Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
Mem. Inst. Oswaldo Cruz
; 101(2): 169-173, Mar. 2006. ilus
Article
em En
| LILACS
| ID: lil-430894
Biblioteca responsável:
BR1.1
RESUMO
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 æM while 7 and 14 were active against amastigotes, inhibiting the parasite development by 60 percent at 20 æg/ml (59 and 90 æM, respectively). On the other hand, none of the compounds was significantly active against the parasite bloodstream forms even at 250 æg/ml (0.6-1.5 mM).
Texto completo:
1
Coleções:
01-internacional
Base de dados:
LILACS
Assunto principal:
Tripanossomicidas
/
Trypanosoma cruzi
/
Inibidores Enzimáticos
/
Furanos
/
NADH NADPH Oxirredutases
Limite:
Animals
Idioma:
En
Revista:
Mem. Inst. Oswaldo Cruz
Assunto da revista:
MEDICINA TROPICAL
/
PARASITOLOGIA
Ano de publicação:
2006
Tipo de documento:
Article
País de afiliação:
Brasil