1研究背景阿尔茨海默病的发生是由于大脑皮层缺失了胆碱乙酰转移酶(ChAT),不能或降低了由胆碱合成乙酰胆碱的能力,皮层的胆碱能传导功能降低,造成记忆障碍和痴呆。所以,提高神经元的胆碱能活性是治疗痴呆患者的一个切入点。此外,胆碱酯酶(AChE)抑制剂也是治疗阿尔茨海默病的重要手段。多奈哌齐的研制就是从寻找新结构类型的胆碱酯酶抑制剂入手的。 1 Background Alzheimer’s disease is caused by the absence of choline acetyltransferase (ChAT) in the cerebral cortex, which can not or reduces the ability to synthesize acetylcholine from choline, reduced cholinergic conduction in the cortex, and memory impairment and dementia. Therefore, increasing the cholinergic activity of neurons is an entry point for the treatment of patients with dementia. In addition, cholinesterase (AChE) inhibitors are also important tools for the treatment of Alzheimer’s disease. Donepezil was developed from the search for a new type of structure of the cholinesterase inhibitors to start.