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 of Plasmodium falciparum were determined.
Katz
E
E
Israel Institute for Biological Research, Ness Ziona, Israel.
Ma
J
J
Kyle
D
D
Ziffer
H
H
D000114:Acetylene / Q000737:chemistry*; D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology*; D006575:Heterocyclic Compounds, 3-Ring / Q000737:chemistry* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000962:Antimalarials; D006575:Heterocyclic Compounds, 3-Ring; D000114:Acetylene