Structure and antimalarial activity of adducts of 11-azaartemisinin with conjugated terminal acetylenes

Several N-substituted 11-azaartemisinins were prepared from 11-azaartemisinin in high yield by the DMAP catalyzed addition of terminal acetylenes conjugated with electron-withdrawing groups. Their antimalarial activities against two drug-resistant strains ofPlasmodium falciparum were determined.