为了寻找新型γ-氨基丁酸(γ-aminobutyric acid,GABA)类抗癫痫药物,以抑制性神经递质γ-氨基丁酸受体(GABAR)为作用靶点,以GABA为原料设计合成了一类全新结构类型的4-(2-乙酰氧基苯甲酰氨基)丁酰胺类化合物(5a～5l),通过IR、1H MNR、EI-MS及元素分析确证了目标化合物的结构。初步药理活性评价结果表明,目标化合物具有良好抗癫痫活性,值得进一步研究,在此基础上,初步讨论了该类化合物的构效关系。 In order to find out a new type of GABA antiepileptic drugs, targeting GABAR, an inhibitory neurotransmitter, GABA The structures of the target compounds were confirmed by IR, 1H MNR, EI-MS and elemental analysis. The structures of 4- (2-acetoxybenzamido) butanamides (5a ~ 5l) Preliminary pharmacological activity evaluation results show that the target compound has good anti-epileptic activity, worthy of further study, on this basis, preliminary study of the structure-activity relationship of these compounds.