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Molecules 2015, 20(5), 9229-9241; doi:10.3390/molecules20059229

Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents

1
Laboratório de Fitoquímica e Síntese Orgânica (LAFIS), Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 90610-000, RS, Brazil
2
Laboratório de Micologia Aplicada, Departamento de Analises, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 90610-000, RS, Brazil
3
Departamento de Farmácia, Universidade Federal do Pampa, Km 592, Uruguaiana 97500-970, RS, Brazil
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 28 February 2015 / Revised: 11 May 2015 / Accepted: 12 May 2015 / Published: 20 May 2015
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1030 KB, uploaded 20 May 2015]   |  

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 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. View Full-Text
Keywords: aldehydes; hydrazones; emerging yeasts; antifungal activity aldehydes; hydrazones; emerging yeasts; antifungal activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Casanova, B.B.; Muniz, M.N.; de Oliveira, T.; de Oliveira, L.F.; Machado, M.M.; Fuentefria, A.M.; Gosmann, G.; Gnoatto, S.C.B. Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents. Molecules 2015, 20, 9229-9241.

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