Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.
A series of aminoalkylazetidines has been discovered as novel ORL1 receptor ligands. Structure-activity relationships have been investigated at the azetidine N and the alkyl side chain sites. Several potent and selective analogues have been identified.
Wu
Wen-Lian
WL
Schering Plough Research Institute, 2015 Galloping Hill Road, MS 2800, Kenilworth, NJ 07033-0539, USA.
Caplen
Mary Ann
MA
Domalski
Martin S
MS
Zhang
Hongtao
H
Fawzi
Ahmad
A
Burnett
Duane A
DA
D000818:Animals; D001384:Azetidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D001667:Binding, Competitive / Q000187:drug effects; D016466:CHO Cells; D006224:Cricetinae; D004174:Diprenorphine / Q000494:pharmacology; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D006801:Humans; D007202:Indicators and Reagents; D008024:Ligands; D009292:Narcotic Antagonists / Q000494:pharmacology; D018847:Opioid Peptides / Q000378:metabolism; D011957:Receptors, Opioid / Q000187:drug effects*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D000094942:Nociceptin Receptor; D000097629:Nociceptin
D001384:Azetidines; D004174:Diprenorphine; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D007202:Indicators and Reagents; D008024:Ligands; D009292:Narcotic Antagonists; D018847:Opioid Peptides; D011957:Receptors, Opioid; D000094942:Nociceptin Receptor; D000097629:Nociceptin