Malaria, a devastating infectious disease caused by parasites of Plasmodium genera is transmitted from person to person through bites of infected mosquitoes. It generally traps underdeveloped nations with poor infrastructure and high population density. It has attracted considerable attention from academic institutions, pharmaceutical industries and government agencies but the efforts to eradicate this threat face a number of technical, economic, financial and institutional hurdles. In the absence of clinically proven vaccines to combat malaria, chemotherapy continues to be the best available option, although it suffers from a big loophole of resistance. Emergence of resistance is associated with the two phases of Plasmodium's life cycle: asexual in humans and sexual in mosquito, which are intricate to target simultaneously. Consequently, the search for novel antimalarial agents is a never-ending task for scientists and chemists. This review aims at highlighting the currently used antimalarial agents, targets for the therapy and present scenario in the development of new antimalarial drugs to combat this global problem.