Journal
REVISTA VIRTUAL DE QUIMICA
Volume 13, Issue 1, Pages 146-155Publisher
SOC BRASILEIRA QUIMICA
DOI: 10.21577/1984-6835.20200136
Keywords
Chagas disease; Flavones; Trypanosoma cruzi; Trypanocidal
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Funding
- CoordenacAo de Aperfeicoamento de Pessoal de Nivel Superior - Brasil (CAPES) [001]
- Universidade Federal de Ouro Preto (UFOP)
- FAPEMIG
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)
- Programa de Pos-graduacAo em Ciencias da Saude, Fiocruz Minas (CAPES/PNPD)
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The synthesis and evaluation of flavones as trypanocidal agents was conducted, with some compounds showing modest activity against T cruzi, particularly those with nitro or methoxy substituents. Structural modifications at position 3 of the dihydropyrone ring resulted in the most active flavone, indicating potential for promising new compounds with trypanocidal properties.
Chagas disease is caused by infection of the parasite protozoan Trypanosoma cruzi and affects about 8 million people in 21 countries in Latin America. Treatment of this disease is still based on the use of benznidazole or nifurtimox, which both present low cure rates in the chronic phase and often have many undesirable side effects. Herein, we describe the synthesis of flavones and evaluation of their trypanocidal activity. The flavones were tested to in vitro against T cruzi and amongst the 13 compounds tested, 6 of these demonstrated some modest trypanocidal activity in vitro. Enhancements in anti T cruzi activity were noted for flavones bearing either nitro or methoxy substituents. Moreover, very low cytotoxicities were maintained for flavones with methoxy groups which suggests that this functional group favors more selective trypanocidal compounds. Finally, structural modification at position 3 of the dihydropyrone ring provided the most active flavone, which suggests that the introduction of different functionalities at this position could yield promising new compounds with trypanocidal properties.
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