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Issue 5, 2019
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Synthesis and biological evaluation of 2,2-dimethylbenzopyran derivatives as potent neuroprotection agents

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Abstract

The development of novel neuroprotection agents is of great significance for the treatment of ischemic stroke. In this study, a series of compounds comprising 2,2-dimethylbenzopyran groups and cinnamic acid groups have been synthesized. Preferential combination principles and bioisostere that improved the neuroprotective effect of the compounds were identified for this series via biological activity assay in vitro. Meanwhile, a functional reversal group of the acrylamide amide resulted in the most active compounds. Among them, BN-07 significantly improved the morphology of neurons and obviously increased cell survival rate of primary neurons induced by oxygen glucose deprivation (OGD), superior to clinically used anti-ischemic stroke drug edaravone (Eda). Overall, our findings may provide an alternative strategy for the design of novel anti-ischemic stroke agents with more potency than Eda.

Graphical abstract: Synthesis and biological evaluation of 2,2-dimethylbenzopyran derivatives as potent neuroprotection agents

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Supplementary files

Article information


Submitted
20 Dec 2018
Accepted
14 Jan 2019
First published
21 Jan 2019

This article is Open Access

RSC Adv., 2019,9, 2498-2508
Article type
Paper

Synthesis and biological evaluation of 2,2-dimethylbenzopyran derivatives as potent neuroprotection agents

F. Du, Q. Zhou, X. Fu, Y. Shi, Y. Chen, W. Fang, J. Yang and G. Chen, RSC Adv., 2019, 9, 2498
DOI: 10.1039/C8RA10424G

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    [Original citation] - Published by The Royal Society of Chemistry.

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