Author | Oliveira, Renata Barbosa de | |
Author | Vaz, Aline Bruna Martins | |
Author | Alves, Rosana de Oliveira | |
Author | Liarte, Daniel Barbosa | |
Author | Donnici, Claudio Luis | |
Author | Romanha, Álvaro José | |
Author | Zani, Carlos Leomar | |
Access date | 2013-06-06T18:32:43Z | |
Available date | 2013-06-06T18:32:43Z | |
Document date | 2006 | |
Citation | 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. | pt_BR |
ISSN | 0074-0276 | |
URI | https://www.arca.fiocruz.br/handle/icict/6575 | |
Sponsorship | Fiocruz, CNPq, Fapemig | pt_BR |
Language | eng | pt_BR |
Rights | open access | pt_BR |
Title | Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors | pt_BR |
Type | Article | pt_BR |
DOI | S0074-02762006000200009 | |
Abstract | 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). | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Química de Produtos Naturais. Belo Horizonte, MG, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Química de Produtos Naturais. Belo Horizonte, MG, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Parasitologia Celular e Molecular. Belo Horizonte, MG, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Parasitologia Celular e Molecular. Belo Horizonte, MG, Brasil. | pt_BR |
Affilliation | Universidade Federal de Minas Gerais. Instituto de Ciências Exatas. Departamento de Química. NEQUIM. Belo Horizonte, MG, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Parasitologia Celular e Molecular. Belo Horizonte, MG, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Química de Produtos Naturais. Belo Horizonte, MG, Brasil. | pt_BR |
Subject | Tropical diseases | pt_BR |
Subject | Chagas disease | pt_BR |
Subject | Arylfurans | pt_BR |
Subject | Trypanothione reductase | pt_BR |