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Development of new and more powerful antimalarial drugs has become more complex because of emergence of multidrug resistant strains of P. falciparum. Due to resistance of malaria parasite against well-known available drugs, the chemotherapy of malaria has become more complex and challenging. In this review we have discussed the life cycle of malaria parasite followed by quinoline based antimalarial drugs. Quinoline containing antimalarial compounds is the most effective class of drugs known for malaria chemotherapy. The list of commercially available antimalarial drugs along with their mode of action on different stages of parasite has been discussed in this review. A brief description of their mechanism of action and advantages and disadvantages are also reported. The combination chemotherapy and drugs under clinical trials and future strategies which are following are summarized in conclusion section. Aim of this review to summarize structure-activity relationship and medicinal chemistry developments in the field of therapeutic 4-amino quinoline derivatives.