一种苯甲酸色胺衍生物及其制备与应用

本发明提供了一种苯甲酸色胺衍生物及其制备与应用。本发明苯甲酸色胺衍生物以水杨酸类化合物为起始原料，经过苄基保护、氨基甲酰化、脱保护、缩合四步反应合成得到。本发明所制备的苯甲酸色胺衍生物具有乙酰胆碱酯酶和丁酰胆碱酯酶双重抑制作用，且其作为混合型可逆抑制剂可以减少细胞和动物水平上AChE的含量和表达。同时具备良好的抗神经炎症活性，可以抑制Aβ的聚集，降低BACE-1的表达。可以显著改善AD模型鼠的学习记忆与抗抑郁能力，在细胞和动物水平上均无明显的毒性，且具有良好的药代动力学性能和血脑屏障通透能力，可应用于制备阿尔兹海默症治疗药物。 The invention provides a benzoic...

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Bibliographic Details
Format Patent
LanguageChinese
Published 07.07.2023
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:本发明提供了一种苯甲酸色胺衍生物及其制备与应用。本发明苯甲酸色胺衍生物以水杨酸类化合物为起始原料，经过苄基保护、氨基甲酰化、脱保护、缩合四步反应合成得到。本发明所制备的苯甲酸色胺衍生物具有乙酰胆碱酯酶和丁酰胆碱酯酶双重抑制作用，且其作为混合型可逆抑制剂可以减少细胞和动物水平上AChE的含量和表达。同时具备良好的抗神经炎症活性，可以抑制Aβ的聚集，降低BACE-1的表达。可以显著改善AD模型鼠的学习记忆与抗抑郁能力，在细胞和动物水平上均无明显的毒性，且具有良好的药代动力学性能和血脑屏障通透能力，可应用于制备阿尔兹海默症治疗药物。 The invention provides a benzoic acid tryptamine derivative as well as preparation and application thereof. The benzoic acid tryptamine derivative takes a salicylic acid compound as an initial raw material, and is synthesized by four steps of reaction of benzyl protection, carbamylation, deprotection and condensation. The prepared benzoic acid tryptamine derivative has dual inhibition effects on acetylcholin esterase and butyrylcholin esterase, and can reduce the content and expression of AChE on cell and animal levels as a mixed reversible inhibitor; meanwhile, the derivative has good anti-neuroinflammation activity, and can inhibit the aggregation of A beta and reduce the expression of BACE-1. and the derivative can significantly improve the lea
Bibliography:Application Number: CN202110856721