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

A series of potent and soluble ORL1 agonists was prepared and evaluated. Compound 41 showed antinociceptive properties in mouse formalin paw test (ED 50 = 1.07 μmol/kg). A series of 3-phenoxypropyl piperidine analogues have been discovered as novel ORL1 receptor agonists. Structure–activity relation...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters Jg. 15; H. 3; S. 589 - 593
Hauptverfasser:	Palin, Ronald, Barn, David R., Clark, John K., Cottney, Jean E., Cowley, Phillip M., Crockatt, Marc, Evans, Louise, Feilden, Helen, Goodwin, Richard R., Griekspoor, Frank, Grove, Simon J.A., Houghton, Andrea K., Jones, Philip S., Morphy, Richard J., Smith, Alasdair R.C., Sundaram, Hardy, Vrolijk, David, Weston, Mark A., Wishart, Grant, Wren, Paul
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	Oxford Elsevier Ltd 01.02.2005 Elsevier
Schlagworte:	Analgesia Analgesics Animals Biological and medical sciences CHO Cells Cricetinae Cyclic AMP - biosynthesis Drug Design Humans Hydrophobic and Hydrophilic Interactions Inhibitory Concentration 50 Male Medical sciences Mice Neuropharmacology Nociception Opioid ORL1 Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - pharmacology Receptors, Opioid - agonists Structure-Activity Relationship Transfection Vas Deferens Nociception Opioid Analgesia ORL1 Agonist Intravenous administration Rodentia Selectivity In vitro In vivo Vertebrata Mammalia Analgesic Structure activity relation Mouse Benzimidazole derivatives N/OFQ receptor Animal Piperidine derivatives Chemical synthesis
ISSN:	0960-894X, 1464-3405
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Zusammenfassung:	A series of potent and soluble ORL1 agonists was prepared and evaluated. Compound 41 showed antinociceptive properties in mouse formalin paw test (ED 50 = 1.07 μmol/kg). 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.
Bibliographie:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.11.049