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三唑衍生物作为阿尔茨海默病抑制剂:最新进展和构效关系。

Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships.

机构信息

School of Materials Science and Engineering, Engineering Research Center of Environmental Materials and Membrane Technology of Hubei Province, Wuhan Institute of Technology, Wuhan, 430205, PR China.

School of Materials Science and Engineering, Engineering Research Center of Environmental Materials and Membrane Technology of Hubei Province, Wuhan Institute of Technology, Wuhan, 430205, PR China.

出版信息

Eur J Med Chem. 2019 Oct 15;180:656-672. doi: 10.1016/j.ejmech.2019.07.059. Epub 2019 Jul 22.

Abstract

Alzheimer's disease (AD) is a well known neurodegenerative disorder alarming millions of people worldwide and the subsequent epidemiological statistics highlights the implication of the disease. AD is a multi-factorial disease, a variety of single-target directed drugs that have reached clinical trials have unsuccessful. Hence, various factors associated without set of AD have been considered in targeted drug discovery and development. Triazoles are five-membered heterocyclic scaffold due to their broad range of biological activities. The present review focuses on the recent developments in the area of medicinal chemistry to explore the diverse chemical structures of potential inhibitors of Alzheimer's disease and also look at its structure-activity relationships (SAR) studies of bioactive compounds for future discovery of suitable drug candidates. The prominence has been given on the major advancements in the medicinal brochure of this pharmacophore for the period during 2012-2019.

摘要

阿尔茨海默病(AD)是一种众所周知的神经退行性疾病,令全球数百万人感到震惊,随后的流行病学统计数据强调了该疾病的影响。AD 是一种多因素疾病,已达到临床试验的多种单靶标导向药物均未成功。因此,在靶向药物发现和开发中考虑了与 AD 无关的各种因素。三唑类是五元杂环支架,由于其广泛的生物活性。本综述重点介绍了药物化学领域的最新进展,以探索阿尔茨海默病潜在抑制剂的各种化学结构,并研究生物活性化合物的结构-活性关系(SAR)研究,以发现合适的药物候选物。在 2012-2019 年期间,该药效团的药物手册取得了重大进展。

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