In this study, we report the synthesis and evaluation of
in vitro
and
in vivo
antitrypanosomal activity of styrylquinoline-like compounds (SQ)
3a-h
. Synthesis was carried out by using quinaldine and 8- hydroxyquinaldine with a variety of aromatic aldehydes. The structure of SQs was corroborated by one and two-dimension NMR spectroscopy.
In vitro
antitrypanosomal activity on
T. cruzi
Talahuen strain was evaluated using β-galactosidase enzymatic method; cytotoxicity on U-937 cells was assessed by using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] method. On the other hand,
in vivo
therapeutical response to
3a-f
compounds was evaluated in BALB/c mice (
Mus musculus
) experimentally infected with
T. cruzi
blood trypomastigotes and then orally administered with 100 mg/kg weight day for 20 days. All of the compounds showed
in vitro
activity with EC
50
values ranging between 4.6 ± 0.1 μg/mL (14.4 μM) and 36.6 ± 6.1 μg/mL (91 μM). Furthermore, treatment with
3a-f
compounds for 20 days resulted in improvement in all of the mice, with a 83–96% decrease in parasitic load at day 90 post-treatment. Treatment with benznidazol (BZ) managed to cure 100% of the mice at the end of treatment. None of the treatments affected the weight of the animals or alanine aminotransferase (ALT), blood urea nitrogen (BUN) and creatinine levels in serum. These results suggest a therapeutic potential of
3a-f
compounds as treatment for the infection.