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Journal of Asian Natural Products Research Volume 21, 2019 - Issue 11
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Original Articles

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]
ORCID Iconhttps://orcid.org/0000-0002-2760-7596
ORCID Icon
Pages 1090-1103 | Received 14 May 2018, Accepted 20 Jun 2018, Published online: 10 Jul 2018
 
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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 Aβ25–35-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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