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2-O-Carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity
- Authors
- Bhattarai, Bharat Raj; Shresthaa, Suja; Ham, Seung Wook; Kim, Kwang Rok; Cheon, Hyae Gyeong; Lee, Keun-Hyeung; Cho, Hyeongjin
- Issue Date
- Oct-2007
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- 2-O-carboxymethylpyrogallol; PTP1B inhibitor; diabetes; glucose tolerance; hyperglycemia; protein tyrosine phosphatase
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.17, no.19, pp 5357 - 5360
- Pages
- 4
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 17
- Number
- 19
- Start Page
- 5357
- End Page
- 5360
- ISSN
- 0960-894X
1464-3405
- Abstract
- 2-O-Carboxymethylpyrogallol derivatives (4-17) were synthesized, with their in vitro inhibitory activities against PTP1B and in vivo antihyperglycemic effects examined. Compound 14, the most potent among the series, showed a K-i value of 1.1 mu M against PTP1B, 7-fold lower than that against TC-PTP. When compound 14 was fed to a high-fat diet-induced diabetic mouse model, significant improvements were observed in both the fasting glucose level and glucose tolerance. (C) 2007 Elsevier Ltd. All rights reserved.
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