Novel multitarget-directed tacrine derivatives as potential candidates for the treatment of Alzheimer's disease.
Novel multitarget-directed tacrine derivatives as potential candidates for the treatment of Alzheimer's disease.
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DOI：
10.1080/14756366.2016.1210139
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发表时间：
2017-12
影响因子：
5.6
通讯作者：
Duan JA
中科院分区：
文献类型：
--
作者：
Wu WY;Dai YC;Li NG;Dong ZX;Gu T;Shi ZH;Xue X;Tang YP;Duan JA
阿尔茨海默病（Alzheimer's disease，AD）是一种复杂的、进行性的神经退行性疾病，不仅威胁着老年人的健康，也给整个社会医疗卫生系统带来了沉重的负担。AD的有效治疗方法有限，疗效仍不令人满意。鉴于AD的流行和预期的发病率增加，设计和开发有效和安全的抗AD药物已成为药学研究领域的热点。由于AD的病因是多因素的，因此多靶点定向配体（MTDLs）方法在寻找治疗AD的新药方面是有希望的。他克林是第一个乙酰胆碱酯酶（AChE）抑制剂，因其结构简单、活性明确，以及在结构修饰方面的优势，被认为是理想的活性片段，可被引入多靶点抗AD药物的整体分子骨架中。本文综述了近年来（2012年至今）他克林的化学修饰研究进展，为进一步研究新型多靶点他克林衍生物治疗AD提供参考。
Alzheimer’s disease (AD) is a neurodegenerative disorder, which is complex and progressive; it has not only threatened the health of elderly people, but also burdened the whole social medical and health system. The available therapy for AD is limited and the efficacy remains unsatisfactory. In view of the prevalence and expected increase in the incidence of AD, the design and development of efficacious and safe anti-AD agents has become a hotspot in the field of pharmaceutical research. Due to the multifactorial etiology of AD, the multitarget-directed ligands (MTDLs) approach is promising in search for new drugs for AD. Tacrine, which is the first acetylcholinesterase (AChE) inhibitor, has been selected as the ideal active fragment because of its simple structure, clear activity, and its superiority in the structural modification, thus it could be introduced into the overall molecular skeletons of the multi-target-directed anti-AD agents. In this review, we have summarized the recent advances (2012 to the present) in the chemical modification of tacrine, which could provide the reference for the further study of novel multi-target-directed tacrine derivatives to treat AD.
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