Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts.
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.
Guillou
C
C
Institut de Chimie des Substances Naturelles, C.N.R.S., Gif-sur-Yvette, France. guillou@icsn.cnrs-gif.fr
Mary
A
A
Renko
D Z
DZ
Gras
E
E
Thal
C
C
D000110:Acetylcholinesterase / Q000187:drug effects / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D019281:Dimerization; D015195:Drug Design; D005702:Galantamine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D002800:Cholinesterase Inhibitors; D005702:Galantamine; D000110:Acetylcholinesterase