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在微波辐射下,利用2-芳氧甲基苯并咪唑-1-乙酰肼(3)与各种(未)取代的溴代苯乙酮进行缩合,合成出了20个新的含苯并咪唑单元的3,6-二取代-1,2,4-三嗪衍生物4,并利用1H NMR,IR和元素分析对所合成的目标化合物进行了结构表征.探索出了最佳合成条件.与经典方法相比较,该合成方法具有反应时间短、操作简便、底物范围广、易纯化、产率较高等优点.对所合成的目标化合物进行了Cdc25B和PTP1B抑制活性的筛选.实验结果表明,目标化合物4g和4j对Cdc25B表现出良好的抑制活性,目标化合物4a,4h,4j,4r和4s对PTP1B表现出良好的抑制活性.值得注意的是,目标化合物4j可作为用于治疗癌症和糖尿病的潜在的Cdc25B和PTP1B抑制剂.
Under microwave irradiation, 20 novel benzimidazoles were synthesized by condensation of 2-aryloxymethylbenzimidazole-1-acetic acid hydrazide (3) with various (un) substituted bromoacetophenones Units of 3,6-disubstituted-1,2,4-triazine derivatives 4, and the use of 1H NMR, IR and elemental analysis of the structure of the target compounds were synthesized to explore the best synthetic conditions and Compared with the classical method, this method has the advantages of short reaction time, simple operation, wide range of substrates, easy purification and high yield, etc. The target compounds were screened for their inhibitory activity against Cdc25B and PTP1B.The results showed that The target compounds 4g and 4j showed good inhibitory activity against Cdc25B, and the target compounds 4a, 4h, 4j, 4r and 4s showed good inhibitory activity against PTP1 B. It is noteworthy that the target compound 4j can be used as a medicament for the treatment of cancer and diabetes Of potential Cdc25B and PTP1B inhibitors.