Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2

Kumiko Takeuchi; William G Holloway; Charles H Mitch; Steven J Quimby; Jamie H McKinzie; Todd M Suter; Michael A Statnick; Peggy L Surface; Paul J Emmerson; Elizabeth M Thomas; Miles G Siegel

doi:10.1016/j.bmcl.2007.10.025

Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6. doi: 10.1016/j.bmcl.2007.10.025. Epub 2007 Oct 17.

Authors

Kumiko Takeuchi¹, William G Holloway, Charles H Mitch, Steven J Quimby, Jamie H McKinzie, Todd M Suter, Michael A Statnick, Peggy L Surface, Paul J Emmerson, Elizabeth M Thomas, Miles G Siegel

Affiliation

¹ Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA.

PMID: 17980586
DOI: 10.1016/j.bmcl.2007.10.025

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-benzo[c]azepin-7-yloxy)nicotinamide scaffold exhibited potent in vitro functional antagonism at all three receptors.

MeSH terms

Acrylic Resins / chemistry
Amides / chemistry*
Carboxylic Acids / chemistry*
Ethers / chemical synthesis
Ethers / chemistry*
Ethers / pharmacology*
Molecular Structure
Narcotic Antagonists*
Receptors, Opioid / metabolism
Structure-Activity Relationship

Substances

Acrylic Resins
Amides
Carboxylic Acids
Ethers
Narcotic Antagonists
Receptors, Opioid
calcium polycarbophil