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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, 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
- Issue Date
- Jul-2013
- Publisher
- Pergamon Press Ltd.
- Keywords
- Glycogen synthase kinase-3; GSK-3 inhibitor; 8-Amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives
- Citation
- Bioorganic & Medicinal Chemistry Letters, v.23, no.13, pp 3983 - 3987
- Pages
- 5
- Indexed
- SCI
SCIE
SCOPUS
- Journal Title
- Bioorganic & Medicinal Chemistry Letters
- Volume
- 23
- Number
- 13
- Start Page
- 3983
- End Page
- 3987
- ISSN
- 0960-894X
1464-3405
- 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 mu M). Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.
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Related Researcher
- Kim, Seung Hyun
- 서울 의과대학 (DEPARTMENT OF NEUROLOGY)