In vitro and in vivo anti-Trypanosoma cruzi activity of a novel nitro-derivative.

Abstract:

: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.

journal_name

Mem Inst Oswaldo Cruz

authors

Muelas-Serrano S,Le-Senne A,Fernandez-Portillo C,Nogal JJ,Ochoa C,Gomez-Barrio A

doi

10.1590/s0074-02762002000400019

subject

Has Abstract

pub_date

2002-06-01 00:00:00

pages

553-7

issue

4

eissn

0074-0276

issn

1678-8060

pii

S0074-02762002000400019

journal_volume

97

pub_type

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