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

2- O-Carboxymethylpyrogallol derivatives were synthesized, with their in vitro inhibitory activities against PTP1B and in vivo antihyperglycemic effects examined. When compound 14 was fed to a high-fat diet-induced diabetic mouse model, significant improvements were observed in both the fasting gluc...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2007-10, Vol.17 (19), p.5357-5360
Hauptverfasser: Bhattarai, Bharat Raj, Shrestha, Suja, Ham, Seung Wook, Kim, Kwang Rok, Cheon, Hyae Gyeong, Lee, Keun-Hyeung, Cho, Hyeongjin
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Sprache:eng
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Zusammenfassung:2- O-Carboxymethylpyrogallol derivatives were synthesized, with their in vitro inhibitory activities against PTP1B and in vivo antihyperglycemic effects examined. 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. 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 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.08.019