Article
Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
Registro en:
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
Autor
Oliveira, Renata Barbosa de
Vaz, Aline Bruna Martins
Alves, Rosana de Oliveira
Liarte, Daniel Barbosa
Donnici, Claudio Luis
Romanha, Álvaro José
Zani, Carlos Leomar
Resumen
Fiocruz, CNPq, Fapemig 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).