Artemisinin, a target for fluorine chemists: challenging molecule, efficient antimalarial drug


Daniele Bonnet-Delpon,, BIOCIS UMR CNRS 8076, Faculte de Pharmacie, Rue JB Clement, 92296 Chatenay-Malabry, France
Artemisinin 1 is the antimalarial principle isolated from a plant used in traditional Chinese medicine. Artemisinin and artemisinin derivatives are very efficient against chloroquine-resistant strains of Plasmodium falciparum. However, they undergo in vivo a rapid biotransformation limiting the duration of the protection and recrudescence of parasitemia is often observed. Fluorine substitution is a new approach to design more metabolically stable artemisinin antimalarials. Some challenges regarding the synthesis of fluoroartemisinins as well the beneficial effects of fluorine substitution on the pharmacological behaviour of artemisinin derivatives will be presented.