RESUMEN

1,3,4-Thiadiazole and urea group were hybridized to form new molecular skeleton and 11 compounds were synthesized and evaluated as acetylcholinesterase (AChE) inhibitors. Most of them showed comparable effects in inhibition of AChE, especially compound 6b which exhibited activity with IC50 value 1.17 µM, as strong as galanthamine. This information offered by our research would be valuable for further investigation of structure-activity relationship (SAR) and useful in future research of AChE inhibitors.

Asunto(s)

Acetilcolinesterasa/metabolismo , Inhibidores de la Colinesterasa/síntesis química , Inhibidores de la Colinesterasa/farmacología , Tiadiazoles/farmacología , Urea/análogos & derivados , Inhibidores de la Colinesterasa/química , Relación Dosis-Respuesta a Droga , Estructura Molecular , Relación Estructura-Actividad , Tiadiazoles/síntesis química , Tiadiazoles/química , Urea/síntesis química , Urea/química , Urea/farmacología