Potent, orally absorbed glucagon receptor antagonists

Authors
de Laszlo, SE Hacker, C Li, B Kim, D MacCoss, M Mantlo, N Pivnichny, JV Colwell, L Koch, GE Cascieri, MA Hagmann, WK
Citation
Se. De Laszlo et al., Potent, orally absorbed glucagon receptor antagonists, BIOORG MED, 9(5), 1999, pp. 641-646
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
5
Year of publication
1999
Pages
641 - 646
Database
ISI
SICI code
0960-894X(19990308)9:5<641:POAGRA>2.0.ZU;2-5
Abstract
The SAR of 2-pyridyl-3,5-diaryl pyrroles, ligands of the human glucagon rec eptor and inhibitors of p38 kinase, were investigated. This effort resulted in the identification of 2-(4-pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-pro pyloxyphenyl)pyrrole 49 (L-168,049), a potent (Kb = 25 nM), selective antag onist of glucagon. (C) 1999 Elsevier Science Ltd. All rights reserved.