1.
Bioorg Med Chem Lett
; 10(7): 637-9, 2000 Apr 03.
Artículo
en Inglés
| MEDLINE
| ID: mdl-10762042
RESUMEN
The syntheses, the anticholinesterase activities and structure-activity relationships of homodimeric (3a-c) and heterodimeric (6a-c) alkylene linked bis-galanthamine are reported. Compounds 6b-c were found to be more potent than galanthamine and tacrine in inhibiting AChE.
Asunto(s)
Acetilcolinesterasa/metabolismo , Inhibidores de la Colinesterasa/farmacología , Galantamina/análogos & derivados , Galantamina/farmacología , Acetilcolinesterasa/efectos de los fármacos , Inhibidores de la Colinesterasa/síntesis química , Inhibidores de la Colinesterasa/química , Dimerización , Diseño de Fármacos , Galantamina/síntesis química , Relación Estructura-Actividad
2.
Bioorg Med Chem
; 6(10): 1835-50, 1998 Oct.
Artículo
en Inglés
| MEDLINE
| ID: mdl-9839013
RESUMEN
New galanthamine derivatives, especially bis-interacting ligands 3-5 and 7-9 were prepared in order to interact with the catalytic and the peripheral sites of acetylcholinesterase (AChE). The synthesis, the anticholinesterase activities, and the structure-activity relationships of bis-interacting ligands are reported. Compounds 4d-e were found to be more potent than galanthamine and tacrine in inhibiting AChE.