N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitorsShow others and affiliations
2017 (English)In: Journal of enzyme inhibition and medicinal chemistry (Print), ISSN 1475-6366, E-ISSN 1475-6374, Vol. 32, no 1, p. 513-521Article in journal (Refereed) Published
Abstract [en]
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.
Place, publisher, year, edition, pages
2017. Vol. 32, no 1, p. 513-521
Keywords [en]
Fatty acid amide hydrolase inhibitors, endocannabinoid system, oxazolo[4, 5-b]pyridine anilines, 1H- idazo[4, 5-b]pyridine anilines
National Category
Medicinal Chemistry Neurosciences
Identifiers
URN: urn:nbn:se:umu:diva-131874DOI: 10.1080/14756366.2016.1265520ISI: 000392591100045PubMedID: 28114819Scopus ID: 2-s2.0-85013857480OAI: oai:DiVA.org:umu-131874DiVA, id: diva2:1076970
2017-02-242017-02-242023-03-23Bibliographically approved