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

Liu, W.-H.; He, D.; Yin, X.-Q.; Liu, Y.

Yao Xue Xue Bao 46(3): 299-304

2011

ISSN/ISBN: 0513-4870
PMID: 21626784
Document Number: 649152
A series of 4-(2-acetoxybenzoylamino) butyrate derivatives were designed and synthesized. All of the novel 12 compounds (7a-7k) were synthesized from gamma-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.

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