8–16 μg/mL, respectively. The compounds’ action on the stability of the cell membrane and cell wall was evaluated, which suggested the action of the compounds on the fungal cell membrane. Cell viability of leukocytes and an alkaline comet assay were performed to evaluate the cytotoxicity. Compound 13a was not cytotoxic at the active concentrations. These results support the discovery of promising candidates for the development of new antifungal agents. |
format | Online Article Text |
id | pubmed-6272182 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2015 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62721822019-01-07 Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents Casanova, Bruna B. Muniz, Mauro N. de Oliveira, Thayse de Oliveira, Luís Flavio Machado, Michel M. Fuentefria, Alexandre M. Gosmann, Grace Gnoatto, Simone C. B. Molecules Article Emerging yeasts are among the most prevalent causes of systemic infections with high mortality rates and there is an urgent need to develop specific, effective and non-toxic antifungal agents to respond to this issue. In this study 35 aldehydes, hydrazones and hydrazines were obtained and their antifungal activity was evaluated against Candida species (C. parapsilosis, C. tropicalis, C. krusei, C. albicans, C. glabrata and C. lusitaneae) and Trichosporon asahii, in an in vitro screening. The minimum inhibitory concentrations (MICs) of the active compounds in the screening was determined against 10 clinical isolates of C. parapsilosis and 10 of T. asahii. The compounds 4-pyridin-2-ylbenzaldehyde] (13a) and tert-butyl-(2Z)-2-(3,4,5-trihydroxybenzylidine)hydrazine carboxylate (7b) showed the most promising MIC values in the range of 16–32 μg/mL and 8–16 μg/mL, respectively. The compounds’ action on the stability of the cell membrane and cell wall was evaluated, which suggested the action of the compounds on the fungal cell membrane. Cell viability of leukocytes and an alkaline comet assay were performed to evaluate the cytotoxicity. Compound 13a was not cytotoxic at the active concentrations. These results support the discovery of promising candidates for the development of new antifungal agents. MDPI 2015-05-20 /pmc/articles/PMC6272182/ /pubmed/26007181 http://dx.doi.org/10.3390/molecules20059229 Text en © 2015 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Casanova, Bruna B. Muniz, Mauro N. de Oliveira, Thayse de Oliveira, Luís Flavio Machado, Michel M. Fuentefria, Alexandre M. Gosmann, Grace Gnoatto, Simone C. B. Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents |
title | Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents |
title_full | Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents |
title_fullStr | Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents |
title_full_unstemmed | Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents |
title_short | Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents |
title_sort | synthesis and biological evaluation of hydrazone derivatives as antifungal agents |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272182/ https://www.ncbi.nlm.nih.gov/pubmed/26007181 http://dx.doi.org/10.3390/molecules20059229 |
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