New aryloxy-quinone derivatives with promising activity on Trypanosoma cruzi
作者： Christian Espinosa‐Bustos , Karina Vázquez , Javier Varela , Hugo Cerecetto , Margot Paulino
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摘要: Continuing with a program to develop new quinone derivatives as biologically active compounds, we designed and synthesized series of aryloxy-quinones, which were evaluated in vitro against Trypanosoma cruzi epimastigote form. Chemical modifications three specific moieties on the aryloxy-quinone core considered for developing anti-T. agents. The majority our quinones showed higher potency (IC50 values <0.70 µM) than nifurtimox, known pharmaceutical used baseline drug 7.00 µM); however, only two them elicited selectivity nifurtimox Vero cells. A structure-activity relationship analysis provided information about stereoelectronic features these are responsible an increase trypanosomicidal activity. Using pharmacophore model, mapped substitution patterns five pharmacophoric We chose Epc1 compounds found no effects. These results useful structural characteristics aryloxy-quinones protozoan parasite T. cruzi.
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