| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370456 | Bioorganic & Medicinal Chemistry Letters | 2011 | 7 Pages |
Abstract
Herein we report the identification of two new fatty acid amide hydrolase (FAAH) inhibitor lead series with FAAH kinact/Ki potency values greater than 1500 M−1 s−1. The two novel spirocyclic cores, 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane, clearly distinguished themselves from the other spirocyclic cores on the basis of their superior potency for FAAH. Lead compounds from these two series have suitable FAAH potency and selectivity for additional medicinal chemistry optimization.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
![Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 1: Identification of 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane as lead scaffolds](/preview/png/1370456.png "First Page Preview: Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 1: Identification of 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane as lead scaffolds")
Authors
Marvin J. Meyers, Scott A. Long, Matthew J. Pelc, Jane L. Wang, Scott J. Bowen, Mark C. Walker, Barbara A. Schweitzer, Heather M. Madsen, Ruth E. Tenbrink, Joseph McDonald, Sarah E. Smith, Susan Foltin, David Beidler, Atli Thorarensen,