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2099-12-31
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ESTUDO DE MÉTODOS DE OBTENÇÃO DE DERIVADOS PIRRÓLICOS E AVALIAÇÃO DA ATIVIDADE ANTI-TRYPANOSOMA CRUZI
Titulo alternativo
Study of Methods for the Synthesis of Pyrrole Derivatives and Evaluation of anti-Trypanosoma cruzi ActivityAutor
Afiliación
Universidade Federal do Rio de Janeiro. Instituto de Química. Rio de Janeiro, RJ, Brasil/Department of Chemical and Biomolecular Engineering. North Carolina State University. Raleigh, Estados Unidos da América
Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil
Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil
Universidade Federal do Rio de Janeiro. Instituto de Química. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil
Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil
Universidade Federal do Rio de Janeiro. Instituto de Química. Rio de Janeiro, RJ, Brasil.
Resumen en ingles
In this paper, pyrrole compounds were synthesized based on the Knorr method consisting of a cyclocondensation reaction between α-amino-β-ketoester with β-ketoesters and β-diketone. Different pyrrole derivatives were obtained by varying the composition of the ester group into β-ketoesters through transesterification reactions. Furthermore, after the synthesis of pyrrole nuclei, acid hydrolysis reactions, decarboxylation of the tert-butyl group, electrophilic aromatic substitution using N-bromosuccinimide or reaction with thiosemicarbazide were explored to vary the composition of the α group in relation to the nitrogen heteroatom of the pyrrole nuclei. Regarding the anti-Trypanosoma cruzi activity of pyrrole derivatives, 4 compounds synthesized were active, with IC50 ranging between 14.1 and >50 µM.
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