新型1,3,5-三嗪-1H-吡唑-三唑并噻二唑衍生物的合成及活性评价
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摘要
以具有优秀药理活性的吡唑杂环为核心,连接1,3,5-三嗪杂环,引入三唑并噻二唑稠并环,设计合成了21个新型1,3,5-三嗪-1H-吡唑-三唑并噻二唑衍生物.应用IR,1H NMR和HRMS等对21种新物质进行了结构表征.评价了21种新型目标产物对Cdc25B和PTP1B的抑制活性,结果发现,大部分目标分子显示了优良的抑制活性.在Cdc25B抑制活性测试中,14个目标分子抑制活性高于阳性参照物Na3VO4,有望成为潜在的Cdc25B抑制剂,在PTP1B抑制活性测试中,9个目标分子抑制活性优于阳性参照物齐墩果酸,有望成为潜在的PTP1B抑制剂.
Twenty-one novel 1,3,5-triazine-1 H-pyrazole-triazolethiadiazole derivatives are designed and synthesized,in which the excellent pharmacological activitive pyrazole is used as key skeleton by connecting 1,3,5-triazine and introducing triazolothiadiazole.The structures of 21 target compounds are characterized by IR,1 H NMR and HRMS.The inhibitory activities of 21 novel target products against Cdc25 B and PTP1 B are evaluated.As a result,most of the target compounds exhibit excellent inhibitory activities.In the Cdc25 B inhibitory activity test,14 target compounds have higher inhibitory activities than the positive reference sodium orthovanadate,and they are expected to be potential of Cdc25 B inhibitors.In the PTP1 B inhibitory activity test,9 target compounds have better inhibitory activities than the control oleanolic acid,and they are expected to be potential of PTP1 B inhibitors.
Twenty-one novel 1,3,5-triazine-1 H-pyrazole-triazolethiadiazole derivatives are designed and synthesized,in which the excellent pharmacological activitive pyrazole is used as key skeleton by connecting 1,3,5-triazine and introducing triazolothiadiazole.The structures of 21 target compounds are characterized by IR,1 H NMR and HRMS.The inhibitory activities of 21 novel target products against Cdc25 B and PTP1 B are evaluated.As a result,most of the target compounds exhibit excellent inhibitory activities.In the Cdc25 B inhibitory activity test,14 target compounds have higher inhibitory activities than the positive reference sodium orthovanadate,and they are expected to be potential of Cdc25 B inhibitors.In the PTP1 B inhibitory activity test,9 target compounds have better inhibitory activities than the control oleanolic acid,and they are expected to be potential of PTP1 B inhibitors.
引文
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[33]Wang,X.M.S.Thesis,Liaoning Normal University,Dalian,2015(in Chinese).(王雪,硕士论文,辽宁师范大学,大连,2015.)
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