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

E Perissutti; F Fiorino; B Severino; F Frecentese; P Massarelli; C Nencini; V Santagada; G Caliendo

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

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

Authors

E Perissutti¹, F Fiorino, B Severino, F Frecentese, P Massarelli, C Nencini, V Santagada, G Caliendo

Affiliation

¹ Dipartimento di Chimica Farmaceutica e Tossicologica1, Università di Napoli Federico II, Napoli, Italy.

PMID: 17663183

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