Síntese e avaliação da atividade antileishmanial in vitro de bioisósteros do resveratrol

Autores

  • Natália Prado da Silva
  • Luciana Maria Ribeiro Antinarelli
  • Juliana Alves dos Santos
  • Adilson David da Silva
  • Raíssa Soares Meinel
  • Ayla das Chagas Almeida
  • Rodrigo Pedro Pinto Soares
  • Elaine Soares Coimbra

DOI:

https://doi.org/10.34019/2179-3700.2018.v18.29863

Palavras-chave:

Leishmania sp., Bioisósteros, Resveratrol, Tratamento

Resumo

As leishmanioses são infecções causadas por protozoários do gênero Leishmania, responsáveis por altas taxas de morbidade e mortalidade em todo mundo. O tratamento está restrito a um número limitado de fármacos com alta toxicidade, variabilidade na eficácia e alto custo. Neste trabalho foram sintetizados quatro bioisósteros do resveratrol que foram avaliados em formas promastigotas de Leishmania amazonensis e L. braziliensis associadas à manifestação tegumentar da doença, além da citotoxicidade em macrófagos murinos. Dois dos compostos, 1a e 1b exibiram promissores resultados, com CI50 variando de 3,0 a 16,44 µM, e não apresentaram toxicidade em macrófagos peritoneais. O composto 1b exibiu o maior índice de seletividade (> 25) para ambas as espécies. Esses resultados indicam o potencial desta classe de compostos para o desenvolvimento de novos agentes antileishmaniais e estimulam a realização de estudos em amastigotas intracelulares e a avaliação do seu mecanismo de ação.

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Publicado

2020-03-05

Como Citar

Silva, N. P. da, Antinarelli, L. M. R., Santos, J. A. dos, Silva, A. D. da, Meinel, R. S., Almeida, A. das C., Soares, R. P. P., & Coimbra, E. S. (2020). Síntese e avaliação da atividade antileishmanial in vitro de bioisósteros do resveratrol. Principia: Caminhos Da Iniciação Científica, 18(1), 10. https://doi.org/10.34019/2179-3700.2018.v18.29863

Edição

Seção

Artigos originais - Ciências Biológicas