Diaryl piperidines as CB1 receptor antagonists

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1278-83. doi: 10.1016/j.bmcl.2009.11.075. Epub 2009 Nov 20.

Abstract

The syntheses and SAR investigations of novel CB(1) receptor antagonists based on a 1,2-diaryl piperidine core have been described. Optimization of this core afforded a compound with robust in vivo potency by reducing food intake in a mouse DIO model.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Diet / adverse effects
  • Eating / drug effects
  • Eating / physiology
  • Mice
  • Mice, Obese
  • Obesity / etiology
  • Obesity / metabolism
  • Piperidines / administration & dosage
  • Piperidines / chemistry*
  • Piperidines / pharmacology*
  • Protein Binding / physiology
  • Receptor, Cannabinoid, CB1 / antagonists & inhibitors*
  • Receptor, Cannabinoid, CB1 / metabolism
  • Structure-Activity Relationship

Substances

  • Piperidines
  • Receptor, Cannabinoid, CB1