Methylenedisalicylic acid derivatives: new PTP1B inhibitors that confer resistance to diet-induced obesity.

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Shrestha S, Bhattarai BR, Chang KJ, Lee KH, Cho H

Methylenedisalicylic acid derivatives: new PTP1B inhibitors that confer resistance to diet-induced obesity.

Bioorg Med Chem Lett. 2007 May 15;17(10):2760-4. Epub 2007 Mar 3.

PubMed ID

17368023 [ View in PubMed

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Abstract

Methylenedisalicylic acid derivatives were synthesized and their inhibitory activities against protein tyrosine phosphatases (PTPases) examined. Two of the compounds, 8 and 9, showed K(i) values of 9.4 and 6.3microM against PTP1B, 4- and 7-fold lower values compared to those against TC-PTP. They were reversible and slow-binding inhibitors against PTP1B. When compound 8 was fed to a mouse model, the weight gain and adipocyte fat storage induced by a high-fat-diet were significantly suppressed.

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	Ki (nM)	11500	N/A	N/A	Details
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