A novel artemisinin–quinine hybrid with potent antimalarial activity

Artemisinin was reduced to dihydroartemisinin and coupled to a carboxylic acid derivative of quinine via an ester linkage. This novel hybrid molecule had potent activity against the 3D7 and (drug-resistant) FcB1 strains of Plasmodium falciparum in culture. The activity was superior to that of artemisinin alone, quinine alone, or a 1:1 mixture of artemisinin and quinine.

Graphical abstractThe artemisinin–quinine hybrid 7 was synthesised and shown to have potent activity against the 3D7 and drug-resistant FcB1 strains of Plasmodium falciparum in culture. Its activity was superior to that of artemisinin alone, quinine alone, or a 1:1 mixture of artemisinin and quinine.Figure optionsDownload full-size imageDownload as PowerPoint slide