English   español  
Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/177357
Share/Impact:
Statistics
logo share SHARE logo core CORE   Add this article to your Mendeley library MendeleyBASE

Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL
Exportar a otros formatos:
Title

Indazolylketones as new multitarget cannabinoid drugs

AuthorsGonzález-Naranjo, Pedro ; Pérez-Macías, Natalia; Pérez, Concepción; Roca, Carlos; Vaca, Gabriela; Girón, Rocío; Sánchez-Robles, E.; Martín-Fontelles, M. I.; Ceballos, María L. de ; Martín-Requero, Ángeles ; Campillo, Nuria E. ; Páez, Juan A.
KeywordsAlzheimer's disease
BuChE inhibitor
CB2R agonist
Indazolylketone
Multitarget drug
BACE-1 inhibitor
Issue Date2019
PublisherElsevier
CitationEuropean Journal of Medicinal Chemistry 166: 90-107 (2019)
AbstractMultitarget cannabinoids could be a promising therapeutic strategic to fight against Alzheimer's disease. In this sense, our group has developed a new family of indazolylketones with multitarget profile including cannabinoids, cholinesterase and BACE-1 activity. A medicinal chemistry program that includes computational design, synthesis and in vitro and cellular evaluation has allowed to us to achieve lead compounds. In this work, the synthesis and evaluation of a new class of indazolylketones have been performed. Pharmacological evaluation includes functional activity for cannabinoid receptors on isolated tissue. In addition, in vitro inhibitory assays in AChE/BuChE enzymes and BACE-1 have been carried out. Furthermore, studies of neuroprotective effects in human neuroblastoma SH-SY5Y cells and studies of the mechanisms of survival/death in lymphoblasts of patients with Alzheimer's disease have been achieved. The results of pharmacological tests have revealed that some of these derivatives (5, 6) behave as CB2 cannabinoid agonists and simultaneously show BuChE and/or BACE-1 inhibition.
Publisher version (URL)http://dx.doi.org/10.1016/j.ejmech.2019.01.030
URIhttp://hdl.handle.net/10261/177357
Identifiersdoi: 10.1016/j.ejmech.2019.01.030
issn: 0223-5234
e-issn: 1768-3254
Appears in Collections:(IQM) Artículos
(CIB) Artículos
Files in This Item:
File Description SizeFormat 
accesoRestringido.pdf15,38 kBAdobe PDFThumbnail
View/Open
Show full item record
Review this work
 

Related articles:


WARNING: Items in Digital.CSIC are protected by copyright, with all rights reserved, unless otherwise indicated.