Synthesis, characterisation and acetylcholinesterase-inhibition activities of 5-benzyl-1, 3, 4-thiadiazol-2-amine derivatives. (1st January 2016)

• Record Type: Journal Article
• Authors: Zhu, Hui-Long; Liu, Yu-Wei; Liu, Wei-Wei; Yin, Fu-Jun; Cao, Zhi-Ling; Bao, Juan; Li, Meng; Qin, Ling-Yan; Shi, Da-Hua
• Is Part Of: Journal of chemical research. Volume 40:Number 1(2016)
• Page Start: 16
• Page End: 20
• Publication Date: 2016-01-01
• Subjects: Chemistry -- Research -- Periodicals; Chemistry -- Periodicals; 540.5
• DOI: 10.3184/174751916X14494964318204
• Languages: English
• ISSNs: 1747-5198

Abstract

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.