Synthesis of 6beta-D-glucosyl and 6-nitroxy (-)-galanthamine derivatives as acetylcholinesterase inhibitors

Pharmazie. 2007 Jun;62(6):403-5.

Abstract

Galanthamine is an alkaloid approved for the treatment of Alzheimer's disease. In this paper the syntheses and the anticholinesterase activities of new glucosyl and nitroxy derivatives substituted on position 6 are reported. Compounds 2, 3 and 5 presented a percentage of inhibition of 35.22%, 47.48% and 67.89% respectively.

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / enzymology
  • Cholinesterase Inhibitors / chemical synthesis*
  • Cholinesterase Inhibitors / pharmacology*
  • Chromatography, High Pressure Liquid
  • Galantamine / analogs & derivatives*
  • Galantamine / chemical synthesis
  • Galantamine / pharmacology*
  • In Vitro Techniques
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Male
  • Molecular Conformation
  • Rats
  • Rats, Sprague-Dawley
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Cholinesterase Inhibitors
  • Indicators and Reagents
  • Galantamine