Fluoroartemisinins: Metabolically More Stable Antimalarial Artemisinin Derivatives

This report is an overview on the design, preparation, and evaluation of metabolically stable artemisinins, using fluorine substitution. The chemical challenges encountered for the incorporation of fluorine‐containing elements and the preparation of a large range of 10‐trifluoromethyl artemisinin derivatives are detailed. Impact of the fluorine substitution on the antimalarial activity is also highlighted. Preclinical data of lead compounds, and evidence for their strong and prolonged antimalarial activity are presented. Fluoroartemisinins. Malaria continues to be one of the most important infectious diseases in the world. The increasing resistance of malaria parasites and resulting dramatic decline in the efficacy of the most affordable antimalarial drugs leads to a broad consensus on the need to develop new antimalarial drugs Artemisinin provides a crucial molecular framework from which medicinal chemists have prepared more efficacious antimalarial drugs.