Bioorganic and Medicinal Chemistry Letters p. 6538 - 6544 (2011)
Update date:2022-07-29
Topics:
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
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-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 and selectivity for additional medicinal chemistry optimization.
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