English   español  
Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/133225
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

New cinnamic – N-benzylpiperidine and cinnamic – N,N-dibenzyl(N-methyl)amine hybrids as Alzheimer-directed multitarget drugs with antioxidant, cholinergic, neuroprotective and neurogenic properties

AuthorsEstrada, Martín ; Herrera-Arozamena, Clara; Pérez, Concepción; Viña, Dolores; Romero, Alejandro ; Morales-García, José A. ; Pérez Castillo, Ana ; Rodríguez-Franco, María Isabel
KeywordsCinnamic-based hybrid
Antioxidants
Neuroprotectants
Neurogenic agents
Human cholinesterases
Human monoamine oxidases
Issue Date4-Oct-2016
PublisherElsevier
CitationEuropean Journal of Medicinal Chemistry 121(4): 376–386 (2016)
AbstractHere we describe new families of multi-target directed ligands obtained by linking antioxidant cinnamic-related structures with N-benzylpiperidine (NBP) or N,N-dibenzyl(N-methyl)amine (DBMA) fragments. Resulting hybrids, in addition to their antioxidant and neuroprotective properties against mitochondrial oxidative stress, are active at relevant molecular targets in Alzheimer’s disease, such as cholinesterases (hAChE and hBuChE) and monoamine oxidases (hMAO-A and hMAO-B). Hybrids derived from umbellic – NBP (8), caffeic – NBP (9), and ferulic – DBMA (12) displayed balanced biological profiles, with IC50s in the low-micromolar and submicromolar range for hChEs and hMAOs, and an antioxidant potency comparable to vitamin E. Moreover, the caffeic – NBP hybrid 9 is able to improve the differentiation of adult SGZ-derived neural stem cells into a neuronal phenotype in vitro.
Publisher version (URL)http://dx.doi.org/10.1016/j.ejmech.2016.05.055
URIhttp://hdl.handle.net/10261/133225
DOI10.1016/j.ejmech.2016.05.055
ISSN0223-5234
E-ISSN1768-3254
Appears in Collections:(IQM) Artículos
(IIBM) Artículos
Files in This Item:
File Description SizeFormat 
New cinnamic hybrids as Alzheimer-directed multitarget drugs.pdf830,41 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.