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Phthalimido-thiazoles As Building Blocks And Their Effects On The Growth And Morphology Of Trypanosoma Cruzi.

P. A. T. Gomes, A. R. Oliveira, M. V. O. Cardoso, E. F. Santiago, Miria de Oliveira Barbosa, Lucianna Rabelo Pessoa de Siqueira, D. Moreira, T. M. Bastos, F. Brayner, M. Soares, Andresa Pereira Oliveira Mendes, M. C. A. B. de Castro, V. Pereira, A. Leite,
Published 2016 · Biology, Medicine

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Chagas disease is a parasitic infection caused by protozoan Trypanosoma cruzi that affects approximately 6-7 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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