Synthesis and Antimalarial Activities of Some Novel 2-Pyridones

Malaria, one of the deadliest diseases that the world is facing, causes over 3 million deaths per year, most of them in Africa, Southeast Asia and South America. Parasite infections are increasing at a fast rate, with Plasmodium falciparum increasing in resistance to existing Antimalarials. Therefore, an urgent provision of more effective antimalarial drugs is required to limit the number of deaths caused by the malaria parasite. A new class of compounds with the envisaged ability to inhibit cysteine proteases, especially of Plasmodium , was designed, based on a 2-pyridone scaffold. Several intermediates were synthesized and showed some antimalarial activity.