N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors

作者：Sunduru Naresh; Svensson Mona; Cipriano Mariateresa; Marwaha Sania; Andersson C David; Svensson Richard; Fowler Christopher J; Elofsson Mikael^*

来源：Journal of Enzyme Inhibition and Medicinal Chemistry, 2017, 32(1): 513-521.

DOI：10.1080/14756366.2016.1265520

• Fatty acid amide hydrolase inhibitors
• endocannabinoid system
• oxazolo[4,5-b]pyridine anilines
• 1H-imidazo[4,5-b]pyridine anilines

Fatty acid amide hydrolase (FAAH) is a promising target for the development of drugs to treat neurological diseases. In search of new FAAH inhibitors, we identified 2-(4-cyclohexylphenoxy)-N-(3-(oxazolo[4,5-b] pyri-din-2-yl) phenyl) acetamide, 4g, with an IC50 of 2.6 mu M as a chemical starting point for the development of potent FAAH inhibitors. Preliminary hit-to-lead optimisation resulted in 2-(4-phenylphenoxy)-N-(3-(oxazolo[4,5-b] pyridin-2-yl)phenyl) acetamide, 4i, with an IC50 of 0.35 mu M.

• 出版日期2017