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中文摘要：
蛋白酪氨酸磷酸酶1B（PTP1B）作为胰岛素和瘦素信号转导通路的负调节因子,已成为治疗糖尿病和肥胖症的潜在靶标.为了寻找非磷酸酯类PTP1B抑制剂,设计、合成了一系列（E）-1-取代苯基-3-[4-（（E）-（2-（4-苯基噻唑-2-基）腙）甲基）苯基]-2-丙烯-1-酮（4a～4n）,并对化合物进行了PTP1B抑制活性测定.结果显示,所有化合物对PTP1B均显示出较强的抑制活性,其中化合物4h活性最佳,IC50为（2.57±0.50）μmol L-1.
英文摘要：
Abstract Protein tyrosine phosphatase 1B （PTP1B） has recently been identified as new drug target for type II diabetes and obesity due to that it is a negative regulator of the insulin and leptin-signaling pathway. In order to find new nonphospho- nate-based pTyr mimetics, a series of novel （E）-1-phenyl-3-（4-（（E）-（2-（4-phenyl-thiazol-2-yl）hydrazono）methyl）phenyl）- prop-2-en-l-one （4a-4n） were designed, synthesized, and evaluated for their PTP1B inhibitory activity. The results demon- strated that all compounds presented potent inhibitory activities against PTP1B, among which compound 4h exhibited most potent with IC50 value of （2.57 ±0.50） μmol·L^-1.
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