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-acetoxy4-(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.
Helesbeux
Jean-Jacques
JJ
SONAS, UFR des Sciences Pharmaceutiques et Ingénierie de la Santé, 16 Bd Daviers, 49100 Angers, France.
Peyronnet
Damien
D
Labaïed
Mehdi
M
Grellier
Philippe
P
Frappier
François
F
Seraphin
Denis
D
Richomme
Pascal
P
Duval
Olivier
O
D000098:Acetophenones / Q000737:chemistry; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D004148:Dioxolanes / Q000138:chemical synthesis* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
D000098:Acetophenones; D000962:Antimalarials; D004148:Dioxolanes