1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor

Authors :: Martyn C. Coldwell
Jeffrey C. Jerman
Wai N. Chan
Phillip Jeffrey
Roderick A. Porter
Amanda Johns
Widdowson Katherine L
Nigel E. Austin
F Jewitt
Darren Smart
Steven Coulton
Michael S. Hadley
Stephen J. Brough
Source :: Bioorganic & Medicinal Chemistry Letters. 11:1907-1910
Publication Year :: 2001
Publisher :: Elsevier BV, 2001.
Abstract: This communication reports SARs for the first orexin-1 receptor antagonist series of 1-aryl-3-quinolin-4-yl and 1-aryl-3-naphthyridin-4-yl ureas. One of these compounds, 31 (SB-334867), has excellent selectivity for the orexin-1 receptor, blood-brain barrier permeability and shows in vivo activity following ip dosing.

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