Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
A series of 4-[2-(aminomethyl)phenyl]-1-[bis(2-chlorophenyl)methyl]-4-hydroxypiperidine analogs has been identified as nociceptin receptor ligands. These compounds display high affinity and functional activity at the nociceptin receptor. The synthesis and structure-activity relationships at the C-4 phenyl and N-1 positions are described and the antitussive activity of a selected compound is reported.
Ho
Ginny D
GD
Department of Chemical Research-CV & CNS, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. ginny.ho@spcorp.com
Bercovici
Ana
A
Tulshian
Deen
D
Greenlee
William J
WJ
Fawzi
Ahmad
A
Fernandez
Xiomara
X
McLeod
Robbie L
RL
Smith Torhan
April
A
Zhang
Hongtao
H
D000818:Animals; D000996:Antitussive Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006168:Guinea Pigs; D006801:Humans; D008024:Ligands; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011957:Receptors, Opioid / Q000819:agonists*; D013329:Structure-Activity Relationship; D000094942:Nociceptin Receptor
D000996:Antitussive Agents; D008024:Ligands; D010880:Piperidines; D011957:Receptors, Opioid; D000094942:Nociceptin Receptor