In:
Current Bioactive Compounds, Bentham Science Publishers Ltd., Vol. 15, No. 6 ( 2020-01-23), p. 648-655
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. 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.
Type of Medium:
Online Resource
ISSN:
1573-4072
DOI:
10.2174/1573407214666180926115745
Language:
English
Publisher:
Bentham Science Publishers Ltd.
Publication Date:
2020
SSG:
15,3
Permalink