Methylenedisalicylic acid derivatives: New PTP1B inhibitors that confer resistance to diet-induced obesity
Compound 8 inhibited PTP1B in vitro and suppressed diet-induced weight gain in mice. 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 6.3 μM aga...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2007-05, Vol.17 (10), p.2760-2764 |
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Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | Compound
8 inhibited PTP1B in vitro and suppressed diet-induced weight gain in mice.
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 6.3
μM 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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2007.02.069 |