Design, synthesis and biological evaluation of novel 1,3 dioxolo 4,5-fisoindolone derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 191-198, 2015.
Artigo
em Chinês
| WPRIM
| ID: wpr-251796
ABSTRACT
A series of [1,3]dioxolo[4,5-f]isoindolone derivatives were designed, synthesized and evaluated as inhibitors of acetylcholinesterases (AChE). Furthermore, their effects on memory impairment of mice induced by scopolamine were investigated with step-through test. The results suggested that most of the target compounds exhibited potential inhibition on AChE with IC50 values at micromolar range. Compounds I1 (IC50 value of 0.086 μmol · L(-1)) and I2 (IC50 value of 0.080 μmol · L(-1)) showed the strongest AChE inhibitory activity, which are equipotent to donepezil (IC50 value of 0.094 μmol · L(-1)). Moreover, compounds I1-I4 could improve the memory impairment induced by scopolamine in mice.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Piperidinas
/
Escopolamina
/
Desenho de Fármacos
/
Química
/
Inibidores da Colinesterase
/
Concentração Inibidora 50
/
Dioxóis
/
Tratamento Farmacológico
/
Isoindóis
/
Indanos
Limite:
Animais
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2015
Tipo de documento:
Artigo
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