| Summary: | Sesquiterpene lactones are naturally occurring compounds mainly found in the Asteraceae family. These types of plant metabolites display a wide range of biological activities, including antiprotozoal activity and are considered interesting structures for drug discovery. Four derivatives were synthesized from estafietin (<b>1</b>), isolated from <i>Stevia alpina</i> (Asteraceae): 11βH,13-dihydroestafietin (<b>2</b>), epoxyestafietin (<b>3a</b> and <b>3b</b>), 11βH,13-methoxyestafietin, (<b>4</b>) and 11βH,13-cianoestafietin. The antiprotozoal activity against <i>Trypanosoma cruzi</i> and <i>Leishmania braziliensis</i> of these compounds was evaluated. Epoxyestafietin was the most active compound against <i>T. cruzi</i> trypomastigotes and amastigotes (IC<sub>50</sub> values of 18.7 and 2.0 µg/mL, respectively). Estafietin (<b>1</b>) and 11βH,13-dihydroestafietin (<b>2</b>) were the most active and selective compounds on <i>L. braziliensis</i> promastigotes (IC<sub>50</sub> values of 1.0 and 1.3 μg/mL, respectively). The antiparasitic activity demonstrated by estafietin and some of its derivatives make them promising candidates for the development of effective compounds for the treatment of Chagas disease and leihsmaniasis.
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