Author | Barbieri, Eduardo | |
Author | Sales Junior, Policarpo Ademar | |
Author | Murta, Silvane Maria Fonseca | |
Author | Silva, Bárbara V. | |
Access date | 2023-08-02T14:18:59Z | |
Available date | 2023-08-02T14:18:59Z | |
Document date | 2022 | |
Citation | BARBIERI, Eduardo et al. Estudo de Métodos de Obtenção de Derivados Pirrólicos e Avaliação da Atividade Anti-Trypanosoma cruzi. Revista Virtual de Química, v. 14, n. 6, p. 966-983, 2022. doi.org/10.21577/1984-6835.20220052. | en_US |
ISSN | 1984-6835 | en_US |
URI | https://www.arca.fiocruz.br/handle/icict/59880 | |
Language | por | en_US |
Publisher | Sociedade Brasileira de Quimica | en_US |
Rights | restricted access | |
Title | Estudo de Métodos de Obtenção de Derivados Pirrólicos e Avaliação da Atividade Anti-Trypanosoma cruzi | en_US |
Alternative title | Study of Methods for the Synthesis of Pyrrole Derivatives and Evaluation of anti-Trypanosoma cruzi Activity | en_US |
Type | Article | |
Abstract | 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. | en_US |
Affilliation | 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 | en_US |
Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil | en_US |
Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil | en_US |
Affilliation | Universidade Federal do Rio de Janeiro. Instituto de Química. Rio de Janeiro, RJ, Brasil. | en_US |
Subject | Pyrrole | en_US |
Subject | Chagas disease | en_US |
Subject | β-ketoesters | en_US |
Subject | chemical transformations | en_US |
Embargo date | 2099-12-31 | |