Arylfurans as potential trypanosoma cruzi trypanothione reductase inhibitors.

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. 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 microM while 7 and 14 were active against amastigotes, inhibiting the parasite development by 60% at 20 microg/ml (59 and 90 microM, respectively). On the other hand, none of the compounds was significantly active against the parasite bloodstream forms even at 250 microg/ml (0.6-1.5 mM).

journal_name

Mem Inst Oswaldo Cruz

authors

de Oliveira RB,Vaz AB,Alves RO,Liarte DB,Donnici CL,Romanha AJ,Zani CL

doi

10.1590/s0074-02762006000200009

subject

Has Abstract

pub_date

2006-03-01 00:00:00

pages

169-73

issue

2

eissn

0074-0276

issn

1678-8060

journal_volume

101

pub_type

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