| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373933 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
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.
Graphical abstractThe synthesis and SAR of a series of benzothiophene piperazine and piperidine urea FAAH inhibitors is described.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Douglas S. Johnson, Kay Ahn, Suzanne Kesten, Scott E. Lazerwith, Yuntao Song, Mark Morris, Lorraine Fay, Tracy Gregory, Cory Stiff, James B. Dunbar Jr., Marya Liimatta, David Beidler, Sarah Smith, Tyzoon K. Nomanbhoy, Benjamin F. Cravatt,