Alzheimer's disease (AD), as the fourth leading cause of death among the elderly worldwide, has brought enormous challenge to the society. Due to its extremely complex pathogeneses, the development of multi-target directed ligands (MTDLs) becomes the major strategy for combating AD. Carbamate moiety, as an essential building block in the development of MTDLs, exhibits structural similarity to neurotransmitter acetylcholine (ACh) and has piqued extensive attention in discovering multifunctional cholinesterase inhibitors. To date, numerous preclinical studies demonstrate that carbamate-based cholinesterase inhibitors can prominently increase the level of ACh and improve cognition impairments and behavioral deficits, providing a privileged strategy for the treatment of AD. Based on the recent research focus on the novel cholinesterase inhibitors with multiple biofunctions, this review aims at summarizing and discussing the most recent studies excavating the potential carbamate-based MTDLs with cholinesterase inhibition efficacy, to accelerate the pace of pleiotropic cholinesterase inhibitors for coping AD.

阿尔茨海默病（Alzheimer's disease，AD）作为全球第四大老年人死因，给社会带来了巨大挑战。由于其极其复杂的发病机制，多靶点定向配体（MTDLs）的开发成为对抗AD的主要策略。氨基甲酸酯部分作为 MTDLs 发展的重要组成部分，表现出与神经递质乙酰胆碱 (ACh) 的结构相似性，并在发现多功能胆碱酯酶抑制剂方面引起了广泛关注。迄今为止，许多临床前研究表明，氨基甲酸酯类胆碱酯酶抑制剂可以显着提高 ACh 水平并改善认知障碍和行为缺陷，为 AD 的治疗提供了一种特殊的策略。