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Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH).


ABSTRACT: The synthesis and structure-activity relationships (SAR) of a series of benzothiophene piperazine and piperidine urea FAAH inhibitors is described. These compounds inhibit FAAH by covalently modifying the enzyme's active site serine nucleophile. Activity-based protein profiling (ABPP) revealed that these urea inhibitors were completely selective for FAAH relative to other mammalian serine hydrolases. Several compounds showed in vivo activity in a rat complete Freund's adjuvant (CFA) model of inflammatory pain.

SUBMITTER: Johnson DS 

PROVIDER: S-EPMC3150822 | BioStudies | 2009-01-01

REPOSITORIES: biostudies

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