Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.
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.
Palin
Ronald
R
Department of Medicinal Chemistry, Organon Laboratories Ltd, Newhouse, Lanarkshire ML1 5SH, UK. r.palin@organon.co.uk
Barn
David R
DR
Clark
John K
JK
Cottney
Jean E
JE
Cowley
Phillip M
PM
Crockatt
Marc
M
Evans
Louise
L
Feilden
Helen
H
Goodwin
Richard R
RR
Griekspoor
Frank
F
Grove
Simon J A
SJ
Houghton
Andrea K
AK
Jones
Philip S
PS
Morphy
Richard J
RJ
Smith
Alasdair R C
AR
Sundaram
Hardy
H
Vrolijk
David
D
Weston
Mark A
MA
Wishart
Grant
G
Wren
Paul
P
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D000242:Cyclic AMP / Q000096:biosynthesis; D015195:Drug Design; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D008297:Male; D051379:Mice; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011957:Receptors, Opioid / Q000819:agonists*; D013329:Structure-Activity Relationship; D014162:Transfection; D014649:Vas Deferens; D000094942:Nociceptin Receptor
D010880:Piperidines; D011957:Receptors, Opioid; D000242:Cyclic AMP; D000094942:Nociceptin Receptor