Author | Diogo, Gabriela Maciel | |
Author | Andrade, Josimara Souza | |
Author | Murta, Silvane Maria Fonseca | |
Author | Santos, Viviane Martins Rebello Dos | |
Author | Taylor, Jason Guy | |
Access date | 2020-04-28T12:36:08Z | |
Available date | 2020-04-28T12:36:08Z | |
Document date | 2020 | |
Citation | DIOGO, Gabriela Maciel et al. Trypanocidal Activity of Flavanone Derivatives. Molecules, v. 25, 397, 2020. | pt_BR |
ISSN | 1420-3049 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/41002 | |
Language | eng | pt_BR |
Publisher | MDPI | pt_BR |
Rights | restricted access | pt_BR |
Title | Trypanocidal Activity of Flavanone Derivatives | pt_BR |
Type | Article | pt_BR |
DOI | 10.3390/molecules25020397 | |
Abstract | Chagas disease, also known as American trypanosomiasis, is classified as a neglected disease by the World Health Organization. For clinical treatment, only two drugs have been on the market, Benznidazole and Nifurtimox, both of which are recommended for use in the acute phase but present low cure rates in the chronic phase. Furthermore, strong side effects may result in discontinuation of this treatment. Faced with this situation, we report the synthesis and trypanocidal activity of 3-benzoyl-flavanones. Novel 3-benzoyl-flavanone derivatives were prepared in satisfactory yields in the 3-step synthetic procedure. According to recommended guidelines, the whole cell-based screening methodology was utilized that allowed for the simultaneous use of both parasite forms responsible for human infection. The majority of the tested compounds displayed promising anti-Trypanosoma cruzi activity and the most potent flavanone bearing a nitrofuran moiety was more potent than the reference drug, Benznidazole. | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biologicas. Departamento de Quimica. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biologicas. Departamento de Quimica. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biologicas. Departamento de Quimica. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biologicas. Departamento de Quimica. Ouro Preto, MG, Brazil | pt_BR |
Subject | Chagas disease | pt_BR |
Subject | flavanones | pt_BR |
Subject | flavonoids | pt_BR |
Subject | Trypanosoma cruzi | pt_BR |
Subject | chromanones | pt_BR |
Subject | in vitro | pt_BR |
Subject | nitroreductase | pt_BR |
Embargo date | 2025-01-01 | |