期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 8, 页码 2492-2496出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.02.052
关键词
FAAH; FAAH inhibitor; Noncovalent; Structure based design
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. (C) 2011 Elsevier Ltd. All rights reserved.
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