1289563-91-2Relevant academic research and scientific papers
ALPHA-KETOHETEROCYCLES AND METHODS OF MAKING AND USING
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Page/Page column 110-111, (2012/08/27)
Compounds are disclosed that are effective in inhibition of fatty acid amide hydrolase, an enzyme responsible for catabolism of endogenous cannabinoids such as anandamide. The compounds are useful as analgesic compounds and as sleep-inducing compounds, that can be orally administered, and that can have a relatively long duration of effect. Methods of preparation of the compounds are also provided. The compounds are conformationally constrained analogs of heterocyclylketones such as oxazolylketones.
Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: Orally active, long-acting analgesics
Ezzili, Cyrine,Mileni, Mauro,McGlinchey, Nicholas,Long, Jonathan Z.,Kinsey, Steven G.,Hochstatter, Dustin G.,Stevens, Raymond C.,Lichtman, Aron H.,Cravatt, Benjamin F.,Bilsky, Edward J.,Boger, Dale L.
supporting information; experimental part, p. 2805 - 2822 (2011/06/24)
A series of α-ketooxazoles containing conformational constraints in the C2 acyl side chain of 2 (OL-135) were examined as inhibitors of fatty acid amide hydrolase (FAAH). Only one of the two possible enantiomers displayed potent FAAH inhibition (S vs R en
