Malaria is a tropical disease caused by infectious species of Plasmodium that
are transmitted to people through the bites of infected mosquitoes. Malaria kills more
than 650,000 people worldwide each year. Plasmodium resistance to antimalarial
medicines, toxicity and high cost are the major obstacles in the fight against this
disease. Therefore, there is an urgent need for the development of new more effective
and less toxic antimalarials, especially compounds that act against novel molecular
targets in order to circumvent the problem of increasing resistance. This chapter is
focused on recent advances in the field of synthesis of compounds having antimalarial
activity based on two strategies: synthesis of hybrid molecules and synthesis of
inhibitors of a cysteine protease (falcipain) that plays a key role in malaria parasites.
Keywords: Malaria, antimalarial drug, hybrid molecules, falcipain inhibitors.
