Synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds.
- Author:
Wen-Hu LIU
1
;
Shi-Bao WANG
;
Yi LIU
Author Information
1. Department of Pharmacology, North Sichuan Medical College, Nanchong 637007, China. lwh790214@163.com
- Publication Type:Journal Article
- MeSH:
4-Aminopyridine;
Amides;
administration & dosage;
chemical synthesis;
chemistry;
therapeutic use;
Animals;
Anticonvulsants;
administration & dosage;
chemical synthesis;
chemistry;
therapeutic use;
Dose-Response Relationship, Drug;
Epilepsy;
chemically induced;
drug therapy;
Female;
Lethal Dose 50;
Male;
Mice;
Molecular Structure;
Random Allocation;
Receptors, GABA;
metabolism;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2012;47(11):1496-1502
- CountryChina
- Language:Chinese
-
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).
