Design, synthesis and evaluation of new acetylcholinesterase inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 346-351, 2014.
Artículo
en Chino
| WPRIM
| ID: wpr-245079
ABSTRACT
A series of novel 2-amino-4-phenylthiazole derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase were investigated. 2-Amino-4-phenylthiazoles were prepared from alpha-bromoacetophenones by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 8a was the best of them. The IC50 of 8a to AChE is 3.54 micromol x L(-1), and the value was better than that of rivastigmine. 2-Amino-4-phenylthiazole derivatives showed a certain bioactivity in vitro, which were worth further investigation.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Farmacología
/
Acetilcolinesterasa
/
Tiazoles
/
Diseño de Fármacos
/
Estructura Molecular
/
Química
/
Inhibidores de la Colinesterasa
/
Concentración 50 Inhibidora
/
Metabolismo
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2014
Tipo del documento:
Artículo
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