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Current Bioactive Compounds

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ISSN (Print): 1573-4072
ISSN (Online): 1875-6646

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Research Article

In vitro Antifungal Activity of Dihydropyrimidinones/Thiones Against Candida albicans and Cryptococcus neoformans

Author(s): Gabriel O. de Azambuja*, Laura Svetaz, Itamar L. Gonçalves, Patricia F. Corbelini, Gilsane L. von Poser, Daniel F. Kawano, Susana Zacchino and Vera L. Eifler-Lima

Volume 15, Issue 6, 2019

Page: [648 - 655] Pages: 8

DOI: 10.2174/1573407214666180926115745

Price: $65

Abstract

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.

Keywords: Biginelli reaction, Cryptococcus neoformans, Candida albicans, Antifungal activity, Structure activity relationship, Multicomponent reaction.

Graphical Abstract

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