Synthesis and antimalarial activities of 12β-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 m...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1995-02, Vol.38 (4), p.613-616
Main Authors: YU MING PU, ZIFFER, H
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimalarials - chemical synthesis
Antimalarials - pharmacology
Antiparasitic agents
Artemisinins
Biological and medical sciences
Dogs
Medical sciences
Mice
Pharmacology. Drug treatments
Plasmodium falciparum - drug effects
Sesquiterpenes - chemical synthesis
Sesquiterpenes - pharmacology
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00004a007