9Th Brazilian Symposium on Medicinal Chemistry

Chagas disease is a neglected infection caused by Trypanosoma cruzi. Daily 10,000 people die from this disease. Available drugs are only effective in the acute phase and there is no treatment for the chronic phase of the disease. New drugs with better efficacy and toxicity profiles are desperately required. Thus, 21 analogs of chalcones hybridized with cyclic amines, compounds 1-21 (GA Text), were evaluated against three developmental stages of T. cruzi. Initially, they were evaluated against the epimastigote stage, as a result 20 compounds showed activity. Following, against the trypomastigote stage, herein 8 compounds were active and presented half maximal inhibitory concentration (IC50) between 0.8 and 44.52µM. Finally, against the amastigote stage, 16 compounds were active and demonstrated IC50 between 1.20 and 16.97μM. Compound 16 was one of the most potent against infectious stages, trypomastigote (acute phase) and amastigote (chronic phase), with IC50 of 0.8 and 1.27µM, respectively.