Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts

C Guillou; A Mary; D Z Renko; E Gras; C Thal

doi:10.1016/s0960-894x(00)00059-7

Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts

Bioorg Med Chem Lett. 2000 Apr 3;10(7):637-9. doi: 10.1016/s0960-894x(00)00059-7.

Authors

C Guillou¹, A Mary, D Z Renko, E Gras, C Thal

Affiliation

¹ Institut de Chimie des Substances Naturelles, C.N.R.S., Gif-sur-Yvette, France. guillou@icsn.cnrs-gif.fr

PMID: 10762042
DOI: 10.1016/s0960-894x(00)00059-7

Abstract

The syntheses, the anticholinesterase activities and structure-activity relationships of homodimeric (3a-c) and heterodimeric (6a-c) alkylene linked bis-galanthamine are reported. Compounds 6b-c were found to be more potent than galanthamine and tacrine in inhibiting AChE.

MeSH terms

Acetylcholinesterase / drug effects
Acetylcholinesterase / metabolism*
Cholinesterase Inhibitors / chemical synthesis
Cholinesterase Inhibitors / chemistry
Cholinesterase Inhibitors / pharmacology*
Dimerization
Drug Design
Galantamine / analogs & derivatives*
Galantamine / chemical synthesis
Galantamine / pharmacology*
Structure-Activity Relationship

Substances

Cholinesterase Inhibitors
Galantamine
Acetylcholinesterase