Design, synthesis and evaluation of N-acyl-4-phenylthiazole-2-amines as acetylcholinesterase inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 813-818, 2014.
Artículo
en Chino
| WPRIM
| ID: wpr-245010
ABSTRACT
N-Acyl-4-phenylthiazole-2-amines were designed and synthesized, moreover their effects on acetylcholinesterase activities were tested. N-Acyl-4-phenylthiazole-2-amines were prepared from substituted 2-bromo-1-acetophenones by three steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The results showed that the target compounds had a certain inhibitory activity on AChE in vitro. Among them, 8c was the best, and IC50 of 8c was 0.51 micromol x L(-1), better than that of rivastigmine and Huperzine-A. The inhibitory activities of N-acyl-4-phenylthiazole-2-amines on acetylcholinesterase are worth while to be further studied.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Farmacología
/
Acetilcolinesterasa
/
Sesquiterpenos
/
Relación Estructura-Actividad
/
Tiazoles
/
Diseño de Fármacos
/
Inhibidores de la Colinesterasa
/
Alcaloides
/
Rivastigmina
/
Aminas
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2014
Tipo del documento:
Artículo
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