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ID: ALA2396573
Journal: Bioorg Med Chem Lett
Title: Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors.
Authors: Chun K, Park JS, Lee HC, Kim YH, Ye IH, Kim KJ, Ku IW, Noh MY, Cho GW, Kim H, Kim SH, Kim J.
Abstract: New potent glycogen synthase kinase-3 (GSK-3) inhibitors, 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives, were designed by modeling, synthesized and evaluated in vitro. Compound 17c showed good potency in enzyme and cell-based assays (IC50=111 nM, EC50=1.78 μM). Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.
CiteXplore: 23683591