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

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 acetylcholinester...

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Bibliographic Details
Published in:Journal of chemical research 2017-11, Vol.41 (11), p.664-667
Main Authors: Shi, Da-Hua, Zhu, Hui-Long, Liu, Yu-Wei, Tang, Zong-Ming, Lu, Chen, Ma, Xiao-Dong, Song, Xiao-Kai, Liu, Wei-Wei, Dong, Tong, Song, Meng-Qiu
Format: Article
Language:English
Subjects:
Crystals
Derivatives
Diffraction
Docking
NMR
Nuclear magnetic resonance
Phenylacetic acid
Single crystals
Thiadiazoles
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Summary: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.
ISSN:1747-5198
2047-6507
DOI:10.3184/174751917X15094552081242