The activity of dispiro peroxides against Fasciola hepatica

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5320-3. doi: 10.1016/j.bmcl.2011.07.024. Epub 2011 Jul 19.

Abstract

Dispiro 1,2,4-trioxanes and 1,2,4,5-tetraoxanes had superior efficacy against Fasciola hepatica than the corresponding ozonides (1,2,4-trioxolanes). For highest efficacy, spiroadamantane and carboxymethyl substructures were required. Three compounds completely cured F. hepatica-infected mice at single oral doses of 50mg/kg and two were partially curative at single doses of 25mg/kg.

Publication types

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

MeSH terms

  • Animals
  • Dose-Response Relationship, Drug
  • Fasciola hepatica / drug effects*
  • Heterocyclic Compounds / chemical synthesis
  • Heterocyclic Compounds / chemistry
  • Heterocyclic Compounds / pharmacology*
  • Mice
  • Molecular Structure
  • Spiro Compounds / chemical synthesis
  • Spiro Compounds / chemistry
  • Spiro Compounds / pharmacology*
  • Stereoisomerism
  • Tetraoxanes / chemical synthesis
  • Tetraoxanes / chemistry
  • Tetraoxanes / pharmacology*

Substances

  • 1,2,4-trioxane
  • Heterocyclic Compounds
  • Spiro Compounds
  • Tetraoxanes