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  • Title: Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.
    Author: Gustin DJ, Ma Z, Min X, Li Y, Hedberg C, Guimaraes C, Porter AC, Lindstrom M, Lester-Zeiner D, Xu G, Carlson TJ, Xiao S, Meleza C, Connors R, Wang Z, Kayser F.
    Journal: Bioorg Med Chem Lett; 2011 Apr 15; 21(8):2492-6. PubMed ID: 21392988.
    Abstract:
    Starting 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.
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