| Abstract | Disalicylic acid derivatives with stilbene and bis-styrylbenzene skeleton were synthesized as PTP1B inhibitors. The most potent in this series exhibited a submicromolar IC(50) value. One of the compounds 7b was tested in an animal model for its efficacy as an anti-diabetic or an anti-obesity agent. In feeding compound 7b to diet-induced obese mice, no significant differences in weight gain and food consumption were observed between the drug-treated and the obese control mice. However, 7b significantly lowered the fasting glucose level and improved the glucose tolerance in the obesity-induced diabetic mice. |
| Authors | Suja Shrestha, Bharat Raj Bhattarai, Bhooshan Kafle, Keun-Hyeung Lee, Hyeongjin Cho
(Affiliation: Department of Chemistry and Institute of Molecular Cell Biology, Inha University, Yonghyun-dong, Nam-ku, Incheon 402-751, Republic of Korea.)
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| Journal | Bioorganic & medicinal chemistry
(Bioorg Med Chem)
Vol. 16
Issue 18
Pg. 8643-52
(Sep 15 2008)
ISSN: 1464-3391 England |
| PMID | 18722777
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
|
| Chemical References |
- Anti-Obesity Agents
- Blood Glucose
- Salicylic Acids
- Stilbenes
- Styrenes
- salicylsalicylic acid
|
| Topics |
- Animals
- Anti-Obesity Agents
(chemical synthesis, pharmacology, therapeutic use)
- Blood Glucose
(analysis, metabolism)
- Disease Models, Animal
- Fasting
- Glucose Tolerance Test
- Hyperglycemia
(drug therapy)
- Mice
- Mice, Inbred C57BL
- Mice, Obese
- Obesity
(drug therapy)
- Salicylic Acids
(chemical synthesis, pharmacology, therapeutic use)
- Stilbenes
(chemical synthesis, pharmacology, therapeutic use)
- Structure-Activity Relationship
- Styrenes
(chemical synthesis, pharmacology, therapeutic use)
- Weight Gain
(drug effects)
|
