Trifluoromethyl ketone inhibitors of fatty acid amide hydrolase: a probe of structural and conformational features contributing to inhibition

…, H Sato, AE Lerner, BJ Austin, JE Patterson…

文献索引：Boger, Dale L.; Sato, Haruhiko; Lerner, Aaron E.; Austin, Bryce J.; Patterson, Jean E.; Patricelli, Matthew P.; Cravatt, Benjamin F. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 2 p. 265 - 270

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被引用次数: 121

摘要

The examination of a series of trifluoromethyl ketone inhibitors of Fatty Acid Amide Hydrolase (FAAH, oleamide hydrolase, anandamide amidohydrolase) is detailed in efforts that define structural and conformational properties that contribute to enzyme inhibition and substrate binding. The results imply an extended bound conformation, highlight a role for the presence, position, and stereochemistry of a Δ9. 10cis double bond, and suggest little ...