Synthesis and antimalarial activities of 12 beta-allyldeoxoartemisinin and its derivatives.
Synthesis of 12 beta-allyldeoxoartemisinin from dihydroartemisinin and subsequent transformations to other 12 beta-alkyldeoxoartemisinins are described. All compounds were tested in vitro versus two drug-resistant strains (Plasmodium falciparum) of malaria. The in vivo activity and toxicity of the most active compound, 12 beta-propyldeoxoartemisinin, were comparable to that of arteether.
Pu
Y M
YM
Laboratory of Chemical Physics, NIDDK, Bethesda, Maryland 20892-0510.
Ziffer
H
H
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D037621:Artemisinins; D004285:Dogs; D051379:Mice; D010963:Plasmodium falciparum / Q000187:drug effects; D012717:Sesquiterpenes / Q000138:chemical synthesis* / Q000494:pharmacology
C092098:12-allyldeoxoartemisinin; D000962:Antimalarials; D037621:Artemisinins; D012717:Sesquiterpenes