2 research outputs found
In vitro Antifungal Activity of Dihydropyrimidinones/Thiones Against Candida albicans and Cryptococcus neoformans
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 ”g·mL-1. Considering activity against C. albicans, the compounds 1-i and 1-n present an MIC50 value of 125-250 ”g·mL-1.
Conclusion: The changes performed in DHPM scaffold appear to be valuable for generating compounds with potential antifungal effect.Fil: De Azambuja, Gabriel Oliveira. Universidade Federal do Rio Grande do Sul; BrasilFil: Svetaz, Laura Andrea. Universidad Nacional de Rosario. Facultad de Ciencias BioquĂmicas y FarmacĂ©uticas. Departamento de QuĂmica OrgĂĄnica. Ărea Farmacognosia; Argentina. Consejo Nacional de Investigaciones CientĂficas y TĂ©cnicas. Centro CientĂfico TecnolĂłgico Conicet - Rosario; ArgentinaFil: Goncalves, Itamar Luis. Universidade Federal do Rio Grande do Sul; BrasilFil: Corbelini, Patricia Frasson. Universidade Federal do Rio Grande do Sul; BrasilFil: von Poser, Gilsane Lino. Universidade Federal do Rio Grande do Sul; BrasilFil: Kawano, Daniel Fabio. Universidade Estadual Do Campinas. Instituto de QuĂmica.; BrasilFil: Zacchino, Susana Alicia Stella. Universidad Nacional de Rosario. Facultad de Ciencias BioquĂmicas y FarmacĂ©uticas. Departamento de QuĂmica OrgĂĄnica. Ărea Farmacognosia; ArgentinaFil: Eifler Lima, Vera Lucia. Universidade Federal do Rio Grande do Sul; Brasi