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目的合成具有新型结构的系列溴酚衍生物,测试其体外蛋白酪氨酸磷脂酶1B(PTP1B)抑制活性并初步探讨其构效关系。方法以香草醛或3,4-二羟基苯甲醛为原料,经溴化、还原、醚化等反应制得目标化合物。借助重组人源PTP1B蛋白水解底物p NPP的方法,测定目标物对PTP1B的抑制活性。结果合成了18个溴酚衍生物,其结构经EI-MS、ESI-MS、~1H-NMR、~(13)C-NMR谱确证。结论目标化合物的PTP1B抑制活性与化合物中溴原子的数目、位置以及烷基链的长度有关;化合物6c体外PTP1B抑制活性最好(IC50=0.572μmol·L~(-1))。
OBJECTIVE: To synthesize a series of bromophenol derivatives with novel structure to test their in vitro activity of protein tyrosine phospholipase 1B (PTP1B) and to explore its structure-activity relationship. Methods Vanillin or 3,4-dihydroxybenzaldehyde as raw materials, the bromination, reduction, etherification reaction of the target compound. The inhibitory activity of the target substance against PTP1B was determined by means of recombinant human PTP1B proteolytic substrate p NPP. Results Eighteen bromophenol derivatives were synthesized and their structures were confirmed by EI-MS, ESI-MS, ~ 1H-NMR and ~ (13) C-NMR. Conclusion The PTP1B inhibitory activity of the target compound is related to the number and position of bromine atoms in the compound and the length of the alkyl chain. Compound 6c has the best PTP1B inhibitory activity (IC50 = 0.572μmol·L -1) in vitro.