Synthesis and evaluation of coumarin/1,2,4-oxadiazole hybrids as selective BChE inhibitors with neuroprotective activity

Juan Zhang School of Biological Science and Technology, University of Jinan , Jinan250022, China; Faculty of Ceilandia, University of Brasília , Brasília72220275, Brazil

Jia-Cheng Li School of Biological Science and Technology, University of Jinan , Jinan250022, China

Jia-Li Song School of Biological Science and Technology, University of Jinan , Jinan250022, China

Zhi-Qiang Cheng School of Biological Science and Technology, University of Jinan , Jinan250022, China

Ji-Zheng Sun School of Life Science, Taishan Medical University , Taian271016, ChinaCorrespondence[email protected]

Cheng-Shi Jiang School of Biological Science and Technology, University of Jinan , Jinan250022, ChinaCorrespondence[email protected]

https://orcid.org/0000-0002-2760-7596

Abstract

A series of new coumarin/1,2,4-oxadiazole hybrids were synthesized and evaluated for cholinesterase inhibitory and neuroprotective activities. Among them, enantiomers 5u and 5v showed potent hBChE inhibitory activity with IC₅₀ values of 8.17 and 9.56 μM, respectively, and also exhibited good selectivity for hBChE over hAChE by 9.49- and 7.58-fold, respectively. In addition, both compounds could protect SH-SY5Y cells against Aβ_25–35-induced neurotoxicity. The preliminary bioassay results provided a new chemotype for multifunctional anti-Alzheimer’s disease agents and continuing investigation into compounds 5u and 5v is warranted.

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Synthesis and evaluation of coumarin/1,2,4-oxadiazole hybrids as selective BChE inhibitors with neuroprotective activity

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Synthesis and evaluation of coumarin/1,2,4-oxadiazole hybrids as selective BChE inhibitors with neuroprotective activity

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