info:eu-repo/semantics/article
In vitro Antifungal Activity of Dihydropyrimidinones/Thiones Against Candida albicans and Cryptococcus neoformans
Fecha
2019-12Registro en:
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
1573-4072
1573-4072
CONICET Digital
CONICET
Autor
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
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.