In Vitro Evaluation of Synthetic Flavones Against Trypanosoma cruzi

@inproceedings{SouzaAndrade2020InVE,
  title={In Vitro Evaluation of Synthetic Flavones Against Trypanosoma cruzi},
  author={Josimara Souza Andrade and Leonardo Gomes de Abreu and Policarpo Ademar Sales Junior and Silvane Maria Fonseca Murta and Jason Guy Taylor},
  year={2020}
}
Resumo: A doença de Chagas é uma infeção causada pelo protozoário parasita Trypanosoma cruzi e afeta cerca de 8 milhões de pessoas em 21 países da América Latina. O tratamento dessa doença ainda se baseia no uso de benzonidazol ou nifurtimox, que apresentam baixas taxas de cura na fase crônica e frequentemente apresentam muitos efeitos colaterais indesejáveis. Aqui, descrevemos a síntese de flavonas e a avaliação de sua atividade tripanocida. As flavonas foram testadas in vitro contra o T… 
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References

SHOWING 1-10 OF 31 REFERENCES

Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity

A majority of the compounds tested were very active and the most active isoxazole against amastigote and trypomastigotes of T. cruzi was slightly more potent than the current medicine benznidazole.

Design, synthesis, molecular modelling, and in vitro evaluation of tricyclic coumarins against Trypanosoma cruzi

The synthesis of tricyclic coumarins that were obtained via NHC organocatalysis and evaluation of their trypanocidal activity showed that these lead compounds are viable candidates for further in vivo assays.

Synthesis and Anti-Trypanosoma cruzi Activity of Diaryldiazepines

Differently substituted 5,7-diaryl-2,3-dihydro-1,4-diazepines were synthesized by cyclocondensation of substituted flavones with ethylenediamine and tested as anti-Trypanosoma cruzi candidates and the most potent diaryldiazepine that reduced epimastigote proliferation exhibited an IC50 value of 0.25 μM, which is significantly more active than benznidazole.

Evaluation of in vitro antiprotozoal activity of Ajuga laxmannii and its secondary metabolites

Many compounds showed moderate to good antiparasitic activity, with isoorientin displaying the most significant antimalarial potential (an IC50 value of 9.7 μg/mL).

Synthesis of Xylitan Derivatives and Preliminary Evaluation of in Vitro Trypanocidal Activity

The importance of the isopropylidene ketal moiety was established and the greater lipophilicity of these compounds suggests enhancement in cell penetration, and the best activity of all the compounds tested was the arylsulfonate xylitan derivative bearing a nitro group.

Trypanocidal activity of Meliaceae and Rutaceae plant extracts.

The results revealed that the order Rutales is a promising source for the search of new drugs for Chagas disease, and two flavonoids were isolated that showed weak trypanocidal activity.

In vitro trypanocidal activity of phenolic derivatives from Peperomia obtusifolia.

The trypanocidal activity of crude extracts and fractions from the leaves and stems of Peperomia obtusifolia (Piperaceae) was evaluated in vitro against the epimastigote forms of Trypanosoma cruzi.

Synthesis and Trypanocidal Properties of New Coumarin-Chalcone Derivatives

The coumarin-chalcone scaffold can be taken into account for further lead optimization and design new and more effective trypanocidal compounds.

Trypanocidal Activity of Flavanone Derivatives

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.