Article
Trypanocidal Activity of Flavanone Derivatives
Registro en:
DIOGO, Gabriela Maciel et al. Trypanocidal Activity of Flavanone Derivatives. Molecules, v. 25, 397, 2020.
1420-3049
10.3390/molecules25020397
Autor
Diogo, Gabriela Maciel
Andrade, Josimara Souza
Murta, Silvane Maria Fonseca
Santos, Viviane Martins Rebello Dos
Taylor, Jason Guy
Resumen
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. 2025-01-01