| 刘斯婕,赵星,何敬宇,王娟.化学通报,2021,84(9):981-984. |
| 新型2H-噻唑[3,2-b][1,2,4]三嗪-3,7-二酮的超声辅助一锅法合成及乙酰胆碱酯酶抑制活性研究 |
| One-pot Synthesis and Acetylcholinesterase Inhibitory Activities of Novel 2H-thiazole [3,2-b] [1,2,4] triazine-3,7-diones Under Ultrasonic Radiation |
| 投稿时间：2021-03-01 修订日期：2021-03-18 |
| DOI： |
| 中文关键词: 2H-噻唑[3,2-b][1,2,4]三嗪-3,7-二酮 超声辅助 合成 乙酰胆碱酯酶抑制活性 |
| 英文关键词:2H-thiazole[3,2-b][1,2,4]triazine-3,7-diones, Ultrasound assisted, Synthesis, Acetylcholinesterase inhibitory activity |
| 基金项目:河北省自然科学基金项目(H2018106015)，河北省杂环类化合物技术创新中心（SG2021122）资助 |
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| 中文摘要: |
| 以取代苯甲醛、溴乙腈和6-苄基-3-硫代-3,4-二氢-1,2,4-三嗪-5(2H)-酮为起始原料,在超声辅助下,一锅合成了9个新型6-苄基-2-亚苄基-2H-噻唑[3,2-b][1,2,4]三嗪-3,7-二酮类化合物,结构经1H NMR,13C NMR和MS（ESI）表征并对其合成机理进行了初步研究。测试了目标化合物(4a~4i)的体外乙酰胆碱酯酶的抑制活性,其中4a和4d抑制活性最好,有进一步研究的价值。 |
| 英文摘要: |
| Nine novel 6-benzyl-2-benzylidene-2H-thiazole[3,2-b][1,2,4]triazine-3,7-diones were synthesized by substituted benzaldehyde, bromoacetonitrile and 6-benzyl-3-thio-3,4-dihydro-1,2,4-triazine-5(2H)-one in one pot under the assistance of ultrasound. The structures were characterized by 1H NMR, 13C NMR and MS (ESI). The synthesis mechanism was preliminarily studied. The acetylcholinesterase inhibitory activities of compounds (4a~4i) were tested. Compounds 4a and 4d have the best inhibitory activities, which are worthy of further studies. |
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