2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity.

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Bhattarai BR, Shrestha S, Ham SW, Kim KR, Cheon HG, Lee KH, Cho H

2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity.

Bioorg Med Chem Lett. 2007 Oct 1;17(19):5357-60. Epub 2007 Aug 15.

PubMed ID

17728130 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
2-(Oxalyl-Amino)-4,5,6,7-Tetrahydro-Thieno[2,3-C]Pyridine-3-Carboxylic Acid	Tyrosine-protein phosphatase non-receptor type 1	IC 50 (nM)	500000	N/A	N/A	Details