Structure-activity studies on acetylcholinesterase inhibition in the lycorine series of Amaryllidaceae alkaloids.
The synthesis of differentially functionalized analogs of the Amaryllidaceae alkaloid lycorine, accessed via a concise chemoselective silylation strategy, is described uncovering two of the most potent inhibitors of acetylcholinesterase (AChE) identified to date in this series. Important elements of this novel pharmacophore were elucidated through structure-activity relationship (SAR) studies.
McNulty
James
J
Department of Chemistry and Chemical Biology, McMaster University, Hamilton, Ontario, Canada. jmcnult@mcmaster.ca
Nair
Jerald J
JJ
Little
Jessamyn R L
JR
Brennan
John D
JD
Bastida
Jaume
J
D000470:Alkaloids / Q000737:chemistry* / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000470:Alkaloids; D002800:Cholinesterase Inhibitors