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

Basic Information

ID: ALA3860064

Journal: Bioorg Med Chem

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

Authors: Galal SA, Khattab M, Andreadaki F, Chrysina ED, Praly JP, Ragab FAF, El Diwani HI.

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.

CiteXplore: 27624527

DOI: 10.1016/j.bmc.2016.08.069

Patent ID: ┄