1217232-97-7Relevant 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
scheme or table, 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.
