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Title

N-Acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer’s disease

AuthorsGonzález Muñoz, Gema C.; Arce, Mariana P. ; López, Beatriz; López, Beatriz; Romero, Alejandro ; del Barrio, Laura; Martín de Saavedra, María Dolores; Egea, Javier; León, Rafael; Villarroya, Mercedes; López, Manuela G.; García, Antonio G.; Conde, Santiago ; Rodríguez-Franco, María Isabel
KeywordsN-Acylaminophenothiazines
Butyrylcholinesterase inhibition
Neuroprotection
Oxidative stress
Okadaic acid
Beta-amyloid peptide
Calcium modulation
Alzheimer’s disease
Issue Date2011
PublisherElsevier
CitationEuropean Journal of Medicinal Chemistry 46 : 2224-2235 (2011)
AbstractWe have previously reported the multifunctional profile of N-(3-chloro-10H-phenothiazin-10-yl)-3- (dimethylamino)propanamide (1) as an effective neuroprotectant and selective butyrylcholinesterase inhibitor. In this paper, we have developed a series of N-acylaminophenothiazines obtained from our compound library or newly synthesised. At micro- and sub-micromolar concentrations, these compounds selectively inhibited butyrylcholinesterase (BuChE), protected neurons against damage caused by both exogenous and mitochondrial free radicals, showed low toxicity, and could penetrate into the CNS. In addition, N-(3-chloro-10H-phenothiazin-10-yl)-2-(pyrrolidin-1-yl)acetamide (11) modulated the cytosolic calcium concentration and protected human neuroblastoma cells against several toxics, such as calcium overload induced by an L-type Ca2þ-channel agonist, tau-hyperphosphorylation induced by okadaic acid and Ab peptide
Publisher version (URL)http://dx.doi.org/10.1016/j.ejmech.2011.03.003
URIhttp://hdl.handle.net/10261/36676
DOI10.1016/j.ejmech.2011.03.003
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