Design, synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide derivatives

To explore new agents of γ-aminobutyric acid (GABA) derivatives with more potent antiepileptic activity, a series of 4-(2-acetoxybenzoylamino) butyramide derivatives were designed and synthesized.  All of the novel compounds (5a−5l) were synthesized from GABA as starting material, and their structures were confirmed with IR, ¹H NMR, EI-MS and elemental analysis.  Preliminary pharmacological test in vitro showed that all target compounds displayed strong antiepileptic activities and were worth for further study.  The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyramide derivatives was also discussed preliminarily.