PHENYL PYRROLIDINE ANALOGS AS POTENT NICOTINIC ACETYLCHOLINE-RECEPTOR(NACHR) LIGANDS

Authors
ELLIOTT RL RYTHER KB ANDERSON DJ RASZKIEWICZ JL CAMPBELL JE SULLIVAN JP GARVEY DS
Citation
Rl. Elliott et al., PHENYL PYRROLIDINE ANALOGS AS POTENT NICOTINIC ACETYLCHOLINE-RECEPTOR(NACHR) LIGANDS, Bioorganic & medicinal chemistry letters, 5(9), 1995, pp. 991-996
Citations number
40
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
9
Year of publication
1995
Pages
991 - 996
Database
ISI
SICI code
0960-894X(1995)5:9<991:PPAAPN>2.0.ZU;2-H
Abstract
The synthesis and SAR of a series of 2-phenyl pyrrolidines as neuronal nAChR ligands are described. Substitution on the aryl ring had a dram atic effect on receptor binding affinity, with K-i values ranging from 46 nM to >10,000 nM. Analogues 8, 9, and 14 were the most potent liga nds evaluated, having Ri values of 68 nM, 75 nM, and 46 nM; respective ly.