9Th Brazilian Symposium on Medicinal Chemistry

Chagas disease is one of the most important parasitic infections in the world and approximately 25 million people are at risk of contamination worldwide1. The current chemotherapy relies only in the nitro-heterocyclic drugs benznidazole, the first-line treatment in most countries; and nifurtimox. They are unsatisfactory due to limitations such side effects, long periods of treatment, and a effectiveness rate not exceeding 30% for patients in chronic phase, exposing the urgency for new trypanocidal agents2. We reported herein the synthesis and antitrypanosomal activitie of coumarinic N-acylhydrazonic derivatives. These compounds were synthesized using methodology with global yields ranging from 46%-70%. T. cruzi in vitro effect were evaluated against trypomastigote and amastigote form and two compounds (E)-N'-(4-hydroxybenzylidene)-2-oxo-2H-chromene-3-carbohydrazide and (E)-N'-(3,4-dihydroxybenzylidene)-2-oxo-2H-chromene-3-carbohydrazide revealed moderate activity displayed as IC50/96h = 20.9 µM and IC50/96h = 20.2 µM for both trypomastigotes and amastigotes intracellular forms could be good leads for the development of new trypanocidal agents.