Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
2016
Chagas disease is a parasitic infection caused by protozoan Trypanosoma cruzi that affects approximately
6e7 million people worldwide. Benznidazole is the only drug approved for treatment during the acute
and asymptomatic chronic phases; however, its efficacy during the symptomatic chronic phase is
controversial. The present work reports the synthesis and anti-T. cruzi activities of a novel series of
phthalimido-thiazoles. Some of these compounds showed potent inhibition of the trypomastigote form
of the parasite at low cytotoxicity concentrations in spleen cells, and the resulting structure-activity
relationships are discussed. We also showed that phthalimido-thiazoles induced ultrastructural alterations
on morphology, flagellum shortening, chromatin condensation, mitochondria swelling, reservosomes
alterations and endoplasmic reticulum dilation. Together, these data revealed, for the first time, a
novel series of phthalimido-thiazoles-structure-based compounds with potential effects against T. cruzi
and lead-like characteristics against Chagas disease.
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