Back to Search
Start Over
[Synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds].
- 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).
- Subjects :
- 4-Aminopyridine
Amides administration & dosage
Amides chemistry
Amides therapeutic use
Animals
Anticonvulsants administration & dosage
Anticonvulsants chemistry
Anticonvulsants therapeutic use
Dose-Response Relationship, Drug
Epilepsy chemically induced
Epilepsy drug therapy
Female
Lethal Dose 50
Male
Mice
Molecular Structure
Random Allocation
Receptors, GABA metabolism
Structure-Activity Relationship
Amides chemical synthesis
Anticonvulsants chemical synthesis
Subjects
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