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Bioorg. Med. Chem. Lett. · Apr 2011
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.
- Darin J Gustin, Zhihua Ma, Xiaoshan Min, Yihong Li, Christine Hedberg, Cris Guimaraes, Amy C Porter, Michelle Lindstrom, Dianna Lester-Zeiner, Guifen Xu, Timothy J Carlson, Shouhua Xiao, Cesar Meleza, Richard Connors, Zhulun Wang, and Frank Kayser.
- Department of Chemistry, Amgen Inc., South San Francisco, 1120 Veterans Blvd., South San Francisco, CA 94080, USA. dgustin@amgen.com
- Bioorg. Med. Chem. Lett. 2011 Apr 15; 21 (8): 2492-6.
AbstractStarting from a series of ureas that were determined to be mechanism-based inhibitors of FAAH, several spirocyclic ureas and lactams were designed and synthesized. These efforts identified a series of novel, noncovalent FAAH inhibitors with in vitro potency comparable to known covalent FAAH inhibitors. The mechanism of action for these compounds was determined through a combination of SAR and co-crystallography with rat FAAH.Copyright © 2011 Elsevier Ltd. All rights reserved.
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