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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PTPlB抑制剂，设计、合成了一系列含3，4-二氢-2（1H）-喹啉酮结构的新型查尔酮衍生物，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（E）-6-{4-[3-（4-氯苯基）-3-氧代-1-丙烯基]苄氧基}-3，4-二氢-2（1／4）-喹啉酮（4e）和（E）-6-{4-[3-（3-溴苯基）-3-氧代-1-丙烯基]苄氧基}-3，4-二氢-2（1H）-喹啉酮（4i）活性最佳，IC50分别为（4．64±0.381和（4．36±0．41）μmol/L.
英文摘要：
Protein tyrosine phosphatase 1B （PTP1B） has recently been identified as new drug target for type II diabetes and obesity due to it is a negative regulator of the insulin and leptin-signaling pathway. In order to find new nonphosphonate-based pTyr mimetics, a series of novel chalcone derivatives bearing the 3,4-dihydroquinolin-2（1/4）-one moieties （4a-4n） were designed, synthesized, and evaluated for their PTP1B inhibitory activity. The results demonstrated that all compounds presented potent inhibitory activities against PTP 1 B, among which compounds 4e and 4i exhibited most potent with IC50 value of （4.64 ± 0.38） and （4.36 ± 0.41） μmol/L, respectively.
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