In the absence of accessible, effective vaccines, the fight against parasitic disease relies mostly on
chemotherapy. Nevertheless, the considerable side effects, high costs and growing number of refractory cases
comprise substantial drawbacks. Thus, the search for new antiparasitic compounds remains a high priority. The
polyamine biosynthesis, conversion and transport pathways offer different targets for selective chemotherapy.
Polyamine analogues and other antagonists may provide tools in the search for new lead compounds. Light and
electron microscopy techniques may encompass valuable approaches to elucidate the possible mechanisms of
action of different antiparasitic compounds, allowing the identification of subcellular target compartments, presumably
establishing the basis for a more rational drug design and/or planning of therapeutic strategies.