In vitro antifungal activity of dihydropyrimidinones/thiones against Candida albicans and Cryptococcus neoformans

Abstract

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 which were obtained employing the Biginelli reaction. Their antifungal activities were assessed against C. neoformans and C. albicans. 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 a MIC50 value of 125-250 μg∙mL-1. The changes performed in DHPM scaffold appear to be valuable for generating compounds with potential antifungal effect.