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  • Title: Synthesis of (benzimidazol-2-yl)aniline derivatives as glycogen phosphorylase inhibitors.
    Author: Galal SA, Khattab M, Andreadaki F, Chrysina ED, Praly JP, Ragab FAF, El Diwani HI.
    Journal: Bioorg Med Chem; 2016 Nov 01; 24(21):5423-5430. PubMed ID: 27624527.
    Abstract:
    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 400-600μM range. Arylsulfonyl derivatives 7 (Ar: phenyl) and 9 (Ar: o-nitrophenyl) of 1 exhibited the highest activity (series 2) among the studied compounds (IC50 324μM and 357μM, respectively) with stronger effect than the p-tolyl analogue 8.
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