Avaliação da atividade antimalárica de análogos de 4-aminoquinolinas e 6-mercaptopurinas em modelo murino

Abstract

Malaria remains over the years as a global public health emergency. There are approximately 87 million cases and 106.820 deaths worldwide each year. The main current strategies to control the disease are based on early diagnosis and appropriate treatment cases and should be considered the resistance of parasites to almost all drugs currently in use, which makes urgent the search for new antimalarials. In this context, analogs of 4-aminoquinolines and 6-mercaptopurines containing 1,2,3-triazole or steroid were synthesized and investigated for their antimalarial activity using the 4-day suppressive test described by Peters in a murine model of infection by Plasmodium berghei NK65. Among the 11 analogues evaluated, 5 exhibited significant antimalarial activity, reaching percentages of suppression up to 81% compared to untreated control. Besides antimalarial activity, a promising compound cannot have undesirable effects on host cells, thus was evaluated the cytotoxicity and hemolytic activity of analogs. Most compounds were considered safe to host cells even at the highest concentrations evaluated. So, this analogs deserve to be object of future investigations aiming compose new antimalarials.