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Design, synthesis and evaluation of malonic acid-based PTP1B inhibitors
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- Author:
- No author available
- Journal Title:
- Acta Pharmaceutica Sinica
- Issue:
- 3
- DOI:
- No doi available
- Key Word:
- PTPIB抑制剂;磷酸酪氨酸模拟物;丙二酸洐生物
Abstract： 蛋白酪氨酸磷酸酶(protein tyrosine phosphatase,PTP) 1B是治疗2型糖尿病(T2DM)及肥胖症的潜在靶点.磷酸酪氨酸(pTyr)是PTP1B去磷酸化作用的底物,本文以丙二酸基团模拟pTyr分子中的磷酸酯,设计合成了丙二酸类PTP1B抑制剂1～7.抑酶活性评价显示,化合物3和4对人重组PTP1B的半数抑制浓度IC50分别为7.66和1.88 μtmol·L-1.
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