【摘要】 前期研究发现,4-(2-乙酰氧基苯甲酰氨基)丁酰胺类化合物具有较好的抗癫痫活性。据此,本文以中枢γ-氨基丁酸受体(γ-aminobutyric acid receptor,GABAR)为靶点,设计合成了系列全新结构的4-(2-乙酰氧基苯甲酰氨基)丁酰胺基杂环类化合物(5a～5n),希望完善此类化合物的构效关系及提高其抗癫痫活性。化合物结构经1H MNR、ESI-MS及元素分析确证。体内药效筛选结果表明,化合物5f、5i～5n对4-AP致癫痫小鼠具有良好抗癫痫活性(ED50值为0.313 7～0.360 4 mmol.kg 1)。更多还原

【Abstract】 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.更多还原