Diarylacetylene piperidinyl amides as novel anxiolytics

Bioorg Med Chem Lett. 2006 Jun 1;16(11):3065-7. doi: 10.1016/j.bmcl.2006.02.027. Epub 2006 Mar 31.

Abstract

N-Phenyl-2-[1-[3-(2-pyridinylethynyl)benzoyl]-4-piperidine]acetamide (9) and related piperidine acetamide derivatives have good oral activity in the elevated plus maze, an animal model predictive of clinical efficacy for the treatment of anxiety. Modest affinity was observed for the neurokinin NK-1 and 2 receptors, which are known to be involved in the regulation of mood and emotion.

MeSH terms

  • Acetylene / chemistry*
  • Amides / chemical synthesis
  • Amides / chemistry*
  • Amides / pharmacology*
  • Animals
  • Anti-Anxiety Agents / chemical synthesis*
  • Anti-Anxiety Agents / chemistry
  • Anti-Anxiety Agents / pharmacology*
  • CHO Cells
  • Cricetinae
  • Humans
  • Mice
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Amides
  • Anti-Anxiety Agents
  • Acetylene