Synthesis, in vitro acetylcholinesterase inhibitory activity and molecular docking of new acridine-coumarin hybrids.
Int J Biol Macromol
; 104(Pt A): 333-338, 2017 Nov.
Article
en En
| MEDLINE
| ID: mdl-28601645
ABSTRACT
A novel series of acridine-coumarin hybrids was synthesized and biologically evaluated for their potential inhibitory effect on both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The newly synthesized derivatives 9a-d have shown higher activity against human AChE (hAChE) compared with 7-MEOTA as the standard drug. Among them derivative 9b exhibited the most potent acetylcholinesterase inhibitory activity, with an IC50 value of 5.85µM compared with 7-MEOTA (IC50=15µM). Molecular modelling studies were performed to predict the binding modes of compounds 9b, 9c and 9f with hAChE/hBuChE.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Acetilcolinesterasa
/
Acridinas
/
Inhibidores de la Colinesterasa
/
Cumarinas
/
Simulación del Acoplamiento Molecular
Tipo de estudio:
Prognostic_studies
Límite:
Humans
Idioma:
En
Revista:
Int J Biol Macromol
Año:
2017
Tipo del documento:
Article