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 …

…, RE Tenbrink, J McDonald, SE Smith, S Foltin…

Index: Meyers, Marvin J.; Long, Scott A.; Pelc, Matthew J.; Wang, Jane L.; Bowen, Scott J.; Walker, Mark C.; Schweitzer, Barbara A.; Madsen, Heather M.; Tenbrink, Ruth E.; McDonald, Joseph; Smith, Sarah E.; Foltin, Susan; Beidler, David; Thorarensen, Atli Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 21 p. 6538 - 6544

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Citation Number: 15

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 1500M− 1s− 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 ...