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蛋白酪氨酸磷酸酶1B(PTP1B)是治疗2型糖尿病和肥胖症的新靶点.根据已报道的磷酸酪氨酸拟似物类PTP1B抑制剂A,通过计算机药物辅助设计,经Negishi偶联、亚磺酰亚胺烯醇式不对称加成及Dess-Martin氧化等11步反应成功合成了一个结构新颖的PTP1B抑制剂1,其对体外人重组PTP1B的半抑制浓度为54.17μmol?L-1.
Protein tyrosine phosphatase 1B (PTP1B) is a new target for the treatment of type 2 diabetes and obesity.According to the reported phosphotyrosine analogue PTP1B inhibitor A, , Sulfoximinol asymmetric addition and Dess-Martin oxidation and other 11 steps successfully synthesized a novel PTP1B inhibitor 1, its in vitro human recombinant PTP1B half-inhibitory concentration of 54.17μmol? L- 1.