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

K Chun, JS Park, HC Lee, YH Kim, IH Ye, KJ Kim…

Index: Chun, Kwangwoo; Park, Ji-Seon; Lee, Han-Chang; Kim, Young-Ha; Ye, In-Hea; Kim, Kang-Jeon; Ku, Il-Whea; Noh, Min-Young; Cho, Goang-Won; Kim, Heejaung; Kim, Seung Hyun; Kim, Jeongmin Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 13 p. 3983 - 3987

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Citation Number: 3

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= 111nM, EC50= 1.78 μM). Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.