Derivatives of 1,4-bis(3-hydroxycarbonyl-4-hydroxyl)styrylbenzene as PTP1B inhibitors with hypoglycemic activity

PTP1B inhibitor with hypoglycemic activity. 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...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2008-09, Vol.16 (18), p.8643-8652
Hauptverfasser: Shrestha, Suja, Bhattarai, Bharat Raj, Kafle, Bhooshan, Lee, Keun-Hyeung, Cho, Hyeongjin
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Sprache:eng
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Zusammenfassung:PTP1B inhibitor with hypoglycemic activity. 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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2008.07.090