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Paper | Regular issue | Vol 100, No. 8, 2020, pp.1163-1171
Published online, 5th June, 2020
DOI: 10.3987/COM-20-14266
Preparation and Acetylcholinesterase Inhibitory Activities of Pyridine-Based 1,3,4-Oxadiazole Derivatives

Xiang Yu,* Wude Yang, Ling Huang, Xingji Zhou, and Yafang Chen*

*Department of Pharmacy, Guizhou University of Traditional Chinese Medicne, , China

Abstract

Fourteen pyridine-based 1,3,4-oxadiazole derivatives were synthesized from pyridine-2-carboxaldehyde via iodine-mediated oxidative cyclisation with substituted hydrazide by using the impregnation method. Their structures were confirmed by melting point, 1H NMR, 13C NMR and HRMS. Preliminary bioassay of these derivatives' activities inhibiting acetylcholinesterase (AChE) was also evaluated in vitro at the concentration of 1 μmol/mL. The result showed that compounds 4c, 4j and 4k had moderate inhibitory activities with 52%, 59% and 59%, respectively. The preliminary structure-activity relationships revealed that the introduction of pyridine ring could enhance the activity. Molecular docking study demonstrated that compound 4k possessed an optimal docking pose with interactions at the middle of the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE.