Abstract:

Chagas disease (CD), caused by the protozoan Trypanosoma cruzi, affects approximately eight million individuals in Latin America. CD is characterized by a short acute phase defined by patent parasitemia and a long and progressive chronic phase. Up to 40%-50% of chronically infected patients develop progressive cardiomyopathy and/or motility disturbances of the esophagus and colon. The available chemotherapy for CD is not satisfactory depending on two heterocyclic agents, nifurtimox and benznidazole. Naphthoquinones are considered privileged structures in medicinal chemistry due to their structural properties and biological activities. Recently, we have described the synthesis, trypanocidal and leishmanicidal activity of lapachone-based 1,2,3-triazoles. In this context, herein we describe the synthesis and evaluation against T. cruzi of 1,2,3-triazole substituted para-and ortho- naphthoquinones.