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

Authors
Lin, NH Abreo, MA Gunn, DE Lebold, SA Lee, EL Wasicak, JT Hettinger, AM Daanen, JF Garvey, DS Campbell, JE Sullivan, JP Williams, M Arneric, SP
Citation
Nh. Lin et al., Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework, BIOORG MED, 9(18), 1999, pp. 2747-2752
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
18
Year of publication
1999
Pages
2747 - 2752
Database
ISI
SICI code
0960-894X(19990920)9:18<2747:SSOANS>2.0.ZU;2-G
Abstract
Analogs of compound 1 with a variety of azacycles and heteroaryl groups wer e synthesized. These analogs exhibited K-i values ranging from 0.15 to 1 10 ,000 nM when tested in vitro for cholinergic channel receptor binding activ ity (displacement of [H-3](-) cytisine from whole rat brain synaptic membra nes). (C) 1999 Elsevier Science Ltd. All rights reserved.