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
Citation
Ra. Porter et al., 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor, BIOORG MED, 11(14), 2001, pp. 1907-1910
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
14
Year of publication
2001
Pages
1907 - 1910
Database
ISI
SICI code
0960-894X(20010723)11:14<1907:1ASNAO>2.0.ZU;2-2
Abstract
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 orex in-1 receptor, blood-brain barrier permeability and shows in vivo activity following ip dosing. (C) 2001 Elsevier Science Ltd. All rights reserved.