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  • Synthesis, docking, and in vitro activity of thiosemicarbazones, aminoacyl-thiosemicarbazides and acyl-thiazolidones against Trypanosoma cruzi.

Synthesis, docking, and in vitro activity of thiosemicarbazones, aminoacyl-thiosemicarbazides and acyl-thiazolidones against Trypanosoma cruzi.

Bioorganic & medicinal chemistry (2006-02-07)
Ana Cristina Lima Leite, Renata Souza de Lima, Diogo Rodrigo de M Moreira, Marcos Veríssimo de O Cardoso, Ana Carolina Gouveia de Brito, Luciene Maria Farias Dos Santos, Marcelo Zaldini Hernandes, Alice Costa Kiperstok, Ricardo Santana de Lima, Milena B P Soares
RESUMEN

A novel series of thiosemicarbazone and aminoacyl-thiazolidones derivatives were synthesized. Their structure suggests that these compounds could have anti-Trypanosoma cruzi activity. Biological evaluation indicates that some of these compounds are able to inhibit the growth of T. cruzi in concentrations non-cytotoxic to mammalian cells. Docking studies were carried out in order to investigate the binding pattern of these compounds for the T. cruzi cruzain (TCC) protein, and these showed a significant correlation with experimental data.

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Bromoacetaldehyde diethyl acetal, 97%