2-O-Carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity

BR Bhattarai, S Shrestha, SW Ham, KR Kim…

Index: Bhattarai, Bharat Raj; Shrestha, Suja; Ham, Seung Wook; Kim, Kwang Rok; Cheon, Hyae Gyeong; Lee, Keun-Hyeung; Cho, Hyeongjin Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 19 p. 5357 - 5360

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Citation Number: 19

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 ...