新型1,2,4-三嗪衍生物的合成、表征及生物活性

Synthesis,characterization and bioactivities of novel 1,2,4-triazine derivatives

以苯并咪唑-1-乙酰肼和不同取代的溴代苯乙酮为原料,合成出了9个新型的含苯并咪唑环的1,2,4-三嗪衍生物,并利用IR、1HNMR和元素分析对所合成的目标化合物结构进行了表征。对目标化合物进行了抗癌、抗糖尿病活性筛选,生物活性实验结果表明,大部分目标化合物对Cdc25B磷酸酯酶具有较强的抑制活性,抑制率在58%～93%,目标化合物3-[(2-苯氧甲基)苯并咪唑-1-亚甲基]-6-(4-甲氧基苯基)-1,2,4-三嗪和3-[(2-苯氧甲基)苯并咪唑-1-亚甲基]-6-联苯基-1,2,4-三嗪对PTP1B具有较高的抑制活性,抑制率分别为59.99%和87.47%。这表明,目标化合物可作为潜在的抗癌和抗糖尿病试剂。

Nine novel 1,2,4-triazine derivatives bearing benz- imidazole moiety have been synthesized by condensation of 2- aryloxymethylbenzimidazole-l-acetylhydrazines with various substituted phenacyl bromides. The structures were confirmed by IR, ~HNMR spectra and elemental analysis. These com- pounds were screened based on anticancer and anti-diabetic activities. The results indicated that most compounds exhibited high activities against Cdc25B phosphatase with the inhibitory rate in the range of 58% -93% ,and compounds 3-[ （2-phe- noxymethyl） benzimidazole-l-methylene ] -6-（ 4-methoxylphe- nyl） -1,2, 4-triazine and 3-[ （ 2-phenoxymethyl ） benzimid- azole-l-methylene ] -6-biphenyl-1, 2,4-triazine showed high activities against PTP1B with the inhibitory rate 59.99% and 87.47% ,respectively. The target compounds could be used as potential anti-cancer and anti-diabetes reagents.