N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors |
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| Authors: | Naresh Sunduru Mona Svensson Mariateresa Cipriano Sania Marwaha C David Andersson Richard Svensson |
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| Institution: | 1. Department of Chemistry, Ume? University, Ume?, Sweden;2. Department of Pharmacology and Clinical Neuroscience, Ume? University, Ume?, Sweden;3. Department of Pharmacy, Uppsala Drug Optimization and Pharmaceutical Profiling platform (UDOPP), Uppsala University, Uppsala, Sweden |
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| 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-(oxazolo4,5-b]pyridin-2-yl)phenyl)acetamide, 4g, with an IC50 of 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-(oxazolo4,5-b]pyridin-2-yl)phenyl)acetamide, 4i, with an IC50 of 0.35?µM. |
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| Keywords: | Fatty acid amide hydrolase inhibitors endocannabinoid system oxazolo[4 5-b]pyridine anilines 1H-imidazo[4 5-b]pyridine anilines |
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