Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
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.
Takeuchi
Kumiko
K
Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA.
Holloway
William G
WG
Mitch
Charles H
CH
Quimby
Steven J
SJ
McKinzie
Jamie H
JH
Suter
Todd M
TM
Statnick
Michael A
MA
Surface
Peggy L
PL
Emmerson
Paul J
PJ
Thomas
Elizabeth M
EM
Siegel
Miles G
MG
D000180:Acrylic Resins / Q000737:chemistry; D000577:Amides / Q000737:chemistry*; D002264:Carboxylic Acids / Q000737:chemistry*; D004987:Ethers / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D009292:Narcotic Antagonists; D011957:Receptors, Opioid / Q000378:metabolism; D013329:Structure-Activity Relationship
D000180:Acrylic Resins; D000577:Amides; D002264:Carboxylic Acids; D004987:Ethers; D009292:Narcotic Antagonists; D011957:Receptors, Opioid; C030312:calcium polycarbophil