Potent, orally absorbed glucagon receptor antagonists.
1999
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)pyrrole 49 (L-168,049), a potent (Kb = 25 nM), selective antagonist of glucagon.
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