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

N H Lin; M A Abreo; D E Gunn; S A Lebold; E L Lee; J T Wasicak; A M Hettinger; J F Daanen; D S Garvey; J E Campbell; J P Sullivan; M Williams; S P Arneric

doi:10.1016/s0960-894x(99)00462-x

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

Bioorg Med Chem Lett. 1999 Sep 20;9(18):2747-52. doi: 10.1016/s0960-894x(99)00462-x.

Authors

N H Lin¹, M A Abreo, D E Gunn, S A Lebold, E L Lee, J T Wasicak, A M Hettinger, J F Daanen, D S Garvey, J E Campbell, J P Sullivan, M Williams, S P Arneric

Affiliation

¹ Abbott Laboratories, Abbott Park, IL 60064-3500, USA.

PMID: 10509928
DOI: 10.1016/s0960-894x(99)00462-x

Abstract

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).

MeSH terms

Animals
Brain / metabolism
Cholinergic Agonists / chemistry
Cholinergic Agonists / metabolism
Cholinergic Agonists / pharmacology*
Ethers / chemistry
Rats
Structure-Activity Relationship

Substances

Cholinergic Agonists
Ethers