Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators.

Basic Information

ID: ALA1153645

Journal: Bioorg Med Chem Lett

Title: Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators.

Authors: Ishikawa M, Nonoshita K, Ogino Y, Nagae Y, Tsukahara D, Hosaka H, Maruki H, Ohyama S, Yoshimoto R, Sasaki K, Nagata Y, Eiki J, Nishimura T.

Abstract: The synthesis and structure-activity-relationships (SARs) of novel 2-(pyridine-2-yl)-1H-benzimidazole glucokinase activators are described. Systematic modification of benzimidazole lead 5a identified from a high-throughput screening led to the discovery of a potent and metabolically stable glucokinase activator 16p(R) with greater structural diversity from GKAs reported to date. The compound also demonstrated acute oral glucose lowering efficacy in rat OGTT model.

CiteXplore: 19540111

DOI: 10.1016/j.bmcl.2009.05.038

Patent ID: