Synthesis and structure-activity relationships of open D-Ring galanthamine analogues

Denyse Herlem; Marie Thérèse Martin; Claude Thal; Catherine Guillou

doi:10.1016/s0960-894x(03)00397-4

Synthesis and structure-activity relationships of open D-Ring galanthamine analogues

Bioorg Med Chem Lett. 2003 Jul 21;13(14):2389-91. doi: 10.1016/s0960-894x(03)00397-4.

Authors

Denyse Herlem¹, Marie Thérèse Martin, Claude Thal, Catherine Guillou

Affiliation

¹ Institut de Chimie des Substances Naturelles, C.N.R.S., 91198 Cedex, Gif-sur-Yvette, France.,

PMID: 12824041
DOI: 10.1016/s0960-894x(03)00397-4

Abstract

Open D-ring galanthamine analogues were prepared using ring-opening reactions of the quaternarized urethane or oxazolidine functions and were evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition potency.

MeSH terms

Animals
Butyrylcholinesterase / metabolism
Cholinesterase Inhibitors / chemical synthesis*
Cholinesterase Inhibitors / pharmacology*
Electric Organ / drug effects
Electric Organ / enzymology
Electrophorus
Galantamine / analogs & derivatives
Galantamine / chemical synthesis*
Galantamine / pharmacology*
Magnetic Resonance Spectroscopy
Models, Molecular
Molecular Conformation
Structure-Activity Relationship
Substrate Specificity

Substances

Cholinesterase Inhibitors
Galantamine
Butyrylcholinesterase