Over the last decades, neglected tropical diseases (NTDs), especially
leishmaniasis, have been the focus of several drug discovery programs. The
identification of the pathogen druggable targets and the ability to map the differences
between parasites and human enzymes have contributed to the increased interest in the
development of new lead compounds. Despite this progress, there remain substantial
gaps with respect to developing efficient medications that can be the foundation for
surmounting the acquired resistance and overcoming treatment failure. With this
background in mind, this chapter will discuss the validated drug targets with a special
focus on the reported structural determinants of activity of novel antileishmanial
agents. The aim is to introduce an updated overview of the medicinal chemistry aspects
of leishmaniasis to the scientific community.
Keywords: Current treatment, Leishmaniasis, Natural antiparasitic agents, Neglected tropical diseases, Semisynthetic antileishmanial agents, Synthetic drugs.
