کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1366694 981600 2007 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Methylenedisalicylic acid derivatives: New PTP1B inhibitors that confer resistance to diet-induced obesity
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Methylenedisalicylic acid derivatives: New PTP1B inhibitors that confer resistance to diet-induced obesity
چکیده انگلیسی

Methylenedisalicylic acid derivatives were synthesized and their inhibitory activities against protein tyrosine phosphatases (PTPases) examined. Two of the compounds, 8 and 9, showed Ki 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.

Compound 8 inhibited PTP1B in vitro and suppressed diet-induced weight gain in mice.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 10, 15 May 2007, Pages 2760–2764
نویسندگان
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