title: N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors.
abstract: 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]pyridin-2-yl)phenyl)acetamide, 4g, with an IC50of 2.6 µM 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 IC50of 0.35 µM.
authors.affiliation: a Department of Chemistry , Umeå University , Umeå , Sweden.
authors.forename: Naresh
authors.initials: N
authors.lastname: Sunduru
authors.affiliation: b Department of Pharmacology and Clinical Neuroscience , Umeå University , Umeå , Sweden.
authors.forename: Mona
authors.initials: M
authors.lastname: Svensson
authors.affiliation: b Department of Pharmacology and Clinical Neuroscience , Umeå University , Umeå , Sweden.
authors.forename: Mariateresa
authors.initials: M
authors.lastname: Cipriano
authors.affiliation: a Department of Chemistry , Umeå University , Umeå , Sweden.
authors.forename: Sania
authors.initials: S
authors.lastname: Marwaha
authors.affiliation: a Department of Chemistry , Umeå University , Umeå , Sweden.
authors.forename: C David
authors.initials: CD
authors.lastname: Andersson
authors.affiliation: c Department of Pharmacy, Uppsala Drug Optimization and Pharmaceutical Profiling platform (UDOPP) , Uppsala University , Uppsala , Sweden.
authors.forename: Richard
authors.initials: R
authors.lastname: Svensson
authors.affiliation: b Department of Pharmacology and Clinical Neuroscience , Umeå University , Umeå , Sweden.
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Fowler
authors.affiliation: a Department of Chemistry , Umeå University , Umeå , Sweden.
authors.forename: Mikael
authors.initials: M
authors.lastname: Elofsson
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000581:Amidohydrolases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats; D013329:Structure-Activity Relationship; D000099252:Fatty Acid Amide Hydrolases
chemical_list: D000081:Acetamides; D000581:Amidohydrolases; D004791:Enzyme Inhibitors; D000099252:Fatty Acid Amide Hydrolases
keywords: 1H-imidazo[4,5-b]pyridine anilines; Fatty acid amide hydrolase inhibitors; endocannabinoid system; oxazolo[4,5-b]pyridine anilines