Article
Síntese, avaliação biológica e modelagem molecular de arilfuranos como inibidores da enzima tripanotiona redutase
Synthesis, biological evaluation and molecular modeling of arylfurans as potential trypanothione reductase inhibitors
Registro en:
OLIVEIRA, Renata B. de et al. Síntese, avaliação biológica e modelagem molecular de arilfuranos como inibidores da enzima tripanotiona redutase. Quím. Nova. 2008, vol.31, n.2, pp. 261-267
0100-4042
10.1590/S0100-40422008000200013
Autor
Oliveira, Renata Barbosa de
Zani, Carlos Leomar
Ferreira, Rafaela Salgado
Leite, Rodrigo S.
Alves, Tânia Maria de Almeida
Silva, Thaís H. A. da
Romanha, Álvaro José
Resumen
CNPq, FAPEMIG e Fiocruz 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.