Synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1496-1502, 2012.
Artículo
en Chino
| 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).
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Relación Estructura-Actividad
/
Estructura Molecular
/
Distribución Aleatoria
/
4-Aminopiridina
/
Química
/
Receptores de GABA
/
Usos Terapéuticos
/
Relación Dosis-Respuesta a Droga
/
Quimioterapia
/
Epilepsia
Límite:
Animales
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2012
Tipo del documento:
Artículo
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