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

This communication reports SARs for the first orexin-1 receptor antagonist series of 1-aryl-3-quifiolin-4-yl and 1-aryl-3-naphthyridin-4-yl ureas. One of these compounds, 31 (5B-334867), has excellent selectivity for the orexin-1 receptor, blood-brain barrier permeability and shows in vivo activity following ip dosing. (C) 2001 Elsevier Science Ltd. All rights reserved.