Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors

Detalhes bibliográficos
Autor(a) principal: Oliveira, Renata Barbosa de
Data de Publicação: 2006
Outros Autores: Vaz, Aline Bruna Martins, Alves, Rosana de Oliveira, Liarte, Daniel Barbosa, Donnici, Claudio Luis, Romanha, Álvaro José, Zani, Carlos Leomar
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/6575
Resumo: Fiocruz, CNPq, Fapemig
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spelling Oliveira, Renata Barbosa deVaz, Aline Bruna MartinsAlves, Rosana de OliveiraLiarte, Daniel BarbosaDonnici, Claudio LuisRomanha, Álvaro JoséZani, Carlos Leomar2013-06-06T18:32:43Z2013-06-06T18:32:43Z2006OLIVEIRA, Renata Barbosa de et al. Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors. Memórias do Instituto Oswaldo Cruz, Rio de Janeiro, v. 101, n. 2, p. 169-173, Mar. 2006.0074-0276https://www.arca.fiocruz.br/handle/icict/6575S0074-02762006000200009Fiocruz, CNPq, FapemigFundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Química de Produtos Naturais. Belo Horizonte, MG, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Química de Produtos Naturais. Belo Horizonte, MG, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Parasitologia Celular e Molecular. Belo Horizonte, MG, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Parasitologia Celular e Molecular. Belo Horizonte, MG, Brasil.Universidade Federal de Minas Gerais. Instituto de Ciências Exatas. Departamento de Química. NEQUIM. Belo Horizonte, MG, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Parasitologia Celular e Molecular. Belo Horizonte, MG, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Química de Produtos Naturais. Belo Horizonte, MG, Brasil.The natural lignans veraguensin and grandisin have been reported to be active against Trypanosoma cruzi bloodstream forms. Aiming at the total synthesis of these and related compounds, we prepared three 2-arylfurans and eight 2,5-diarylfurans. They were evaluated for their potential as T. cruzitrypanothione reductase (TR) inhibi-tors as well against the parasite’s intracellular (amastigote) and bloodstream (trypomastigote) forms. Compound 12 was the most effective against TR with an IC50 of 48.5 µM while 7and 14 were active against amastigotes, inhibiting the parasite development by 60% at 20 µg/ml (59 and 90 µM, respectively). On the other hand, none of the compounds was significantly active against the parasite bloodstream forms even at 250 µg/ml (0.6-1.5 mM).engArylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitorsinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleTropical diseasesChagas diseaseArylfuransTrypanothione reductaseinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZORIGINAL87.pdf87.pdfapplication/pdf480919https://www.arca.fiocruz.br/bitstream/icict/6575/1/87.pdf0ec2d7dcbb146ddb70e377368034b213MD51LICENSElicense.txtlicense.txttext/plain; charset=utf-81914https://www.arca.fiocruz.br/bitstream/icict/6575/2/license.txt7d48279ffeed55da8dfe2f8e81f3b81fMD52TEXT87.pdf.txt87.pdf.txtExtracted texttext/plain23885https://www.arca.fiocruz.br/bitstream/icict/6575/5/87.pdf.txt9202155dafdcfef78fa11a82aef1480cMD55THUMBNAIL87.pdf.jpg87.pdf.jpgGenerated Thumbnailimage/jpeg2154https://www.arca.fiocruz.br/bitstream/icict/6575/4/87.pdf.jpg69150144097db540b861e4b50f2c9afdMD54icict/65752018-05-11 15:54:43.158oai:www.arca.fiocruz.br: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ório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352018-05-11T18:54:43Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.pt_BR.fl_str_mv Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
title Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
spellingShingle Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
Oliveira, Renata Barbosa de
Tropical diseases
Chagas disease
Arylfurans
Trypanothione reductase
title_short Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
title_full Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
title_fullStr Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
title_full_unstemmed Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
title_sort Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
author Oliveira, Renata Barbosa de
author_facet Oliveira, Renata Barbosa de
Vaz, Aline Bruna Martins
Alves, Rosana de Oliveira
Liarte, Daniel Barbosa
Donnici, Claudio Luis
Romanha, Álvaro José
Zani, Carlos Leomar
author_role author
author2 Vaz, Aline Bruna Martins
Alves, Rosana de Oliveira
Liarte, Daniel Barbosa
Donnici, Claudio Luis
Romanha, Álvaro José
Zani, Carlos Leomar
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Oliveira, Renata Barbosa de
Vaz, Aline Bruna Martins
Alves, Rosana de Oliveira
Liarte, Daniel Barbosa
Donnici, Claudio Luis
Romanha, Álvaro José
Zani, Carlos Leomar
dc.subject.en.pt_BR.fl_str_mv Tropical diseases
Chagas disease
Arylfurans
Trypanothione reductase
topic Tropical diseases
Chagas disease
Arylfurans
Trypanothione reductase
description Fiocruz, CNPq, Fapemig
publishDate 2006
dc.date.issued.fl_str_mv 2006
dc.date.accessioned.fl_str_mv 2013-06-06T18:32:43Z
dc.date.available.fl_str_mv 2013-06-06T18:32:43Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.citation.fl_str_mv OLIVEIRA, Renata Barbosa de et al. Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors. Memórias do Instituto Oswaldo Cruz, Rio de Janeiro, v. 101, n. 2, p. 169-173, Mar. 2006.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/6575
dc.identifier.issn.none.fl_str_mv 0074-0276
dc.identifier.doi.none.fl_str_mv S0074-02762006000200009
identifier_str_mv OLIVEIRA, Renata Barbosa de et al. Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors. Memórias do Instituto Oswaldo Cruz, Rio de Janeiro, v. 101, n. 2, p. 169-173, Mar. 2006.
0074-0276
S0074-02762006000200009
url https://www.arca.fiocruz.br/handle/icict/6575
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