Synthesis and Antimalarial Activity of Some New 1,2-Dioxolane Derivatives

The synthesis of 1,2-dioxolane derivatives in two different acetophenone series, as simplified models of natural coumarins is described. 2-Acetyl-3-acetoxy-4-(3-hydroperoxy-3-methylbut-1-enyl)phenyl acetate and 2-acetyl-5-acetoxy-4-(3-hydroperoxy-3-methylbut-1-enyl) phenyl acetate synthons are used...

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Veröffentlicht in:	Journal of enzyme inhibition and medicinal chemistry 2002-01, Vol.17 (6), p.431-437
Hauptverfasser:	Helesbeux, Jean-Jacques, Peyronnet, Damien, Labaïed, Mehdi, Grellier, Philippe, Frappier, François, Seraphin, Denis, Richomme, Pascal, Duval, Olivier
Format:	Artikel
Sprache:	eng
Schlagworte:	1,2-Dioxolane Acetophenones - chemistry Animals Antimalarial Activity Antimalarials - chemical synthesis Antimalarials - pharmacology Chemical Sciences Dioxolanes - chemical synthesis Dioxolanes - pharmacology Inhibitory Concentration 50 Life Sciences Microbiology and Parasitology Molecular Structure Natural Product Models Photochemistry Plasmodium falciparum - drug effects Structure-Activity Relationship Tertiary Allylic Hydroperoxide
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Zusammenfassung:	The synthesis of 1,2-dioxolane derivatives in two different acetophenone series, as simplified models of natural coumarins is described. 2-Acetyl-3-acetoxy-4-(3-hydroperoxy-3-methylbut-1-enyl)phenyl acetate and 2-acetyl-5-acetoxy-4-(3-hydroperoxy-3-methylbut-1-enyl) phenyl acetate synthons are used as precursors to these structures. In vitro antimalarial activity of the 1,2-dioxolane derivatives has been investigated.
ISSN:	1475-6366 1475-6374
DOI:	10.1080/1475636021000005677