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

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.

• Authors: Amy Timmons, Mark Seierstad, Rich Apodaca, Matt Epperson, Dan Pippel, Sean Brown, Leon Chang, Brian Scott, Michael Webb, Sandra R Chaplan, J Guy Breitenbucher
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 18 Issue 6 Pg. 2109-13 (Mar 15 2008) ISSN: 1464-3405 [Electronic] England
• PMID: 18289847 (Publication Type: Journal Article)

Chemical References

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

Topics

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