Recent developments in antimalarial activities of 4-aminoquinoline derivatives

Malaria is the fifth most lethal parasitic infection in the world. Antimalarial medications have played a crucial role in preventing and eradicating malaria. Numerous heterocyclic moieties have been incorporated into the creation of effective antimalarial drugs. The 4-aminoquinoline moiety is favoured in antimalarial drug discovery due to the diverse biological applications of its derivative. Since the 1960s, 4-aminoquinoline has been an important antimalarial drug due to its low toxicity, high tolerability, and rapid absorption after administration. This review focused on the antimalarial efficacy of the 4-aminoquinoline moiety hybridised with various heterocyclic scaffolds developed by scientists since 2018 against diverse Plasmodium clones. It could aid in the future development of more effective antimalarial agents. [Display omitted] •Developing drug resistance in malaria parasites is one of the most important problems with malaria control.•N-Containing heterocycles play an important role in designing and discovering novel malaria-active compounds.•Various 4-aminoquinoline derivatives have been broadly studied for antimalarial potency in recent years.•This review enclosed, physicochemical properties, molecular docking, cytotoxicity, and SAR results.