1005202-09-4Relevant academic research and scientific papers
Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3β
Saitoh, Morihisa,Kunitomo, Jun,Kimura, Eiji,Hayase, Yoji,Kobayashi, Hiromi,Uchiyama, Noriko,Kawamoto, Tomohiro,Tanaka, Toshimasa,Mol, Clifford D.,Dougan, Douglas R.,Textor, Garret S.,Snell, Gyorgy P.,Itoh, Fumio
experimental part, p. 2017 - 2029 (2009/05/26)
Glycogen synthase kinase-3β (GSK-3β) is implicated in abnormal hyperphosphorylation of tau protein and its inhibitors are expected to be a promising therapeutic agents for the treatment of Alzheimer's disease. Here we report design, synthesis and structure-activity relationships of a novel series of oxadiazole derivatives as GSK-3β inhibitors. Among these inhibitors, compound 20x showed highly selective and potent GSK-3β inhibitory activity in vitro and its binding mode was determined by obtaining the X-ray co-crystal structure of 20x and GSK-3β.
