Synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds

It has been demonstrated by our previous research that 4-(2-acetoxybenzoylamino) butyramide derivatives exhibited good antiepileptic activities.  In this paper, to explore the SAR and improve the antiepileptic activities of these derivatives, a series of novel 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds (5a−5n) were synthesized and biologically evaluated.  Their structures were confirmed by ¹H MNR, ESI-MS and elemental analysis.  Pharmacological test in vivo showed that target compounds (5f, 5i−5n) displayed strong antiepileptic activities on 4-AP induced epilepsy in mice with ED₅₀ values ranging from 0.313 7 to 0.360 4 mmol·kg⁻¹.