Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors

Memórias do Instituto Oswaldo Cruz

Renata B De Oliveira²  Aline Bm Vaz²  Rosana O Alves¹  Daniel B Liarte¹  Claudio L Donnici¹  Alvaro J Romanha¹  Carlos L Zani² 

[1] ,Fiocruz Centro de Pesquisas René Rachou Laboratório de Química de Produtos NaturaisBelo Horizonte MG ,Brasil

关键词: tropical diseases;    Chagas disease;    arylfurans;    trypanothione reductase;   

DOI  :  10.1590/S0074-02762006000200009

来源: SciELO

【 摘 要 】

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. 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).

【 授权许可】

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