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Memórias do Instituto Oswaldo Cruz
Fundação Oswaldo Cruz, Fiocruz
ISSN: 1678-8060
EISSN: 1678-8060
Vol. 101, No. 2, 2006, pp. 169-173
Bioline Code: oc06032
Full paper language: English
Document type: Research Article
Document available free of charge

Memórias do Instituto Oswaldo Cruz, Vol. 101, No. 2, 2006, pp. 169-173

 en Arylfurans as potential Trypanosoma cruzi check for this species in other resources trypanothione reductase inhibitors
Renata B de Oliveira; Aline BM Vaz; Rosana O Alves; Daniel B Liarte; Claudio L Donnici; Alvaro J Romanha & Carlos L Zani

Abstract

The natural lignans veraguensin and grandisin have been reported to be active against Trypanosoma cruzi check for this species in other resources 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. cruzi trypanothione reductase (TR) inhibitors 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 7 and 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).

Keywords
tropical diseases - Chagas disease - arylfurans - trypanothione reductase

 
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