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Thiazolidinedione derivatives as PTP1B inhibitors with antihyperglycemic and antiobesity effects
- Authors
- Bhattarai, Bharat Raj; Kafle, Bhooshan; Hwang, Ji-Sun; Khadka, Deegendra; Lee, Sun-Myung; Kang, Jae-Seung; Ham, Seung Wook; Han, Inn-Oc; Park, Hwangseo; Cho, Hyeongjin
- Issue Date
- Nov-2009
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- PTP1B inhibitor; Thiazolidinedione; Obesity; Diabetes; Glitazones
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.19, no.21, pp 6161 - 6165
- Pages
- 5
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 19
- Number
- 21
- Start Page
- 6161
- End Page
- 6165
- ISSN
- 0960-894X
1464-3405
- Abstract
- Benzylidene-2,4-thiazolidinedione derivatives with substitutions on the phenyl ring at the ortho or para positions of the thiazolidinedione (TZD) group were synthesized as PTP1B inhibitors with IC50 values in a low micromolar range. Compound 3e, the lowest, bore an IC50 of 5.0 mu M. In vivo efficacy of 3e as an antiobesity and hypoglycemic agent was evaluated in a mouse model system. Significant improvement of glucose tolerance was observed. This compound also significantly suppressed weight gain and significantly improved blood parameters such as TG, total cholesterol and NEFA. Compound 3e was also found to activate peroxisome proliferator-activated receptors (PPARs) indicating multiple mechanisms of action. (c) 2009 Elsevier Ltd. All rights reserved.
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