Artículo
In vitro Antifungal Activity of Dihydropyrimidinones/Thiones Against Candida albicans and Cryptococcus neoformans
De Azambuja, Gabriel Oliveira; Svetaz, Laura Andrea
; Goncalves, Itamar Luis; Corbelini, Patricia Frasson; von Poser, Gilsane Lino; Kawano, Daniel Fabio; Zacchino, Susana Alicia Stella; Eifler Lima, Vera Lucia
Fecha de publicación:
12/2019
Editorial:
Bentham Science Publishers
Revista:
Current Bioactive Compounds
ISSN:
1573-4072
e-ISSN:
1573-4072
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
Background: Since the Monastrol discovery in 1999 as the first inhibitor of Eg5, functionalized dihydropyrimidinones/thiones (DHPMs) have emerged as prototypes for drug design in different targets. The present work aimed to evaluate the antifungal activity of a chemical library of DHPMs.
Methods: The compounds were obtained employing Biginelli reaction. Their antifungal activities were assessed against C. neoformans and C. albicans.
Results: The compounds 1-i and 1-k inhibited moderately the fungal growth of C. neoformans, with compound 2-k presenting MIC80 values of 62.5-125 µg·mL-1. Considering activity against C. albicans, the compounds 1-i and 1-n present an MIC50 value of 125-250 µg·mL-1.
Conclusion: The changes performed in DHPM scaffold appear to be valuable for generating compounds with potential antifungal effect.
Archivos asociados
Licencia
Identificadores
Colecciones
Articulos(CCT - ROSARIO)
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - ROSARIO
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - ROSARIO
Citación
De Azambuja, Gabriel Oliveira; Svetaz, Laura Andrea; Goncalves, Itamar Luis; Corbelini, Patricia Frasson; von Poser, Gilsane Lino; et al.; In vitro Antifungal Activity of Dihydropyrimidinones/Thiones Against Candida albicans and Cryptococcus neoformans; Bentham Science Publishers; Current Bioactive Compounds; 15; 6; 12-2019; 648-655
Compartir
Altmétricas