Synthesis and antimalarial activity of dihydroperoxides and tetraoxanes conjugated with bis(benzyl)acetone derivatives

Chem Biol Drug Des. 2012 May;79(5):790-7. doi: 10.1111/j.1747-0285.2012.01345.x. Epub 2012 Mar 16.

Abstract

Dihydroperoxides and tetraoxanes derived from symmetrically substituted bis(arylmethyl)acetones were synthesized in modest to good yields using several methods. Three of these compounds exhibit an important in vitro antimalarial activity (1.0 μm ≤ IC(50) ≤ 5.0 μm) against blood forms of the human malaria parasite Plasmodium falciparum.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetone / chemical synthesis
  • Acetone / chemistry
  • Acetone / pharmacology
  • Antimalarials / chemical synthesis
  • Antimalarials / chemistry*
  • Antimalarials / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Malaria, Falciparum / drug therapy
  • Peroxides / chemical synthesis
  • Peroxides / chemistry*
  • Peroxides / pharmacology*
  • Plasmodium falciparum / drug effects*
  • Structure-Activity Relationship
  • Tetraoxanes / chemical synthesis
  • Tetraoxanes / chemistry*
  • Tetraoxanes / pharmacology*

Substances

  • Antimalarials
  • Peroxides
  • Tetraoxanes
  • Acetone