Synthesis and study of thiocarbonate derivatives of choline as potential inhibitors of acetylcholinesterase

NAJ Boyle, V Talesa, E Giovannini…

Index: Boyle, Nicholas A. J.; Talesa, Vincenzo; Giovannini, Elvio; Rosi, Gabriella; Norton, Scott J. Journal of Medicinal Chemistry, 1997 , vol. 40, # 19 p. 3009 - 3013

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Citation Number: 9

Abstract

Fourteen alkyl and aryl thiocarbonate derivatives of choline were synthesized and studied as potential inhibitors of acetylcholinesterase (AChE). Twelve of the compounds inhibited AChEs derived from calf forebrain, human red blood cells, and octopus brain ranging from low to moderately high inhibition potency. The concentration of each inhibitory compound giving 50% inhibition of enzyme activity (IC50 values, which ranged from 1× 10-2 to 8× 10- ...