Malaria-infected mice are cured by a single dose of novel artemisinin derivatives

J Med Chem. 2007 May 17;50(10):2516-9. doi: 10.1021/jm070149m. Epub 2007 Apr 17.

Abstract

We disclose here for the first time the curative activity of a new generation of trioxane dimers, designed logically and prepared easily from the natural trioxane artemisinin in only four or five chemical steps that would be easily accomplished also on a manufacturing scale. Four of these trioxane dimers cure malaria-infected mice after only a single subcutaneous dose, and two other dimers cure after three oral doses.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / chemical synthesis*
  • Antimalarials / chemistry
  • Antimalarials / therapeutic use
  • Artemisinins / chemical synthesis*
  • Artemisinins / chemistry
  • Artemisinins / therapeutic use
  • Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis*
  • Bridged Bicyclo Compounds, Heterocyclic / chemistry
  • Bridged Bicyclo Compounds, Heterocyclic / therapeutic use
  • Malaria / drug therapy*
  • Malaria / mortality
  • Mice
  • Plasmodium berghei
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Artemisinins
  • Bridged Bicyclo Compounds, Heterocyclic