RT Journal Article
T1 Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease
A1 González-Naranjo, Pedro
A1 Pérez-Macias, Natalia
A1 Campillo, Nuria
A1 Pérez, Concepción
A1 Arán, Vicente
A1 Girón, Rocio
A1 Sánchez-Robles, Eva
A1 Páez, Juan
A1 Gómez Cañas, María
A1 Martín Fontelles, María Isabel
A1 García Arencibia, Moisés
A1 Fernández Ruiz, José Javier
AB Designing drugs with a specific multi-target profile is a promising approach against multifactorial ill nesses as Alzheimer’s disease. In this work, new indazole ethers that possess dual activity as both cannabinoid agonists CB2 and inhibitors of BuChE have been designed by computational methods. On the basis of this knowledge, the synthesis, pharmacological evaluation and docking studies of a new class of indazoles has been performed. Pharmacological evaluation includes radioligand binding assays with [3H]-CP55940 for CB1R and CB2R and functional activity for cannabinoid receptors on isolated tissue. Additionally, in vitro inhibitory assays of AChE/BuChE and the corresponding competition studies have been carried out. The results of pharmacological tests have revealed that three of these derivatives behave as CB2 cannabinoid agonists and simultaneously show BuChE inhibition. In particular, com pounds 3 and 24 have emerged as promising candidates as novel cannabinoids that inhibit BuChE by a non-competitive or mixed mechanism, respectively. On the other hand, both molecules show antioxidantproperties.
PB European Journal of Medical Chemistry
SN 0223-5234
YR 2014
FD 2014
LK https://hdl.handle.net/20.500.14352/93640
UL https://hdl.handle.net/20.500.14352/93640
LA eng
NO González-Naranjo  P, Pérez-Macias  N, Campillo  NE, Pérez  C, Arán  VJ, Girón  R, Sánchez-Robles E, Martín MI, Gómez-Cañas M, García-Arencibia M, Fernández-Ruiz J, Páez JA. Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease. Eur J MedChem. 2014, 73:56-72.
NO Ministerio de Ciencia e Innovación (España)
NO Comunidad de Madrid
DS Docta Complutense
RD 28 dic 2025