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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
- 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
- Author
- 김승현
- Keywords
- Glycogen synthase kinase-3; GSK-3 inhibitor; 8-Amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives
- Issue Date
- 2013-07
- Publisher
- Elsevier Science B.V., Amsterdam.
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 권: 23, 호: 13, 페이지: 3983-3987
- 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. (c) 2013 Elsevier Ltd. All rights reserved.
- URI
- https://www.sciencedirect.com/science/article/pii/S0960894X13004472?via%3Dihubhttp://hdl.handle.net/20.500.11754/45569
- ISSN
- 0960-894X
- Appears in Collections:
- COLLEGE OF MEDICINE[S](의과대학) > MEDICINE(의학과) > Articles
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