摘要
阿尔茨海默病 (AD) 是一种不可逆的进行性神经退行性疾病,可能占全球痴呆病例的约 60-70%。 AD的特点是行为和认知功能受损,包括记忆、语言、概念、注意力、判断力和推理问题。 AD 的两个重要标志是根据疾病的病因,分别在大脑中出现斑块和缠结的淀粉样蛋白-β (Aβ) 和 tau 蛋白,包括胆碱能损伤、金属失调、氧化应激和降解神经递质。目前,使用的药物只能缓解症状,但不能有效治愈疾病,这就需要开发新的分子来治疗 AD。杂环化合物已被证明有能力开发为治疗各种疾病的药物。由于结构变异的可能性,五元杂环化合物三唑因发现新药而备受关注。而且,它已经证明了它在各种药物类别中的重要性。本综述主要总结了新型 1,2,3-三唑和 1,2,4-三唑基分子在靶向各种 AD 靶标(如磷酸二酯酶 1 (PDE1) 抑制剂、细胞凋亡)的药物发现过程中的最新进展信号调节激酶 1 (ASK1) 抑制剂、生长抑素受体亚型 4 (SSTR4) 激动剂、其他几种可成药靶点、分子模型研究,以及用于合成含有分子的三唑类的各种方法,如点击反应、佩利扎里反应和艾因霍恩-布伦纳反应。
关键词: 阿尔茨海默病、1,2,3-三唑、1,4-三唑、Aβ-淀粉样蛋白、tau 蛋白、磷酸二酯酶 1 抑制剂、佩利扎里反应、分子对接。
图形摘要
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