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dc.contributor.author
De Azambuja, Gabriel Oliveira
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Svetaz, Laura Andrea
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Goncalves, Itamar Luis
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Corbelini, Patricia Frasson
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von Poser, Gilsane Lino
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Kawano, Daniel Fabio
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Zacchino, Susana Alicia Stella
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Eifler Lima, Vera Lucia
dc.date.available
2020-05-07T21:13:59Z
dc.date.issued
2019-12
dc.identifier.citation
De Azambuja, Gabriel Oliveira; Svetaz, Laura Andrea; Goncalves, Itamar Luis; Corbelini, Patricia Frasson; von Poser, Gilsane Lino; et al.; In vitro Antifungal Activity of Dihydropyrimidinones/Thiones Against Candida albicans and Cryptococcus neoformans; Bentham Science Publishers; Current Bioactive Compounds; 15; 6; 12-2019; 648-655
dc.identifier.issn
1573-4072
dc.identifier.uri
http://hdl.handle.net/11336/104572
dc.description.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.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Bentham Science Publishers
dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc/2.5/ar/
dc.subject
BIGINELLI REACTION
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CRYPTOCOCCUS NEOFORMANS
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CANDIDA ALBICANS
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ANTIFUNGAL ACTIVITY
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STRUCTURE ACTIVITY RELATIONSHIP
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MULTICOMPONENT REACTION
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Química Orgánica
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Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
dc.title
In vitro Antifungal Activity of Dihydropyrimidinones/Thiones Against Candida albicans and Cryptococcus neoformans
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2020-04-17T14:33:10Z
dc.identifier.eissn
1573-4072
dc.journal.volume
15
dc.journal.number
6
dc.journal.pagination
648-655
dc.journal.pais
Emiratos Árabes Unidos
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Sharjah
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Fil: De Azambuja, Gabriel Oliveira. Universidade Federal do Rio Grande do Sul; Brasil
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Fil: Svetaz, Laura Andrea. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina
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Fil: Goncalves, Itamar Luis. Universidade Federal do Rio Grande do Sul; Brasil
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Fil: Corbelini, Patricia Frasson. Universidade Federal do Rio Grande do Sul; Brasil
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Fil: von Poser, Gilsane Lino. Universidade Federal do Rio Grande do Sul; Brasil
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Fil: Kawano, Daniel Fabio. Universidade Estadual Do Campinas. Instituto de Química.; Brasil
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Fil: Zacchino, Susana Alicia Stella. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina
dc.description.fil
Fil: Eifler Lima, Vera Lucia. Universidade Federal do Rio Grande do Sul; Brasil
dc.journal.title
Current Bioactive Compounds
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.eurekaselect.com/165687/article
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.2174/1573407214666180926115745
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