乙酰胆碱酯酶抑制剂3,6-二芳基-7H-噻唑并[3,2-b]-1,2,4-三嗪-7-酮类化合物的设计、合成与生物活性

目的 初步探讨乙酰胆碱酯酶(AChE)抑制剂7H-噻唑并3,2-b]-1,2,4-三嗪-7-酮类化合物的合成及构效关系.方法 利用分子对接技术设计一些新的7H-噻唑并3,2-b]-1,2,4-三嗪-7-酮类化合物,采用化学方法合成这些目标化合物,采用Ellman法对目标化合物进行体外乙酰胆碱酯酶抑制活性筛选.首先由...

Design, synthesis and biological activity of 3,6-diaryl- 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives as acetylcholinesterase inhibitors

Based on our previous work that 6-arylmethyl-7H-thiazolo3,2-b]-1,2,4-triazin-7-ones derivatives inhibiting acetylcholinesterase(AChE) activity,in order to study on the influence of the different groups and side chains on the 7H-thiazolo3,2-b]-1,2,4-triazin-7-one scaffold on the AChE inhibitory activity and the active sites of AChE,eleven 3,6-diaryl-7H-thiazolo-3,2-b]-1,2,4-triazin-7-one derivatives were designed using molecular docking and synthesized.The synthetic routes of the target compounds were as ...