Design, synthesis, and biological evaluation of novel Nav1.2 inhibitors as antiepileptic agents

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12 Nov 2026 0 comments

Voltage-gated sodium channel Nav1.2 is a validated target for anticonvulsant therapy, yet Nav1.2 inhibitors remain scarce. To explore the unexplored N-4 position of the [1,2,4]triazolo[1,5-a]pyrimidine scaffold, we designed and synthesized two series of novel derivatives bearing diverse substituents at this position. Their Nav1.2 inhibitory activities were evaluated using FLIPR membrane potential and whole-cell patch-clamp assays, while their anticonvulsant efficacy and neurotoxicity were...