Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 1 de 1
Filtrar
Más filtros












Base de datos
Intervalo de año de publicación
1.
Bioorg Chem ; 119: 105548, 2022 02.
Artículo en Inglés | MEDLINE | ID: mdl-34959174

RESUMEN

Epilepsy is a disease that affects millions of people around the globe and has a multifactorial cause. Inflammation is a process that can be involved in the development of seizures. Thus, the present study proposed the design and synthesis of new candidates for antiepileptic drugs that would also control the inflammatory process. Nine new derivatives of the substituted thiazophthalimide hybrid core were obtained with satisfactory purity ≥99% and yields between 27% and 87%. All compounds showed cell viability values greater than 90% in the culture of PBMC cells from healthy volunteers and, therefore, were not considered cytotoxic. These compounds modulated proinflammatory cytokines IFN-y and IL-17A and can mitigate inflammation. Acute toxicity studies of compound 7i in an animal model indicated that the compound has low toxicity and an LD50 greater than 2 g/kg in healthy adult rats. The same compound did not show positive results for anticonvulsant activity through the PTZ test. However, 7i demonstrates the interaction with the target GABA-A receptor in silico, indicating a possible activity as an agonist of that receptor. Thus, further studies are needed to investigate the anticonvulsant activity, in particular, using models in which the inflammatory process triggers epileptic seizures.


Asunto(s)
Anticonvulsivantes/uso terapéutico , Epilepsia/tratamiento farmacológico , Ftalimidas/uso terapéutico , Convulsiones/tratamiento farmacológico , Tiazoles/uso terapéutico , Animales , Anticonvulsivantes/síntesis química , Anticonvulsivantes/química , Células Cultivadas , Relación Dosis-Respuesta a Droga , Epilepsia/patología , Humanos , Masculino , Simulación del Acoplamiento Molecular , Estructura Molecular , Ftalimidas/síntesis química , Ftalimidas/química , Ratas , Ratas Wistar , Convulsiones/patología , Relación Estructura-Actividad , Tiazoles/síntesis química , Tiazoles/química
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA
...