4.6 Article

Trypanocidal Activity of Flavanone Derivatives

期刊

MOLECULES
卷 25, 期 2, 页码 -

出版社

MDPI
DOI: 10.3390/molecules25020397

关键词

Chagas disease; flavanones; flavonoids; Trypanosoma cruzi; chromanones; in vitro; nitroreductase

资金

  1. Brazilian funding agency Fundacao de Amparo a Pesquisa do Estado de Minas Gerais (FAPEMIG) [APQ-01629-16]
  2. Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior-Brasil (CAPES) [001]

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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.

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