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

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

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.

MeSH terms

  • Animals
  • Antitussive Agents / chemical synthesis
  • Antitussive Agents / chemistry*
  • Antitussive Agents / pharmacology*
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Guinea Pigs
  • Humans
  • Ligands
  • Nociceptin Receptor
  • Piperidines / chemical synthesis
  • Piperidines / chemistry*
  • Piperidines / pharmacology*
  • Receptors, Opioid / agonists*
  • Structure-Activity Relationship

Substances

  • Antitussive Agents
  • Ligands
  • Piperidines
  • Receptors, Opioid
  • Nociceptin Receptor