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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy
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Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy

机译：用于阿尔茨海默病治疗的丙氨酸胺衍生的多目标定向配体

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摘要

Current options for the treatment of Alzheimers disease have been restricted to prescription of acetylcholinesterase inhibitors or N-methyl-D-aspartate receptor antagonist, memantine. Propargylamine-derived multi-target directed ligands, such as ladostigil, M30, ASS234 and contilisant, involve different pathways. Apart from acting as inhibitors of both cholinesterases and monoamine oxidases, they show improvement of cognitive impairment, antioxidant activities, enhancement of iron-chelating activities, protect against tau hyperphosphorylation, block metal-associated oxidative stress, regulate APP and A beta expression processing by the nonamyloidogenic a-secretase pathway, suppress mitochondrial permeability transition pore opening, and coordinate protein kinase C signaling and Bcl-2 family proteins. Other hybrid propargylamine derivatives are also reported.
机译：用于治疗阿尔茨海默病的目前的选项仅限于乙酰胆碱酯酶抑制剂或N-甲基-D-天冬氨酸受体拮抗剂，Memantine的处方。 Propargylamine衍生的多目标定向配体，例如Ladostigil，M30，Ass234和波动涉及不同的途径。 除了作为胆碱酯酶和单胺氧化酶的抑制剂外，它们显示出改善认知障碍，抗氧化活性，增强铁螯合活性，防止TAU超磷酸化，阻断金属相关的氧化应激，调节APP和β表达处理 壬烷过生A分泌酶途径，抑制线粒体渗透率过渡孔口开口，坐标蛋白激酶C信号和BCL-2家族蛋白。 还报道了其他杂种丙氨酸衍生物。

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