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

  • Bioorg Med Chem Lett. 2001 Jul 23;11(14):1907-10. doi: 10.1016/s0960-894x(01)00343-2.
R A Porter  1 ,  W N Chan ,  S Coulton ,  A Johns ,  M S Hadley ,  K Widdowson ,  J C Jerman ,  S J Brough ,  M Coldwell ,  D Smart ,  F Jewitt ,  P Jeffrey ,  N Austin
Affiliations
  • 1. GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park North, Third Avenue, Harlow, CM19 5AW, Essex, UK. [email protected]
PMID: 11459658 DOI: 10.1016/s0960-894x(01)00343-2
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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