DB-766 is a potential chemotherapeutic candidate for Chagas' disease treatment. DB-766 exhibits strong trypanocidal activity and excellent selectivity for bloodstream trypomastigotes and intracellular amastigotes (Y strain), giving IC(50)s of 60 and 25 nM, respectively. The trypanocidal efficacy of DB766, suggesting that this AIA may represent a new lead compound candidate to Chagas.