Nitroheterocyclic N-acylhydrazones as antischistosomal agents

Vol. 1, 2019 - 110426
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Resumo

N-acylhydrazone is a privileged chemical group which have been widely explored against parasitic diseases Our group has been exploring different series of N-acylhydrazones, with and without nitro group, against Leishmania amazonensis and L. donovani with promising results. These molecules, however, have never been tested against Schistosoma mansoni. Herein we report the evaluation of 23 N-acylhydrazones derivatives, bearing or not the nitro group, against S. mansoni adult worms, as well as against HaCaT cells to assess the cytotoxicity (CC50). Three analogues exhibited IC50 values below 10 µM and eleven compounds, IC50 from 10 to 50 µM. These fourteen compounds presented CC50>250 µM. The 5-nitrofurans exhibited the best performance while only one non-nitrated analogue showed activity below 10 µM. Interesting this compound was also the only non-nitrated analogue which exhibited previous antileishmanial activity at the same range of concentration. These results reveal the N-acylhydrazones as new potential scaffolds to antischistosomal agents.

Instituições
  • 1 Núcleo de Pesquisa em Doenças Negligenciadas / Universidade Guarulhos
Palavras-chave
Schistosoma mansoni
N-acylhydrazones
nitro compounds
antischistosomal agents