Synthesis and biological activity against Trypanosoma cruzi of substituted 1,4-naphthoquinones

The discovery and development of essential drugs for Chagas disease is a major concern worldwide. New substituted 1,4-naphthoquinones were synthesized and tested against the infective bloodstream form of Trypanosoma cruzi, the etiological agent of Chagas disease. These products exhibited substantial activity against T. cruzi, especially 2-((8E,11Z)-heptadeca-8,11-dienyl)-3-hydroxynaphthalene-1,4-dione (9) with IC50 of 7.8 μM. [Display omitted] ► New substituted 1,4-naphthoquinones were synthesized. ► The products exhibited substantial activity against T. cruzi. ► The more active compound 9 showed a IC50 of 7.8 μM against T. cruzi.