Arylfurans as potential Trypanosoma cruzi trypanothione reductase inhibitors
Mem. Inst. Oswaldo Cruz
;
101(2): 169-173, Mar. 2006. ilus
Artículo
en Inglés
| LILACS
| ID: lil-430894
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:
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Índice:
LILACS (Américas)
Asunto principal:
Tripanocidas
/
Trypanosoma cruzi
/
Inhibidores Enzimáticos
/
Furanos
/
NADH NADPH Oxidorreductasas
Límite:
Animales
Idioma:
Inglés
Revista:
Mem. Inst. Oswaldo Cruz
Asunto de la revista:
Medicina Tropical
/
Parasitología
Año:
2006
Tipo del documento:
Artículo
País de afiliación:
Brasil
Institución/País de afiliación:
Fundação Oswaldo Cruz/BR
/
Universidade Federal de Minas Gerais/BR
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