Discovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists

Abstract

A novel series of thiophene-containing biaryl amide glucagon receptor (GCGR) antagonists were designed and synthesized. Two compounds of this series, 14f and 14h, exhibited good GCGR binding (IC₅₀ = 6.1 μM and 4.4 μM, respectively) and cAMP functional activities (IC₅₀ = 4.4 μM and 14.4 μM, respectively). The possible binding modes of compounds 14f and 14h with GCGR were explored by molecular simulation.

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A series of novel thiophene-containing biary amide analogs were designed, synthesized, and their activity profiled. Two compounds, 14f and 14h, exhibited sound GCGR binding with IC50 values of 6.1 μM and 4.4 μM, respectively, and displayed good cAMP functional activities (IC50 = 4.4 μM and 14.4 μM, respectively).

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