Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework.
Analogs of compound 1 with a variety of azacycles and heteroaryl groups were synthesized. These analogs exhibited Ki 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).
Lin
N H
NH
Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
Abreo
M A
MA
Gunn
D E
DE
Lebold
S A
SA
Lee
E L
EL
Wasicak
J T
JT
Hettinger
A M
AM
Daanen
J F
JF
Garvey
D S
DS
Campbell
J E
JE
Sullivan
J P
JP
Williams
M
M
Arneric
S P
SP
D000818:Animals; D001921:Brain / Q000378:metabolism; D018679:Cholinergic Agonists / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D004987:Ethers / Q000737:chemistry; D051381:Rats; D013329:Structure-Activity Relationship
D018679:Cholinergic Agonists; D004987:Ethers