In vitro Antifungal Activity of Dihydropyrimidinones/Thiones Against Candida albicans and Cryptococcus neoformans-Reference-Cited by-同舟云学术

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

Published:2020-01-23 Issue:6 Volume:15 Page:648-655
ISSN:1573-4072
Container-title:Current Bioactive Compounds
language:en
Short-container-title:CBC

Author:

de Azambuja Gabriel O.¹,Svetaz Laura²,Gonçalves Itamar L.¹,Corbelini Patricia F.¹,von Poser Gilsane L.¹,Kawano Daniel F.³,Zacchino Susana²,Eifler-Lima Vera L.¹

Affiliation:

1. Laboratorio de Sintese Organica Medicinal/LaSOM, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil

2. Farmacognosia, National University of Rosario, Rosario, Argentina

3. Instituto de Quimica, Universidade Federal de Campinas, Campinas, Brazil

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.

Publisher

Bentham Science Publishers Ltd.

Subject

General Pharmacology, Toxicology and Pharmaceutics

Reference24 articles.

1. Welsch M.E.; Snyder S.A.; Stockwell B.R.; Privileged scaffolds for library design and drug discovery. Curr Opin Chem Biol 2010,14(3),347-361

2. de Fátima Â.; Braga T.C.; Neto, Lda.S.; Terra, B.S.; Oliveira, B.G.F.; da Silva, D.L.; Modolo, L.V. A mini-review on Biginelli adducts with notable pharmacological properties. J Adv Res 2015,6(3),363-373

3. Chitra S.; Devanathan D.; Pandiarajan K.; Synthesis and in vitro microbiological evaluation of novel 4-aryl-5-isopropoxycarbonyl-6-methyl-3,4-dihydropyrimidinones. Eur J Med Chem 2010,45(1),367-371

4. Beena K.; Akelesh T.; Synthesis and screening of some dihydropyrimidine derivatives as antimicrobial agents. Int Res J Pharm 2012,3(9),303-304

5. Sedaghati B.; Fassihi A.; Arbabi S.; Ranjbar M.; Memarian H.R.; Saghaie L.; Omidi A.; Sardari A.; Jalali M.; Abedi D.; Synthesis and antimicrobial activity of novel derivatives of Biginelli pyrimidines. Med Chem Res 2012,21(12),3973-3983

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