Synthesis of (benzimidazol-2-yl)aniline derivatives as glycogen phosphorylase inhibitors

Add time:08/23/2019    Source:sciencedirect.com

A series of (benzimidazol-2-yl)-aniline (1) derivatives has been synthesized and evaluated as glycogen phosphorylase (GP) inhibitors. Kinetics studies revealed that compounds displaying a lateral heterocyclic residue with several heteroatoms (series 3 and 5) exhibited modest inhibitory properties with IC50 values in the 400–600 μM range. Arylsulfonyl derivatives 7 (Ar: phenyl) and 9 (Ar: o-nitrophenyl) of 1 exhibited the highest activity (series 2) among the studied compounds (IC50 324 μM and 357 μM, respectively) with stronger effect than the p-tolyl analogue 8.

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