In Vitro Evaluation of Synthetic Flavones Against Trypanosoma cruzi

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.

Automated summary

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.