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ID: ALA1132135

Journal: Bioorg Med Chem Lett

Title: 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.

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.

CiteXplore: 10201821

DOI: 10.1016/s0960-894x(99)00081-5