Biological activities of 1,4-naphthoquinones derivatives against T. cruzi and L. amazonensis

Abstract

Introduction: Chagas disease and Leishmaniasis are neglected diseases caused bythe Trypanosoma cruzi and kentoplastid parasites Leishmania spp. Parasitic diseasescause great impact on social and economic, affecting millions of people in the worldand represent a major global health problem. In the search for new alternatives for thetreatment of Leishmaniasis and Chagas disease, strategies have been used to discovernew active molecules, because there is an urgent need for the development of newdrugs. In this scenario, 1,4-naphthoquinones have shown notable activity in thecontext of neglected diseases. Aim: To synthesis of 1,4-naphthoquinones derivativesand evaluated these compounds against Trypanosoma cruzi epimastigotes, Leishmaniapromastigotes (Leishmania amazonensis) and cytotoxicity to LLCMK2 cells.Results: Nine 1,4-naphthoquinones derivatives were synthesized using 2-Bromo-1,4-naphthoquinone (1), 1,4-Naphthoquinone (5) and 2-Hydroxi-1,4-naphthoquinone(9) as starting material. Derivative 6a exhibited excellent trypanocidal activity,IC50 of 0.25 ± 0.02 μM, superior potency compared with the reference drug Benznidazol.Besides, these compounds displayed low activity against promastigote from L.amazonensis. Conclusion: The results indicate that compound 6a may have potentialfor agent against Chagas disease.