Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties

Bioorg Med Chem Lett. 2009 Jan 1;19(1):31-5. doi: 10.1016/j.bmcl.2008.11.026. Epub 2008 Nov 13.

Abstract

A series of alpha-amidosulfones were found to be potent and selective agonists of CB(2). The discovery, synthesis, and structure-activity relationships of this series of agonists are reported. In addition, the pharmacokinetic properties of the most promising compounds are profiled.

MeSH terms

  • Amides / chemistry
  • Amides / pharmacology
  • Animals
  • Humans
  • Microsomes, Liver
  • Pharmacokinetics
  • Rats
  • Receptor, Cannabinoid, CB2 / agonists*
  • Structure-Activity Relationship
  • Sulfones / chemistry*
  • Sulfones / pharmacology

Substances

  • Amides
  • Receptor, Cannabinoid, CB2
  • Sulfones