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

Detalhes bibliográficos
Autor(a) principal: Azambuja, Gabriel Oliveira de
Data de Publicação: 2017
Tipo de documento: Trabalho de conclusão de curso
Idioma: eng
Título da fonte: Repositório Institucional da UFRGS
Texto Completo: http://hdl.handle.net/10183/217668
Resumo: 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.
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spelling Azambuja, Gabriel Oliveira deEifler-Lima, Vera Lucia2021-02-02T04:05:36Z2017http://hdl.handle.net/10183/217668001066025Since 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.application/pdfengAntifúngicosBiginelli reactionMulticomponent reactionStructure activity relationshipAntifungal activityCandida albicansCryptococcus neoformansIn vitro antifungal activity of dihydropyrimidinones/thiones against Candida albicans and Cryptococcus neoformansinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/bachelorThesisUniversidade Federal do Rio Grande do SulFaculdade de FarmáciaPorto Alegre, BR-RS2017Farmáciagraduaçãoinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UFRGSinstname:Universidade Federal do Rio Grande do Sul (UFRGS)instacron:UFRGSTEXT001066025.pdf.txt001066025.pdf.txtExtracted Texttext/plain80280http://www.lume.ufrgs.br/bitstream/10183/217668/2/001066025.pdf.txt29565ff6e6c7e9df8dec125517a792b5MD52ORIGINAL001066025.pdfTexto completoapplication/pdf1567464http://www.lume.ufrgs.br/bitstream/10183/217668/1/001066025.pdfc836d56c8fe5cb45e6c6885efa36ea67MD5110183/2176682021-03-09 04:47:28.688104oai:www.lume.ufrgs.br:10183/217668Repositório de PublicaçõesPUBhttps://lume.ufrgs.br/oai/requestopendoar:2021-03-09T07:47:28Repositório Institucional da UFRGS - Universidade Federal do Rio Grande do Sul (UFRGS)false
dc.title.pt_BR.fl_str_mv In vitro antifungal activity of dihydropyrimidinones/thiones against Candida albicans and Cryptococcus neoformans
title In vitro antifungal activity of dihydropyrimidinones/thiones against Candida albicans and Cryptococcus neoformans
spellingShingle In vitro antifungal activity of dihydropyrimidinones/thiones against Candida albicans and Cryptococcus neoformans
Azambuja, Gabriel Oliveira de
Antifúngicos
Biginelli reaction
Multicomponent reaction
Structure activity relationship
Antifungal activity
Candida albicans
Cryptococcus neoformans
title_short In vitro antifungal activity of dihydropyrimidinones/thiones against Candida albicans and Cryptococcus neoformans
title_full In vitro antifungal activity of dihydropyrimidinones/thiones against Candida albicans and Cryptococcus neoformans
title_fullStr In vitro antifungal activity of dihydropyrimidinones/thiones against Candida albicans and Cryptococcus neoformans
title_full_unstemmed In vitro antifungal activity of dihydropyrimidinones/thiones against Candida albicans and Cryptococcus neoformans
title_sort In vitro antifungal activity of dihydropyrimidinones/thiones against Candida albicans and Cryptococcus neoformans
author Azambuja, Gabriel Oliveira de
author_facet Azambuja, Gabriel Oliveira de
author_role author
dc.contributor.author.fl_str_mv Azambuja, Gabriel Oliveira de
dc.contributor.advisor1.fl_str_mv Eifler-Lima, Vera Lucia
contributor_str_mv Eifler-Lima, Vera Lucia
dc.subject.por.fl_str_mv Antifúngicos
topic Antifúngicos
Biginelli reaction
Multicomponent reaction
Structure activity relationship
Antifungal activity
Candida albicans
Cryptococcus neoformans
dc.subject.eng.fl_str_mv Biginelli reaction
Multicomponent reaction
Structure activity relationship
Antifungal activity
Candida albicans
Cryptococcus neoformans
description 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.
publishDate 2017
dc.date.issued.fl_str_mv 2017
dc.date.accessioned.fl_str_mv 2021-02-02T04:05:36Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/bachelorThesis
format bachelorThesis
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10183/217668
dc.identifier.nrb.pt_BR.fl_str_mv 001066025
url http://hdl.handle.net/10183/217668
identifier_str_mv 001066025
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
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instacron:UFRGS
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institution UFRGS
reponame_str Repositório Institucional da UFRGS
collection Repositório Institucional da UFRGS
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