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

…, S Coulton, A Johns, MS Hadley, K Widdowson…

Index: Porter, Roderick A; Chan, Wai N; Coulton, Steven; Johns, Amanda; Hadley, Michael S; Widdowson, Katherine; Jerman, Jeffrey C; Brough, Stephen J; Coldwell, Martyn; Smart, Darren; Jewitt, Frances; Jeffrey, Phillip; Austin, Nigel Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 14 p. 1907 - 1910

Full Text: HTML

Citation Number: 116

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.

Related Articles:

Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: possible confounding effects on in vivo and in vitro studies

[McElhinny Jr., Charles J.; Lewin, Anita H.; Mascarella, S. Wayne; Runyon, Scott; Brieaddy, Lawrence; Carroll, F. Ivy Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 21 p. 6661 - 6664]

Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: possible confounding effects on in vivo and in vitro studies

[McElhinny Jr., Charles J.; Lewin, Anita H.; Mascarella, S. Wayne; Runyon, Scott; Brieaddy, Lawrence; Carroll, F. Ivy Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 21 p. 6661 - 6664]

More Articles...