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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
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N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.

机译：N-酰基氨基吩噻嗪：具有多功能活性的神经保护剂，可潜在治疗阿尔茨海默氏病。

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摘要

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 Ca2+-channel agonist, tau-hyperphosphorylation induced by okadaic acid and Abeta peptide.
机译：我们以前已经报告了N-（3-氯-10H-吩噻嗪-10-基）-3-（二甲基氨基）丙酰胺（1）作为有效的神经保护剂和选择性丁酰胆碱酯酶抑制剂的多功能概况。在本文中，我们开发了一系列从化合物库中获得或新合成的N-酰基氨基吩噻嗪。在微摩尔和亚微摩尔浓度下，这些化合物选择性抑制丁酰胆碱酯酶（BuChE），保护神经元免受外源和线粒体自由基造成的损害，毒性低，并且可以渗透到CNS中。此外，N-（3-氯-10H-吩噻嗪-10-基）-2-（吡咯烷-1-基）乙酰胺（11）调节细胞内钙的浓度，并保护人类神经母细胞瘤细胞免受多种毒性，例如钙超载由L型Ca2 +通道激动剂诱导，由冈田酸和Abeta肽诱导的tau-超磷酸化。

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