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Synthesis and Evaluation of 5-Benzyl-1,3,4-Thiadiazole Derivatives as Acetylcholinesterase Inhibitors

Journal 2017 · IF 0.646 · 发表于 2017 年 11 月 1 日
作者: Da-Hua Shi,Hui-Long Zhu,Yu-Wei Liu,Zong-Ming Tang,Chen Lu,Xiao-Dong Ma,Xiao-Kai Song,Wei-Wei Liu,Tong Dong,Meng-Qiu Song
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摘要

Three novel 5-benzyl-1,3,4-thiadiazole derivatives were synthesised starting from phenylacetic acid derivatives. These compounds were characterised by NMR, HRMS and single-crystal X-ray diffraction analysis. 2-Pyrrolidyl-5-[2-(4-bromophenyl)methyl]-1,3,4-thiadiazole showed moderate acetylcholinesterase-inhibition activity with a 50% inhibitory concentration value of 33.16 μM. 2-Pyrrolidyl-5-[2-(4-bromophenyl)methyl]-1,3,4-thiadiazole and acetylcholinesterase docking was demonstrated using the Molecular Operating Environment program.