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 (5NO
2
TM), 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.