RESUMEN
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.
Asunto(s)
Animales , Femenino , Masculino , Ratones , 4-Aminopiridina , Amidas , Química , Usos Terapéuticos , Anticonvulsivantes , Química , Usos Terapéuticos , Epilepsia , Quimioterapia , Estructura Molecular , Distribución Aleatoria , Relación Estructura-Actividad , Ácido gamma-Aminobutírico , QuímicaRESUMEN
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.