抗阿尔茨海默病噻唑衍生物的设计策略及构效关系研究进展

Research progress on design strategies and structure-activity relationship of anti-Alzheimer thiazole derivatives

噻唑是一种五元含硫、氮杂环化合物,由于其特殊的结构和电子性质以及具有的多种生物学活性,已成为药物化学领域中广泛运用的化学骨架之一.在过去的几十年里,噻唑及其衍生物在抗阿尔茨海默病的研究中展现出极大的潜力,其衍生物的化学结构及设计策略和抗阿尔茨海默病的活性密切相关.本文从阿尔茨海默病潜在的靶点出发,基于以乙酰胆碱酯酶为主导的单靶点或者多靶点策略,综述了近年来具有抗阿尔茨海默病活性的噻唑衍生物的设计策略及构效关系研究进展.

Thiazole is a five-membered sulfur-containing and nitrogen heterocyclic compound,which has become one of the widely used chemical frameworks in the field of medicinal chemistry due to its special structure and electronic properties and a variety of biological activities.In the past few decades,thiazole and its derivatives have shown great potential in anti-Alzheimer's research,and the chemical structure and design strategy of its derivatives are closely related to anti-Alzheimer's activity.Starting from the potential targets of Alzheimer's disease,this article reviewed the design strategies and structure-activity research progress of thiazole derivatives with anti-Alzheimer's activity in recent years based on acetylcholinesterase dominated single-target or multi-target strategies.