Despite over a hundred years of drug development, malaria remains one of the most devastating infectious diseases in the world, both in terms of mortality and morbidity, and its worldwide occurrence in tropical and subtropical regions. During the last few decades, chloroquine and other aminoquinolines were the front-line antimalarial agents because of their excellent therapeutic efficacy and lower cost. However, the emergence and spread of resistance of malaria parasite, especially, most deadly species, P. falciparum towards currently available drugs, especially chloroquine, has become a major health concern around the globe and therefore, development of new chemotherapeutic agents is an urgent need to fight against resistant malaria.