Synthesis, antiepileptic effects, and structure-activity relationships of α-asarone derivatives: In vitro and in vivo neuroprotective effect of selected derivatives

BIOORGANIC CHEMISTRY(2021)

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摘要
•In the present study, we compared the antiepileptic effects of α-asarone derivatives to explore their structure-activity relationships using the PTZ-induced seizure model.•Our research revealed that electron-donating methoxy groups in the 3,4,5-position on phenyl ring increased antiepileptic potency but the placement of other groups at different positions decreased activity.•Besides, in allyl moiety, the optimal activity was reached with either an allyl or a 1-butenyl group in conjugation with the benzene ring.•5 and 19 exerted better neuroprotective effects against epilepsy in vitro(cell) and in vivo(mouse) models.
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关键词
Structure-activity relationships, alpha-asarone, Epilepsy, PTZ
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