Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596574 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Seung-Chul Lee, Hyun Tae Kim, Choul-Hong Park, Do Young Lee, Ho-Jin Chang, Soobong Park, Joong Myung Cho, Sunggu Ro, Young-Ger Suh,