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ID: ALA1137434
Journal: Bioorg Med Chem Lett
Title: 2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity.
Authors: Bhattarai BR, Shrestha S, Ham SW, Kim KR, Cheon HG, Lee KH, Cho H.
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 K(i) value of 1.1 microM 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.
CiteXplore: 17728130