新型联苯/联苄基衍生物作为乙酰胆碱酯酶和丁酰胆碱酯酶双重抑制剂的设计、合成及生物学评价
Design, Synthesis, and Biological Evaluation of a New Series of Biphenyl/Bibenzyl Derivatives Functioning as Dual Inhibitors of Acetylcholinesterase and Butyrylcholinesterase.
作者信息
Wang Dong-Mei, Feng Bo, Fu Hui, Liu Ai-Lin, Wang Lin, Du Guan-Hua, Wu Song
机构信息
State Key Laboratory of Bioactive Substances and Functions of Natural Medicines & Ministry of Health Key Laboratory of Biosynthesis of Natural Products, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
Beijing Institutes For Drug Control, Beijing 100050, China.
出版信息
Molecules. 2017 Jan 20;22(1):172. doi: 10.3390/molecules22010172.
Alzheimer's disease (AD), the most common form of dementia in adults, is a progressive neurodegenerative disorder of the brain characterized by loss of memory and steady deterioration of cognition. Here, a series of symmetrical molecules containing biphenyl/bibenzyl scaffolds (-) were designed, synthesized, and evaluated for their ability to inhibit both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). A biological evaluation showed that most of these biphenyl derivatives were potent AChE and BuChE inhibitors. Among them, compound displayed the greatest ability to inhibit BuChE (IC = 0.74 µM) and was also a good AChE inhibitor (IC = 1.18 µM). Compound was not only a potent AChE inhibitor (IC = 0.096 µM), but also a mild BuChE inhibitor (IC =1.25 µM). Overall, these results suggested that compound may be a promising agent in the treatment of AD.
阿尔茨海默病（AD）是成人中最常见的痴呆形式，是一种进行性神经退行性脑疾病，其特征为记忆丧失和认知功能持续恶化。在此，设计、合成了一系列含有联苯/联苄支架（-）的对称分子，并评估了它们抑制乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BuChE）的能力。生物学评估表明，这些联苯衍生物中的大多数都是有效的AChE和BuChE抑制剂。其中，化合物 表现出最强的抑制BuChE的能力（IC = 0.74 µM），并且也是一种良好的AChE抑制剂（IC = 1.18 µM）。化合物 不仅是一种有效的AChE抑制剂（IC = 0.096 µM），也是一种轻度的BuChE抑制剂（IC =1.25 µM）。总体而言，这些结果表明化合物 可能是治疗AD的一种有前景的药物。
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