Derivatives of 1,4-bis(3-hydroxycarbonyl-4-hydroxyl)styrylbenzene as PTP1B inhibitors with hypoglycemic activity. Bioorganic & medicinal chemistry [Bioorg Med Chem] Journal article

Title	Derivatives of 1,4-bis(3-hydroxycarbonyl-4-hydroxyl)styrylbenzene as PTP1B inhibitors with hypoglycemic activity.
Author(s)	Shrestha S, Bhattarai BR, Kafle B, Lee KH, Cho H
Institution	Department of Chemistry and Institute of Molecular Cell Biology, Inha University, Yonghyun-dong, Nam-ku, Incheon 402-751, Republic of Korea.
Source	Bioorg Med Chem 2008 Sep 15; 16(18):8643-52.
MeSH	Animals Anti-Obesity Agents Blood Glucose Disease Models, Animal Fasting Glucose Tolerance Test Hyperglycemia Mice Mice, Inbred C57BL Mice, Obese Obesity Salicylic Acids Stilbenes Structure-Activity Relationship Styrenes Weight Gain
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.
Language	eng
Pub Type(s)	Journal Article Research Support, Non-U.S. Gov't
PubMed ID	18722777

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