ABSTRACT

194Metal complexes have demonstrated to be a promising alternative in the search of new drugs for the treatment of neglected tropical diseases and, particularly, those caused by trypanosomatid parasites. Although random screening has been a useful weapon in metal-based drug discovery of antiparasitic compounds, current research and development (R&D) in this field should be guided by rational design. The precise selection of the metal ion and the nature of the coordinated ligands are crucial in tuning the chemical and biological properties of the metal complex. In fact, the complexation of bioactive ligands has been extensively used as a strategy to improve the pharmacological properties of metal-based drugs. Additionally, ancillary ligands or co-ligands could also be included in the metal ion coordination sphere. On the one hand, properties like stability, water solubility, or lipophilicity of the metal compound can be tuned through the correct selection of the co-ligand. On the other hand, co-ligands could have an intrinsic biological activity leading to multifunctional metal compounds. In this chapter, some examples of these approaches in the design of prospective antiparasitic metal-based compounds will be discussed.