Title of article
2-O-Carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity
Author/Authors
Bharat Raj Bhattarai، نويسنده , , Suja Shrestha، نويسنده , , Seung Wook Ham، نويسنده , , Kwang Rok Kim، نويسنده , , Hyae Gyeong Cheon، نويسنده , , Keun-Hyeung Lee، نويسنده , , Hyeongjin Cho، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
5357
To page
5360
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 Ki value of 1.1 μM 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.
Keywords
2-O-Carboxymethylpyrogallol , PTP1B inhibitor , Diabetes , glucose tolerance , Hyperglycemia , protein tyrosine phosphatase
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798613
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