Malaria is a parasitic disease caused to humans due to the infection spread by the parasite of genus Plasmodium and then it is transmitted by female Anopheles. The genus Plasmodium consists of many species but among them P. falciparum is the deadliest one. To avert potential public health crisis, a new antimalarial drug with single dose cures are required urgently. Several approaches to antimalarial drugs development are ranging from the modifications of existing agents that will design the novel agents which act against novel targets. Modern advances in parasite biology with various genomic techniques is available which target the development of new therapies. Proteases kinases, Plasmodium sugar transporter inhibitor, dihydroorotate dehydrogenase inhibitor, topoisomerase and Novel Quinazolin-2,4-Dione hybrid molecules are the inhibitors. The enzymes are involved in the lipid metabolism and DNA replication. These are the most fascinating antimalarial target proteins which are recently being studied. This review focus and summerises the novel molecular targets and inhibitors for antimalarial drug development strategies.