Design, synthesis and antiepileptic activity of 4-(2-acetoxybenzoylamino) butyrate derivatives.
- Author:
Wen-Hu LIU
1
;
Dian HE
;
Xin-Qiang YIN
;
Yi LIU
Author Information
1. Department of Pharmacology, North Sichuan Medical College, NanChong 637000, China.
- Publication Type:Journal Article
- MeSH:
4-Aminopyridine;
Animals;
Anticonvulsants;
chemical synthesis;
chemistry;
therapeutic use;
Butyrates;
chemical synthesis;
chemistry;
therapeutic use;
Drug Design;
Epilepsy;
chemically induced;
drug therapy;
Female;
Lethal Dose 50;
Male;
Mice;
Molecular Structure;
Random Allocation;
Structure-Activity Relationship;
gamma-Aminobutyric Acid;
chemistry
- From:
Acta Pharmaceutica Sinica
2011;46(3):299-304
- CountryChina
- Language:Chinese
-
Abstract:
A series of 4-(2-acetoxybenzoylamino) butyrate derivatives were designed and synthesized. All of the novel 12 compounds (7a-7k) were synthesized from gamma-aminobutyric acid (1) as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that most of these title compounds possessed antiepileptic activity. Compounds 7i-7k displayed strong antiepileptic activity and are worth for further development. Compounds 4, 7d-7h showed moderate antiepileptic activity. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyrate derivatives is also discussed preliminarily.
