In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of a Novel Nitro-derivative
AUTOR(ES)
Muelas-Serrano, Susana, Le-Senne, Ana, Fernández-Portillo, Carlos, Nogal, Juan José, Ochoa, Carmen, Gómez-Barrio, Alicia
FONTE
Memórias do Instituto Oswaldo Cruz
DATA DE PUBLICAÇÃO
2002-06
RESUMO
Nitroarylidenemalononitriles and their cyanoacetamide derivatives with remarkable anti-epimastigote properties, were synthesized attempting to obtain new 3,5-diamino-4-(5'-nitroarylidene)-4H-thiadiazine 1,1-dioxide derivatives, which in previous reports had shown anti-Trypanosoma cruzi activity. Tests to evaluate the cytotoxicity of compounds were performed on J774 macrophages. 5-nitro-2-thienyl-malononitrile (5NO2TM), was the only product which maintained a high anti-epimastigote activity at concentrations in which it was no longer cytotoxic, thus it was assayed against intracellular amastigotes. Its anti-amastigote activity was similar to that of nifurtimox. Afterwards in vivo toxicity and anti-chagasic activity were determined. A reduction in parasitemia was observed.
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