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Sulfur-containing therapeutics in the treatment of Alzheimer’s disease
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2021-01-15 , DOI: 10.1007/s00044-020-02687-1
Haizhou Zhu 1 , Venkateshwara Dronamraju 1 , Wei Xie 1 , Swati S More 1
Affiliation  

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.



中文翻译:

治疗阿尔茨海默病的含硫疗法

硫作为有机硫广泛存在于天然产物和合成有机化合物中,通常与多种生物活性相关。O苯并噻唑,其中苯环稠合到噻唑基硫化合物的4,5位上,在药物化学领域,特别是在阿尔茨海默病(AD)治疗药物的开发中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,也是年龄相关性痴呆的主要原因,造成严重的社会和经济负担。不幸的是,AD 无法治愈。由于含硫化合物具有先天的抗氧化潜力,人们对 AD 背景下的含硫化合物进行了大量研究,其中一些目前正在临床试验中进行评估。在这篇综述中,我们描述了该领域的新兴趋势,特别是多靶点的概念和疾病缓解策略的制定。还讨论了 SAR、药理学靶点、体外/体内 ADMET、AD 动物模型的功效以及此类硫化合物在临床试验中的应用。本文对基于有机硫的 AD 治疗剂进行了全面综述,并对其未来发展提供了见解。

更新日期:2021-01-15
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