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Synthesis and biological evaluation of hydrazone derivatives as antifungal agents

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Synthesis and biological evaluation of hydrazone derivatives as antifungal agents

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Título Synthesis and biological evaluation of hydrazone derivatives as antifungal agents
Outro título Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents
Autor Casanova, Bruna Bento
Muniz, Mauro Neves
Oliveira, Thayse Viana de
Oliveira, Luis Flávio Souza de
Machado, Michel Mansur
Fuentefria, Alexandre Meneghello
Gosmann, Grace
Gnoatto, Simone Cristina Baggio
Abstract 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 ofleukocytes 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.
Contido em Molecules. Basel. Vol. 20, no.5 (2015), p. 9229-9241
Assunto Aldeidos
Atividade antifúngica
Hidrazonas
Levedura
[en] Aldehydes
[en] Antifungal activity
[en] Emerging yeasts
[en] Hydrazones
Origem Estrangeiro
Tipo Artigo de periódico
URI http://hdl.handle.net/10183/140211
Arquivos Descrição Formato
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