2. Academic Validation
  3. Substituted imidazoles as glucagon receptor antagonists

Substituted imidazoles as glucagon receptor antagonists

  • Bioorg Med Chem Lett. 2001 Sep 17;11(18):2549-53. doi: 10.1016/s0960-894x(01)00498-x.
L L Chang 1,  K L Sidler,  M A Cascieri,  S de Laszlo,  G Koch,  B Li,  M MacCoss,  N Mantlo,  S O'Keefe,  M Pang,  A Rolando,  W K Hagmann
Affiliations

Affiliation

  • 1 Department of Medicinal Chemical Research, Merck Research Laboratories, Rahway, NJ 07065, USA. linda_chang@merck.com
PMID: 11549467 DOI: 10.1016/s0960-894x(01)00498-x
Abstract

A modestly active, nonselective triarylimidazole lead was optimized for binding affinity with the human Glucagon Receptor. This led to the identification of a 2- and/or 4-alkyl or alkyloxy substituent on the imidazole C4-aryl group as a structural determinant for significant enhancement in binding with the Glucagon Receptor (e.g., 41, IC(50)=0.053 microM) and selectivity (>1000x) over p38MAP kinase in this class of compounds.

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