Design, synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide derivatives.
- Author:
Wen-Hu LIU
1
;
Shi-Bao WANG
;
Xian YU
;
Xin-Qiang YIN
;
Yi LIU
Author Information
1. Department of Pharmacology, School of Pharmacy, North Sichuan Medical College, Nanchong 637000, China. lwh790214@163.com
- Publication Type:Journal Article
- MeSH:
4-Aminopyridine;
Amides;
chemical synthesis;
chemistry;
therapeutic use;
Animals;
Anticonvulsants;
chemical synthesis;
chemistry;
therapeutic use;
Epilepsy;
chemically induced;
drug therapy;
Female;
Male;
Mice;
Molecular Structure;
Random Allocation;
Structure-Activity Relationship;
gamma-Aminobutyric Acid;
chemistry
- From:
Acta Pharmaceutica Sinica
2012;47(2):194-199
- CountryChina
- Language:Chinese
-
Abstract:
To explore new agents of gamma-aminobutyric acid (GABA) derivatives with more potent antiepileptic activity, a series of 4-(2-acetoxybenzoylamino) butyramide derivatives were designed and synthesized. All of the novel compounds (5a-51) were synthesized from GABA as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that all target compounds displayed strong antiepileptic activities and were worth for further study. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyramide derivatives was also discussed preliminarily.
