The present invention relates to various novel substituted dipeptide derived nitrogen-containing heterocyclic compounds, their pharmaceutically acceptable salt derivatives, and their methods of use. In one aspect the present invention relates to compositions and methods for the treatment and prevention of disease in a mammal comprising administering the compounds of the invention in a pharmaceutically acceptable form to a mammal. In particular, the invention relates to medicaments comprising various novel substituted dipeptide derived nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salt derivatives and methods for administration to a mammal for the treatment and prevention of malarial diseases. The compounds of the invention may optionally be administered with at least one pharmaceutically acceptable excipient, another biologically active agent or a combination thereof.