2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2011 Nov 1;21(21):6538-44. doi: 10.1016/j.bmcl.2011.08.055.
Marvin J Meyers 1,  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
Affiliations

Affiliation

  • 1 Pfizer Global Research & Development, St. Louis Laboratories, 700 Chesterfield Parkway West, Chesterfield, MO 63017, United States. mmeyers8@slu.edu
PMID: 21924614 DOI: 10.1016/j.bmcl.2011.08.055
Abstract

Herein we report the identification of two new fatty acid amide hydrolase (FAAH) inhibitor lead series with FAAH k(inact)/K(i) potency values greater than 1500M(-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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