Quinoxaline derivatives as antiparasitic drugs: proof of concept

Abstract

Quinoxalines are a class of heterocyclic compounds that have been intensively studied for their biological activities, showing promising activity against protozoa. In an ongoing study towards the discovery of new antiparasitic compounds, we have synthesized a library of quinoxaline derivatives, which has been evaluated in vitro against epimastigote, promastigote, and trypomastigote forms of Trypanossoma cruzi and intracellular amastigote and promastigote forms of Leishmania amazonensis. From this screening, we have selected the most active compounds for in vivo and mechanistic studies. The main objective of this project is to prove the biological activity of these compounds in the drug development for tropical diseases such as Chagas'disease and leishmaniasis. More specifically, our goal is the synthesis of quinoxaline derivatives aiming at improving yield, a scalable and safe process and decreasing of chemical residues. Looking into pharmaceutical application of these drug candidates, they will be evaluated in vitro and in vivo in order to determine their mechanism of action against T. cruzi and L. amazonensis. (AU)