M. Jung, Jewn‐Giew Park, Kong Jae Yang
Mar 1, 2001
Citations
0
Influential Citations
21
Citations
Journal
Archiv der Pharmazie
Abstract
3‐Methyl‐1,2,3,4‐tetrahydropyrimidine‐5‐carbaldehyde O‐substituted oximes 4 and 1‐(3‐methyl‐1,2,3,4‐tetrahydropyrimidin‐5‐yl)ethanone O‐substituted oximes 9 have been prepared as bioisosteric congeners of arecoline which is a muscarinic agonist for treatment of Alzheimer s disease. Starting from pyrimidine‐5‐carbaldehyde 1, formation of the 3‐methylpyrimidinium salt and subsequent reduction afforded 1,2,3,4‐tetrahydropyrimidine derivatives which were converted into oxalate salts in the interest of purity and stability. Binding affinities of prepared compounds for the cloned human muscarinic M1 receptor (h‐M1) were determined by radioligand binding assay using [3H]‐N‐methylscopolamine (NMS).