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

Bharat Raj Bhattarai; Suja Shrestha; Seung Wook Ham; Kwang Rok Kim; Hyae Gyeong Cheon; Keun Hyeung Lee; Hyeongjin Cho

doi:10.1016/j.bmcl.2007.08.019

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

Bharat Raj Bhattarai, Suja Shrestha, Seung Wook Ham, Kwang Rok Kim, Hyae Gyeong Cheon, Keun Hyeung Lee, Hyeongjin Cho

Research output: Contribution to journal › Article › peer-review

17 Scopus citations

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 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.

Original language	English
Pages (from-to)	5357-5360
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	19
DOIs	https://doi.org/10.1016/j.bmcl.2007.08.019
State	Published - 1 Oct 2007

Bibliographical note

Funding Information:
This work was supported by a Grant (C00344) from the basic research program of the Korean Research Foundation. B. R. Bhattarai was a recipient of a BK21 fellowship.

Keywords

2-O-Carboxymethylpyrogallol
Diabetes
Glucose tolerance
Hyperglycemia
PTP1B inhibitor
Protein tyrosine phosphatase

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2007.08.019

Cite this

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title = "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 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 fasting glucose level and glucose tolerance.",

keywords = "2-O-Carboxymethylpyrogallol, Diabetes, Glucose tolerance, Hyperglycemia, PTP1B inhibitor, Protein tyrosine phosphatase",

author = "Bhattarai, {Bharat Raj} and Suja Shrestha and Ham, {Seung Wook} and Kim, {Kwang Rok} and Cheon, {Hyae Gyeong} and Lee, {Keun Hyeung} and Hyeongjin Cho",

note = "Funding Information: This work was supported by a Grant (C00344) from the basic research program of the Korean Research Foundation. B. R. Bhattarai was a recipient of a BK21 fellowship. ",

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T1 - 2-O-Carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity

AU - Bhattarai, Bharat Raj

AU - Shrestha, Suja

AU - Ham, Seung Wook

AU - Kim, Kwang Rok

AU - Cheon, Hyae Gyeong

AU - Lee, Keun Hyeung

AU - Cho, Hyeongjin

N1 - Funding Information: This work was supported by a Grant (C00344) from the basic research program of the Korean Research Foundation. B. R. Bhattarai was a recipient of a BK21 fellowship.

PY - 2007/10/1

Y1 - 2007/10/1

N2 - 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 fasting glucose level and glucose tolerance.

AB - 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 fasting glucose level and glucose tolerance.

KW - 2-O-Carboxymethylpyrogallol

KW - Diabetes

KW - Glucose tolerance

KW - Hyperglycemia

KW - PTP1B inhibitor

KW - Protein tyrosine phosphatase

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 19

ER -

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

Abstract

Bibliographical note

Keywords

UN SDGs

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