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Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2
Authors:Takeuchi Kumiko  Holloway William G  Mitch Charles H  Quimby Steven J  McKinzie Jamie H  Suter Todd M  Statnick Michael A  Surface Peggy L  Emmerson Paul J  Thomas Elizabeth M  Siegel Miles G
Institution:

aLilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA

Abstract:A series of 6-bicycloaryloxynicotinamides were identified as opioid receptor antagonists at mu, kappa, and delta receptors. Compounds in the 6-(2,3,4,5-tetrahydro-1H-benzoc]azepin-7-yloxy)nicotinamide scaffold exhibited potent in vitro functional antagonism at all three receptors.
Keywords:Opioid receptor antagonists (OpRAs)  Carboxamido-biaryl ethers  Obesity
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