2. Academic Validation
  3. Potent, orally absorbed glucagon receptor antagonists

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

Affiliation

  • 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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