Reversible Competitive α-Ketoheterocycle Inhibitors of Fatty Acid Amide Hydrolase Containing Additional Conformational Constraints in the Acyl Side Chain: Orally Active, Long Acting Analgesics

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 enantiomer), and their potency is comparable or...

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Main Authors: 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.
Formato: Artigo
Idioma:Inglês
Publicado: 2011
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC3085948/
https://ncbi.nlm.nih.gov/pubmed/21428410
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm101597x
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