title: Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
abstract: 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.
authors.affiliation: Department of Chemical Research-CV & CNS, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. ginny.ho@spcorp.com
authors.forename: Ginny D
authors.initials: GD
authors.lastname: Ho
authors.forename: Ana
authors.initials: A
authors.lastname: Bercovici
authors.forename: Deen
authors.initials: D
authors.lastname: Tulshian
authors.forename: William J
authors.initials: WJ
authors.lastname: Greenlee
authors.forename: Ahmad
authors.initials: A
authors.lastname: Fawzi
authors.forename: Xiomara
authors.initials: X
authors.lastname: Fernandez
authors.forename: Robbie L
authors.initials: RL
authors.lastname: McLeod
authors.forename: April
authors.initials: A
authors.lastname: Smith Torhan
authors.forename: Hongtao
authors.initials: H
authors.lastname: Zhang
mesh_terms: 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
chemical_list: D000996:Antitussive Agents; D008024:Ligands; D010880:Piperidines; D011957:Receptors, Opioid; D000094942:Nociceptin Receptor