Synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1496-1502, 2012.
Article
in Chinese
| WPRIM
| ID: wpr-274632
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).
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Structure-Activity Relationship
/
Molecular Structure
/
Random Allocation
/
4-Aminopyridine
/
Chemistry
/
Receptors, GABA
/
Therapeutic Uses
/
Dose-Response Relationship, Drug
/
Drug Therapy
/
Epilepsy
Limits:
Animals
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2012
Type:
Article
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