Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework

Abstract

Analogs of compound 1 with a variety of azacycles and heteroaryl groups were synthesized. These analogs exhibited K i values ranging from 0.15 to > 10,000 nM when tested in vitro for cholinergic channel receptor binding activity (displacement of [ 3H](−) cytisine from whole rat brain synaptic membranes).