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N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors
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- Sunduru, Naresh (author)
- Umeå universitet,Kemiska institutionen
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- Svensson, Mona (author)
- Umeå universitet,Farmakologi
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- Cipriano, Mariateresa (author)
- Umeå universitet,Farmakologi
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- Svensson, Richard (author)
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- (creator_code:org_t)
- 2017-01-23
- 2017
- English.
- In: Journal of enzyme inhibition and medicinal chemistry (Print). - : Informa UK Limited. - 1475-6366 .- 1475-6374. ; 32:1, s. 513-521
- Journal article (peer-reviewed)
Abstract
Subject headings
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- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Neurovetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Neurosciences (hsv//eng)
Keyword
- Fatty acid amide hydrolase inhibitors
- endocannabinoid system
- oxazolo[4
- 5-b]pyridine anilines
- 1H- idazo[4
- 5-b]pyridine anilines
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- ref (subject category)
- art (subject category)
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