Síntese, avaliação biológica e modelagem molecular de arilfuranos como inibidores da enzima tripanotiona redutase


Autoria(s): Oliveira,Renata B. de; Zani,Carlos L.; Ferreira,Rafaela S.; Leite,Rodrigo S.; Alves,Tânia M. A.; Silva,Thaís H. A. da; Romanha,Alvaro J.
Data(s)

01/01/2008

Resumo

Trypanosoma cruzi is a protozoan parasite that causes a severe disease (Chagas'disease) in Central and South America. The currently available chemotherapeutic agents against this disease are still inadequate. The enzyme trypanothione reductase (TR) is considered a validated molecular target for the development of new drugs against this parasite. In this regard, a series of arylfurans based on 2,5-bis-(4-acetamidophenyl)furan was synthesized and tested for their in vitro inhibitory activity against TR. Molecular modeling studies of putative enzyme-inhibitor complexes revealed a possible mechanism of interaction. From synthesized compounds, a benzylaminofuran derivative was found to be more active than the lead compound.

Formato

text/html

Identificador

http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422008000200013

Idioma(s)

pt

Publicador

Sociedade Brasileira de Química

Fonte

Química Nova v.31 n.2 2008

Palavras-Chave #trypanothione reductase #molecular modeling #arylfurans
Tipo

journal article