Citation: Zhang Chenglu, Li Chuanyin, Gu Yaodong, Sun Xiaona, Tang Jie, Wang Jing, Li Yizheng, Wang Huayu. Synthesis and Bioactivity Evaluation of Novel 1, 3, 5-Triazine-1H-pyrazole-triazol-ethiadiazole Derivatives[J]. Chinese Journal of Organic Chemistry, ;2018, 38(5): 1223-1232. doi: 10.6023/cjoc201704028 shu

Synthesis and Bioactivity Evaluation of Novel 1, 3, 5-Triazine-1H-pyrazole-triazol-ethiadiazole Derivatives

College of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian 116029

Corresponding author: Zhang Chenglu, zhangchenglu@lnnu.edu.cn
Received Date: 17 April 2017
Revised Date: 28 June 2017
Available Online: 3 May 2018
Fund Project: Project supported by the Science and Technology Research Program of Liaoning Provincial Department of Education (No. 2009A426)the Science and Technology Research Program of Liaoning Provincial Department of Education 2009A426

Figures(3)

Twenty-one novel 1, 3, 5-triazine-1H-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, ¹H NMR and HRMS. The inhibitory activities of 21 novel target products against Cdc25B and PTP1B are evaluated. As a result, most of the target compounds exhibit excellent inhibitory activities. In the Cdc25B inhibitory activity test, 14 target compounds have higher inhibitory activities than the positive reference sodium orthovanadate, and they are expected to be potential of Cdc25B inhibitors. In the PTP1B inhibitory activity test, 9 target compounds have better inhibitory activities than the control oleanolic acid, and they are expected to be potential of PTP1B inhibitors.
- pyrazole,
- 1, 3, 5-triazine,
- triazolothiadiazole,
- Cdc25B inhibitor,
- PTP1B inhibitor
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