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[Synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds].

Authors :
Liu WH
Wang SB
Liu Y
Source :
Yao xue xue bao = Acta pharmaceutica Sinica [Yao Xue Xue Bao] 2012 Nov; Vol. 47 (11), pp. 1496-502.
Publication Year :
2012

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 0.3137 to 0.3604 mmol x kg(-1).

Details

Language :
Chinese
ISSN :
0513-4870
Volume :
47
Issue :
11
Database :
MEDLINE
Journal :
Yao xue xue bao = Acta pharmaceutica Sinica
Publication Type :
Academic Journal
Accession number :
23387083