Kumiko Takeuchi,
William G Holloway,
Jamie H McKinzie,
Todd M Suter,
Michael A Statnick,
Peggy L Surface,
Paul J Emmerson,
Elizabeth M Thomas,
Miles G Siegel,
James E Matt, Chad N Wolfe,
Charles H Mitch
[show abstract]
[hide abstract]
ABSTRACT: A structurally unique and new class of opioid receptor antagonists (OpRAs) that bear no structural resemblance with morphine or endogenous opioid peptides has been discovered. A series of carboxamido-biaryl ethers were identified as potent receptor antagonists against mu, kappa and delta opioid receptors. The structure-activity relationship indicated para-substituted aryloxyaryl primary carboxamide bearing an amine tether on the distal phenyl ring was optimal for potent in vitro functional antagonism against three opioid receptor subtypes.
Bioorganic & Medicinal Chemistry Letters 11/2007; 17(19):5349-52. · 2.55 Impact Factor
