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ID: ALA1134731

Journal: Bioorg Med Chem Lett

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

Authors: Porter RA, Chan WN, Coulton S, Johns A, Hadley MS, Widdowson K, Jerman JC, Brough SJ, Coldwell M, Smart D, Jewitt F, Jeffrey P, Austin N.

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.

CiteXplore: 11459658

DOI: 10.1016/s0960-894x(01)00343-2