Synthesis and antimalarial activity of some new 1,2-dioxolane derivatives

J Enzyme Inhib Med Chem. 2002 Dec;17(6):431-7. doi: 10.1080/1475636021000005677.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetophenones / chemistry
  • Animals
  • Antimalarials / chemical synthesis*
  • Antimalarials / pharmacology*
  • Dioxolanes / chemical synthesis*
  • Dioxolanes / pharmacology*
  • Inhibitory Concentration 50
  • Molecular Structure
  • Plasmodium falciparum / drug effects
  • Structure-Activity Relationship

Substances

  • Acetophenones
  • Antimalarials
  • Dioxolanes