Objective：This study aims to synthesize multifunctional neuroprotective agent with antioxidant and γ-aminobutyric acid （GABA） activity and test their neuroprotective activity against stroke. Methods：The edaravone analogues were synthesized from phenols with distinct substitutes；the antioxidant activity was determined by 1，1-diphenyl-2-picryhydrazyl （DPPH） free radical scavenging activity；the GABA activity was evaluated by patch clamp，and the neuroprotective effect of the compounds was tested by MCAO model in rats. Results：The 3′，5′-Diisopropyl-4′-hydroxyedaravone（6a）and 3′-methyl-5′-tert-butyl-4′-hydroxy- edaravone（6b）were successfully synthesized，both compounds showed good in vitro antioxidant activity and stronger neuroprotection than edaravone on the MCAO model；electrophysiological experiments showed that compound 6b hod GABA enhancement activity at low concentration and direct GABAR agonistic activity at high concentration. Conclusion：Based on the molecular framework of edaravone，two new neuroprotecting agents with both antioxidant activity and GABA activity were successfully constructed.