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首页> 外文期刊>Future Journal of Pharmaceutical Sciences >N-substituted-piperidines as Novel Anti-alzheimer Agents: Synthesis, antioxidant activity, and molecular docking study
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N-substituted-piperidines as Novel Anti-alzheimer Agents: Synthesis, antioxidant activity, and molecular docking study

机译: N -取代的哌啶类药物作为新型抗早老性痴呆剂的合成,抗氧化活性和分子对接研究

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摘要

Design, synthesis and evaluation of new acetylcholinesterase inhibitors by combining carbamoylpiperidine analogs containing nipecotic acid scaffold were described. Then, a series of hybrids have been developed by introducing Free radical scavengers. Molecular modeling was performed and structure activity relationships are discussed. Among the series, most potent compounds showed effective AchE inhibitions, high selectivity over butyrylcholinesterase and high radical scavenging activities. On the basis of this work, the ability of analogs containing nipecotic acid scaffold to serve in the design of N -benzyl-piperidine linked multipotent molecules for the treatment of Alzheimer Disease.
机译:描述了通过结合含有尼泊金菌酸支架的氨基甲酰基哌啶类似物来设计,合成和评估新的乙酰胆碱酯酶抑制剂。然后,通过引入自由基清除剂开发了一系列杂种。进行了分子建模并讨论了结构活性关系。在该系列中,最有效的化合物显示出有效的AchE抑制作用,对丁酰胆碱酯酶的高选择性和高自由基清除活性。在这项工作的基础上,含有尼克酸支架的类似物在设计用于治疗阿尔茨海默氏病的N-苄基-哌啶连接的多能分子中的能力。

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