2-(ARYLOXYMETHYL)AZACYCLIC ANALOGS AS NOVEL NICOTINIC ACETYLCHOLINE-RECEPTOR (NACHR) LIGANDS

Authors
ELLIOTT RL KOPECKA H GUNN DE LIN NH GARVEY DS RYTHER KB HOLLADAY MW ANDERSON DJ CAMPBELL JE SULLIVAN JP BUCKLEY MJ GUNTHER KL ONEILL AB DECKER MW ARNERIC SP
Citation
Rl. Elliott et al., 2-(ARYLOXYMETHYL)AZACYCLIC ANALOGS AS NOVEL NICOTINIC ACETYLCHOLINE-RECEPTOR (NACHR) LIGANDS, Bioorganic & medicinal chemistry letters, 6(19), 1996, pp. 2283-2288
Citations number
36
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
19
Year of publication
1996
Pages
2283 - 2288
Database
ISI
SICI code
0960-894X(1996)6:19<2283:2AANNA>2.0.ZU;2-T
Abstract
A series of 2-(aryloxymethyl) azetidine and pyrrolidine nAChR ligands in which the 3-pyridyl moiety of a previously described series(1) was replaced by a substituted phenyl group was explored. Aromatic substitu tion afforded analogues with K-i values ranging from 3 Co >10,000 nM. Generally, substitution at the ortho- and para-position was unfavorabl e, whereas electron-withdrawing groups at the meta-position improved t he Ki values. Copyright (C) 1996 Elsevier Science Ltd