English   español  
Por favor, use este identificador para citar o enlazar a este item: http://hdl.handle.net/10261/121674
Título

α-aryl-N-alkyl nitrones, as potential agents for stroke treatment: Synthesis, theoretical calculations, antioxidant, anti-inflammatory, neuroprotective, and brain-blood barrier permeability properties

AutorChioua, Mourad ; Sucunza, D.; Soriano, Elena ; Hadjipavlou-Litina, Dimitra; Alcázar González, Alberto; Ayuso, I.; Oset-Gasque, María J.; Gonzalez, M. P.; Monjas, Leticia ; Rodríguez-Franco, María Isabel ; Marco-Contelles, José ; Marco-Contelles, José ; Samadi, Abdelouahid
Fecha de publicación2015
EditorAmerican Chemical Society
CitaciónJournal of Medicinal Chemistry 55: 153-168 (2015)
ResumenWe report the synthesis, theoretical calculations, the antioxidant, anti-inflammatory, and neuroprotective properties, and the ability to cross the blood-brain barrier (BBB) of (Z)-α-aryl and heteroaryl-N-alkyl nitrones as potential agents for stroke treatment. The majority of nitrones compete with DMSO for hydroxyl radicals, and most of them are potent lipoxygenase inhibitors. Cell viability-related (MTT assay) studies clearly showed that nitrones 1-3 and 10 give rise to significant neuroprotection. When compounds 1-11 were tested for necrotic cell death (LDH release test) nitrones 1-3, 6, 7, and 9 proved to be neuroprotective agents. In vitro evaluation of the BBB penetration of selected nitrones 1, 2, 10, and 11 using the PAMPA-BBB assay showed that all of them cross the BBB. Permeable quinoline nitrones 2 and 3 show potent combined antioxidant and neuroprotective properties and, therefore, can be considered as new lead compounds for further development in specific tests for potential stroke treatment. © 2011 American Chemical Society.
URIhttp://hdl.handle.net/10261/121674
DOI10.1021/jm201105a
Identificadoresdoi: 10.1021/jm201105a
issn: 0022-2623
e-issn: 1520-4804
Aparece en las colecciones: (IQM) Artículos
Ficheros en este ítem:
Fichero Descripción Tamaño Formato  
accesoRestringido.pdf15,38 kBAdobe PDFVista previa
Visualizar/Abrir
Mostrar el registro completo
 

Artículos relacionados:


NOTA: Los ítems de Digital.CSIC están protegidos por copyright, con todos los derechos reservados, a menos que se indique lo contrario.