Chagas disease is a neglected tropical disease caused by the protozoan parasite Trypanosoma cruzi affecting more than 6 million people worldwide.Its treatment is based in old and toxic nitroderivative drugs necessitating for new alternatives.Imatinib is a tyrosine kinase inhibitor used in cancer therapy and previous reports demonstrate that some derivatives are active against T.cruzi justifying further synthesis screening of novel compounds derived from imatinib.Our results demonstrate that all test derivatives are highly active against the intracellular forms of T. cruzi being similar or even more potent than the reference drug for Chagas disease -Benznidazole.Besides, they were much more active than the parent molecule, displaying low EC 90 values ( 10), which are relevant characteristics of a novel hit compound for Chagas disease therapy.However, when screened against bloodstream trypomastigotes, only one derivative, named PLDC 23/19, was as active (EC 50 = 18.8 M) as Benznidazole (EC 50 = 18.8 M), while the others did not show activity up to 20 M.
Freitas et al. (Wed,) studied this question.