Artemisinin-quinoline hybrid-dimers: Synthesis and in vitro antiplasmodial activity

Novel artemisinin-quinoline hybrid-dimers were synthesized from dihydroartemisinin and different aminoquinolines at elevated temperatures (90-110 degrees C). All compounds were obtained as the beta-isomers and were tested against both chloroquine sensitive and resistant strains of Plasmodium falciparum. Hybrid-dimer 8 showed the highest antiplasmodial activity, inheriting the optimum chain length of three carbon atoms. (C) 2010 Elsevier Ltd. All rights reserved.