944746-01-4Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel imidazopyridines as potential antidiabetic GSK3β inhibitors
Lee, Seung-Chul,Kim, Hyun Tae,Park, Choul-Hong,Lee, Do Young,Chang, Ho-Jin,Park, Soobong,Cho, Joong Myung,Ro, Sunggu,Suh, Young-Ger
, p. 4221 - 4224 (2012/07/17)
Design, synthesis and biological evaluation of the imidazopyridine analogs as novel GSK3β inhibitors for treatment of type 2 diabetes mellitus are described. Most of the analogs exhibited excellent inhibitory activities (IC50 44 nM) against glycogen synthase kinase 3β (GSK3β). The structure-activity relationship (SAR) of the imidazopyridine analogs and the binding mode of analog 23 in the catalytic domain of GSK3β, based on our X-ray crystallography study, are described. In particular, analog 28, which was selected as a potential drug candidate for treatment of type 2 diabetes mellitus, exhibited excellent GSK3β inhibition, pharmacokinetic profiles and blood glucose lowering effect in mouse.
IMIDAZOPYRIDINE DERIVATIVES INHIBITING PROTEIN KINASE ACTIVITY, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
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Page/Page column 101-102, (2008/06/13)
The inventive imidazopyridine derivative can be used in a pharmaceutical composition for preventing or treating diseases such as diabetes, obesity, dementia, cancer, and inflammation, since it can efficiently inhibit the activities of several protein kina
