Potent, orally absorbed glucagon receptor antagonists

  • Bioorg Med Chem Lett. 1999 Mar 8;9(5):641-6. doi: 10.1016/s0960-894x(99)00081-5.
S E de Laszlo  1 ,  C Hacker ,  B Li ,  D Kim ,  M MacCoss ,  N Mantlo ,  J V Pivnichny ,  L Colwell ,  G E Koch ,  M A Cascieri ,  W K Hagmann
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
PMID: 10201821 DOI: 10.1016/s0960-894x(99)00081-5
Abstract

The SAR of 2-pyridyl-3,5-diaryl pyrroles, ligands of the human Glucagon Receptor and inhibitors of p38 kinase, were investigated. This effort resulted in the identification of 2-(4-pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)pyrr ole 49 (L-168,049), a potent (Kb = 25 nM), selective antagonist of glucagon.

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