Design, synthesis and antiepileptic activity of 4-(2-acetoxybenzoylamino) butyrate derivatives

A series of 4-(2-acetoxybenzoylamino) butyrate derivatives were designed and synthesized.  All of the novel 12 compounds (7a−7k) were synthesized from γ-aminobutyric acid (1) as starting material, and their structures were confirmed with IR, ¹H NMR, EI-MS and elemental analysis.  Preliminary pharmacological test in vitro showed that most of these title compounds possessed antiepileptic activity.  Compounds 7i−7k displayed strong antiepileptic activity and are worth for further development.  Compounds 4, 7d−7h showed moderate antiepileptic activity.  The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyrate derivatives is also discussed preliminarily.