**Abstract**

Leishmaniasis is one of the most important neglected tropical diseases. The chemotherapy for its treatment uses very toxic compounds with a low efficacy rate. Thus, there is an urgent need to develop new chemotherapeutic agents to help countries control this devasting disease. In drug development, different approaches can be used to identify potential cellular targets that allow us to understand better the cell biology of eukaryotic cells. Several groups are dedicated to studying new molecules, searching for promising candidates against *Leishmania*. Different techniques have been used to characterize the cell biology, biochemistry, and molecular biology alterations induced by the treatments, trying to understand the mechanisms of action. The main goal of this chapter is to describe an overview of the literature exploring the several studies published about the chemotherapy of anti-*Leishmania* concerning the mechanisms of action of different classes of molecules or therapeutic alternatives.

**Keywords:** chemotherapy, drug development, cell biology, ergosterol, histone deacetylases, organometallic compounds, therapeutic combination, nanotechnology
