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JOURNAL OF CHEMICAL RESEARCH · 2017 · IF 0.646

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

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

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.

研究领域: 药物化学 · 神经生物学 · 有机化学

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JOURNAL OF CHEMICAL RESEARCH · 2016 · IF 0.661

Synthesis, Characterisation and Acetylcholinesterase-Inhibition Activities of 5-benzyl-1,3,4-thiadiazol-2-amine Derivatives

Hui-Long Zhu,Yu-Wei Liu,Wei-Wei Liu,Fu-Jun Yin,Zhi-Ling Cao,Juan Bao,Meng Li,Ling-Yan Qin,Da-Hua Shi

Four 5-benzyl-1,3,4-thiadiazol-2-amine derivatives were synthesised from phenylacetic acid derivatives. The structures of the 5-benzyl-1,3,4-thiadiazole derivatives were characterised by NMR spectroscopy and X-ray crystallography. The acetylcholinesterase-inhibition activities were also tested. Among the four compounds, 5- (4-bromobenzyl)-1,3,4-thiadiazol-2-amine showed the best acetylcholinesterase-inhibition activity with an IC50 of 49.86 μM. The docking study performed with AUTODOCK demonstrated that this compound could interact with the catalytic active site of acetylcholinesterase.

研究领域: 药物化学 · 生物化学 · 结构生物学

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

Synthesis, Characterisation and Acetylcholinesterase-Inhibition Activities of 5-benzyl-1,3,4-thiadiazol-2-amine Derivatives