Objective: To synthesize multifunctional neuroprotective agent with antioxidant and 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 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: 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 shows GABA enhancement activity at low concentration and direct GABAR agonistic activity at high concentration. Conclusion: Based on the molecular framework of edaravone, we have successfully constructed two new neuroprotecting agents with both antioxidant activity and GABA activity.