Synthesis and structure-activity relationships of open D-Ring galanthamine analogues.
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.
Herlem
Denyse
D
Institut de Chimie des Substances Naturelles, C.N.R.S., 91198 Cedex, Gif-sur-Yvette, France.,
Martin
Marie Thérèse
MT
Thal
Claude
C
Guillou
Catherine
C
D000818:Animals; D002091:Butyrylcholinesterase / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D004557:Electric Organ / Q000187:drug effects / Q000201:enzymology; D004593:Electrophorus; D005702:Galantamine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D002800:Cholinesterase Inhibitors; D005702:Galantamine; D002091:Butyrylcholinesterase