药学学报, 2011, 46(3): 299-304
引用本文:
刘文虎 贺 殿 阴新强 刘 毅. 4-(2-乙酰氧基苯甲酰氨基) 丁酸酯类化合物的设计、合成及抗癫痫活性研究[J]. 药学学报, 2011, 46(3): 299-304.
LIU Wen-Hu, He- Dian, Lin-Xin-Jiang, Liu- Yi. Design, synthesis and antiepileptic activity of 4-(2-acetoxybenzoylamino) butyrate derivatives[J]. Acta Pharmaceutica Sinica, 2011, 46(3): 299-304.

4-(2-乙酰氧基苯甲酰氨基) 丁酸酯类化合物的设计、合成及抗癫痫活性研究
刘文虎1, 贺 殿2, 阴新强1, 刘 毅1*
(1. 川北医学院药理教研室, 四川 南充 637000; 2. 兰州大学药学院药物化学研究所, 甘肃 兰州 730000)
摘要:

以中枢抑制性神经递质γ-氨基丁酸 (GABA) 受体调节位点为靶点, GABA (1) 为原料设计合成了12个未见文献报道的4-(2-乙酰氧基苯甲酰氨基) 丁酸及酯类化合物 (7a7k)。目标化合物经IR1H MNREI-MS及元素分析确证了结构。初步体外活性表明, 所合成的化合物具有不同程度的抗癫痫活性, 其中化合物7i7k具有很好的抗癫痫活性, 值得进一步研究, 化合物47d7h显示较好的抗癫痫活性。在此基础上, 初步讨论了该类化合物的构效关系。

关键词:   
Design, synthesis and antiepileptic activity of 4-(2-acetoxybenzoylamino) butyrate derivatives
Abstract:

A series of 4-(2-acetoxybenzoylamino) butyrate derivatives were designed and synthesized.  All of the novel 12 compounds (7a7k) 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 7i7k displayed strong antiepileptic activity and are worth for further development.  Compounds 4, 7d7h showed moderate antiepileptic activity.  The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyrate derivatives is also discussed preliminarily.

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