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Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/36676
Title: N-Acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer’s disease
Authors: González 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
Keywords: N-Acylaminophenothiazines
Butyrylcholinesterase inhibition
Oxidative stress
Okadaic acid
Beta-amyloid peptide
Calcium modulation
Alzheimer’s disease
Issue Date: 2011
Publisher: Elsevier
Citation: European Journal of Medicinal Chemistry 46 : 2224-2235 (2011)
Abstract: We 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
URI: http://hdl.handle.net/10261/36676
DOI: 10.1016/j.ejmech.2011.03.003
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