Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH)

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2109-13. doi: 10.1016/j.bmcl.2008.01.091. Epub 2008 Jan 30.

Abstract

Efforts to improve the properties of the well studied ketooxazole FAAH inhibitor OL-135 resulted in the discovery of a novel propylpiperidine series of FAAH inhibitors that has a modular design and superior properties to OL-135. The efficacy of one of these compounds was demonstrated in a rat spinal nerve ligation model of neuropathic pain in rats.

MeSH terms

  • Amidohydrolases / antagonists & inhibitors*
  • Amidohydrolases / metabolism
  • Animals
  • Binding Sites
  • Humans
  • Oxazoles / chemical synthesis
  • Oxazoles / chemistry
  • Oxazoles / pharmacology*
  • Pain / drug therapy*
  • Pain / enzymology*
  • Pain Measurement / drug effects*
  • Pyridines / pharmacology
  • Rats
  • Spinal Nerves / drug effects*
  • Spinal Nerves / injuries
  • Structure-Activity Relationship

Substances

  • 1-oxo-1-(5-(2-pyridyl)-2-yl)-7-phenylheptane
  • Oxazoles
  • Pyridines
  • Amidohydrolases
  • fatty-acid amide hydrolase