Artemisinin‐derived dimers and their antimalarial activities

Malaria is a tropical disease that leads around half a million people to succumb annually. Antimalarial agents such as artemisinin and its derivatives are crucial to malaria treatment; however, the rapid development of drug resistance to clinically used antimalarials is still the major obstacle to effective chemotherapy. To tackle the growing resistance issue, new antimalarial agents are urgently needed. Using artemisinin-derived dimers as pharmacological scaffolds has demonstrated promising antimalarial activity; therefore, rational design of the dimers may provide valuable therapeutic intervention to treat malaria or even drug-resistant malaria. This review emphasized two aspects: (a) different linker-tethered artemisinin-derived dimers with potential antimalarial activity and (b) the structure-activity relationships discussed to provide an insight for rational design of dimers with improved efficiency.