Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists

Ronald Palin; David R Barn; John K Clark; Jean E Cottney; Phillip M Cowley; Marc Crockatt; Louise Evans; Helen Feilden; Richard R Goodwin; Frank Griekspoor; Simon J A Grove; Andrea K Houghton; Philip S Jones; Richard J Morphy; Alasdair R C Smith; Hardy Sundaram; David Vrolijk; Mark A Weston; Grant Wishart; Paul Wren

doi:10.1016/j.bmcl.2004.11.049

Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists

Bioorg Med Chem Lett. 2005 Feb 1;15(3):589-93. doi: 10.1016/j.bmcl.2004.11.049.

Affiliation

¹ Department of Medicinal Chemistry, Organon Laboratories Ltd, Newhouse, Lanarkshire ML1 5SH, UK. r.palin@organon.co.uk

PMID: 15664818
DOI: 10.1016/j.bmcl.2004.11.049

Abstract

A series of 3-phenoxypropyl piperidine analogues have been discovered as novel ORL1 receptor agonists. Structure-activity relationships have been explored around the 3-phenoxypropyl region with several potent and selective analogues identified.

MeSH terms

Animals
CHO Cells
Cricetinae
Cyclic AMP / biosynthesis
Drug Design
Humans
Hydrophobic and Hydrophilic Interactions
Inhibitory Concentration 50
Male
Mice
Nociceptin Receptor
Piperidines / chemical synthesis*
Piperidines / pharmacology*
Receptors, Opioid / agonists*
Structure-Activity Relationship
Transfection
Vas Deferens

Substances

Piperidines
Receptors, Opioid
Cyclic AMP
Nociceptin Receptor