Sulfur-containing therapeutics in the treatment of Alzheimer's disease.

Sulfur-containing therapeutics in the treatment of Alzheimer's disease.
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含硫治疗剂在阿尔茨海默病治疗中的应用。

DOI:
10.1007/s00044-020-02687-1
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发表时间:
2021-03
期刊:
Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents
影响因子:
--
通讯作者:
More SS
More SS
中科院分区:
其他
文献类型:
--
作者:
Zhu H;Dronamraju V;Xie W;More SS

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硫以有机硫的形式广泛存在于天然产物和合成有机化合物中,与多种生物活性密切相关。在药物化学领域,尤其是在阿尔茨海默病(AD)治疗药物的开发中,苯环与噻唑类含硫化合物的4,5-位融合在一起的苯并噻唑继续受到越来越多的关注。AD是一种致命的神经退行性疾病,是老年性痴呆的主要原因,造成严重的社会和经济负担。不幸的是,阿尔茨海默病没有治愈方法。在阿尔茨海默病的背景下,人们对含硫化合物进行了大量的研究,因为它们具有天然的抗氧化能力,其中一些目前正在进行临床试验。在这篇综述中,我们描述了该领域的新趋势,特别是多目标的概念和疾病修正战略的制定。还讨论了合成孔径雷达、药理靶点、体内外ADMET、在AD动物模型中的疗效以及此类硫化物在临床试验中的应用。本文对以有机硫磺为基础的AD治疗药物进行了全面的综述,并对其未来的发展提出了见解。
Sulfur is widely existent in natural products and synthetic organic compounds as organosulfur, which are often associated with a multitude of biological activities. OBenzothiazole, in which benzene ring is fused to the 4,5-positions of the thiazolerganosulfur compounds continue to garner increasing amounts of attention in the field of medicinal chemistry, especially in the development of therapeutic agents for Alzheimer’s disease (AD). AD is a fatal neurodegenerative disease and the primary cause of age-related dementia posing severe societal and economic burdens. Unfortunately, there is no cure for AD. A lot of research has been conducted on sulfur-containing compounds in the context of AD due to their innate antioxidant potential and some are currently being evaluated in clinical trials. In this review, we have described emerging trends in the field, particularly the concept of multi-targeting and formulation of disease-modifying strategies. SAR, pharmacological targets, in vitro/vivo ADMET, efficacy in AD animal models, and applications in clinical trials of such sulfur compounds have also been discussed. This article provides a comprehensive review of organosulfur-based AD therapeutic agents and provides insights into their future development.
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