1.
Eur J Med Chem
; 43(1): 166-73, 2008 Jan.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17574306
RESUMEN
A series of helicid analogues were prepared and evaluated in vitro for the cholinesterase (AChE and BuChE) inhibitory activities via UV spectroscopy. The results indicated that compounds 5, 6d and 8 exhibited potent AChE inhibitory activities with IC(50) values of 0.45+/-0.02microM, 0.49+/-0.02microM, and 0.20+/-0.01microM, respectively. High selectivity for AChE over BuChE was also observed. Kinetic study showed that the mechanism of AChE inhibition of compounds 5, 6d and 8 was all mixed-type.
Asunto(s)
Acetilcolinesterasa/metabolismo , Benzaldehídos/síntesis química , Benzaldehídos/farmacología , Inhibidores de la Colinesterasa/síntesis química , Benzaldehídos/química , Benzaldehídos/metabolismo , Productos Biológicos/química , Productos Biológicos/metabolismo , Productos Biológicos/farmacología , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/metabolismo , Inhibidores de la Colinesterasa/farmacología , Evaluación Preclínica de Medicamentos , Glicósidos/farmacología , Humanos , Concentración 50 Inhibidora , Cinética , Bases de Schiff/química , Sensibilidad y Especificidad , Espectrofotometría Ultravioleta
2.
Bioorg Med Chem Lett
; 17(8): 2123-5, 2007 Apr 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17317172
RESUMEN
A new class of inhibitors of acetylcholinesterase (methyl 2-(2-(4-formylphenoxy)acetamido)-2-substituted acetate derivatives) is described. Compounds 4b and 4i were found to be more potent than galanthamine in inhibiting acetylcholinesterase.
