Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.

作者信息

Ho Ginny D, Bercovici Ana, Tulshian Deen, Greenlee William J, Fawzi Ahmad, Fernandez Xiomara, McLeod Robbie L, Smith Torhan April, Zhang Hongtao

机构信息

Department of Chemical Research-CV & CNS, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.

出版信息

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. doi: 10.1016/j.bmcl.2007.03.062. Epub 2007 Mar 21.

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.