Introduction: Malaria, a devastating infectious parasitic disease, has been recognized by the World Health Organization (WHO) as a major public health problem worldwide. It is one of the leading causes of morbidity and mortality in developing countries. There are a number of antimalarial drugs available in the market to combat this deadly disease. The situation is further worsened due to the emergence of resistant strains of Plasmodium falciparum, which warrants the search for novel antimalarial drugs capable of acting at multiple targets to expand the current antimalarial drug arsenal for better therapeutic outcome.

Objectives: This review aimed to provide the reader with the recent advances and progress made in the development of chemotherapeutic agents for malaria.

Methods: Literature review data on the chemistry and antimalarial activity of natural and synthetic heterocyclic compounds published in the last ten years were compiled by referring to various peerreviewed journal websites and medical search engines.

Results and Discussion: This review covers the recent advances and progress made in the treatment strategies, patent granted, synthetic approaches, mechanism of action with more emphasis on a Structure- activity Relationship (SAR) of potential chemotherapeutic agents as antimalarial agents which could pave the way for the development of more effective and potent antimalarial agents. This review might interest fellow researchers working on the development of novel antimalarial drug candidates with better therapeutic index.

Conclusion: Based on the literature covered in the current review article and seeing the recent trends, authors are of the opinion that the multi-target conjugated hybrid approach is the best strategy to discover and develop effective antimalarial agents.