Antimalarial activity of thiophenyl- and benzenesulfonyl-dihydroartemisinin

Each diastereomer of 10-thiophenyl- and 10-benzenesulfonyl-dihydroartemisinin was synthesized from artemisinin in three steps, and screened against chloroquine-resistance and chloroquine-sensitive Plasmodium falciparum. Three of the four tested compounds were found to be effective. Especially, 10 beta-benzenesulfonyl-dihydroartemisinin showed stronger antimalarial activity than artemisinin.