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…

Index: 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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Citation Number: 121

Abstract

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 ...