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.
Article
en Zh
| WPRIM
| ID: wpr-251796
Biblioteca responsable:
WPRO
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:
1
Índice:
WPRIM
Asunto principal:
Piperidinas
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Escopolamina
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Diseño de Fármacos
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Química
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Inhibidores de la Colinesterasa
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Concentración 50 Inhibidora
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Dioxoles
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Quimioterapia
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Isoindoles
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Indanos
Límite:
Animals
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2015
Tipo del documento:
Article