2. Academic Validation
  3. 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor

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

Affiliation

  • 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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