Antimalarial activity of yingzhaosu A analogues

J Med Chem. 2002 Oct 10;45(21):4732-6. doi: 10.1021/jm020208q.

Abstract

Iodonium ion mediated cyclization of unsaturated hydroperoxides 1 afforded the expected yingzhaosu A analogues 2. In some cases, however, the corresponding cyclic ethers 5 were formed competitively with the cyclic peroxides 2, the ratios of these two products being a marked function of the structure of the starting materials. Some of the cyclic peroxides 2 showed significant antimalarial activities in vitro and in vivo.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / chemical synthesis*
  • Antimalarials / pharmacology
  • Antimalarials / toxicity
  • Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis*
  • Bridged Bicyclo Compounds, Heterocyclic / chemistry*
  • Bridged Bicyclo Compounds, Heterocyclic / pharmacology
  • Bridged Bicyclo Compounds, Heterocyclic / toxicity
  • Catalysis
  • Cell Line
  • Cyclization
  • Malaria / drug therapy
  • Mice
  • Mice, Inbred ICR
  • Onium Compounds
  • Peroxides*
  • Plasmodium berghei
  • Plasmodium falciparum / drug effects
  • Pyridines
  • Sesquiterpenes*
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Bridged Bicyclo Compounds, Heterocyclic
  • Onium Compounds
  • Peroxides
  • Pyridines
  • Sesquiterpenes
  • iodonium dicollidine
  • yingzhaosu A