944745-89-5Relevant articles and documents
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.
Fused imidazoheterocyclic compounds and pharmaceutical compositions
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, (2008/06/13)
Imidazoheterocyclic compounds having the formula: STR1 wherein the A ring is pyridine in any of its four positions; B is carbonyl, thioxomethyl or hydroxymethylene; Z is hydrogen, halogen, loweralkyl, hydroxy, loweralkoxy, diloweralkylamino or nitro; Ar i