Chemical and biological analysis of 4-acyloxy-3-nitrocoumarins as trypanocidal agents

Chagas disease is the most widespread contagious tropical in Latin America, being an important public health problem. Treatments against this are still very ineffective, presenting several side effects. Therefore, search for alternative therapeutic solutions urgent. In present work, we evaluate trypanocidal activity and mechanism of action a select series synthetic 4-acyloxy-3-nitrocoumarins. All coumarin derivatives showed moderate trypomastigotes, along with low cytotoxicity. addition, compound 1 decreased number infected Vero cells intracellular T. cruzi model. Electron spin resonance electrochemical studies formation nitro radical anions. The Fukui index provided additional information to elucidate proposed reduction mechanism. Furthermore, vitro demonstrated potential these compounds achieve higher concentrations free radicals, proposing oxidative stress as possible no correlation was observed between diffusion compounds, which shows that lipophilicity not predominant factor activity. Elsevier Ltd. rights reserved.