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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

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

doi

10.1016/j.bmcl.2007.08.019

subject

Has Abstract

pub_date

2007-10-01 00:00:00

pages

5357-60

issue

19

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00941-9

journal_volume

17

pub_type

杂志文章

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