Bioactive heterocycles: Green synthesis and its anti-Alzheimer activity

IF 1.1 Q3 CHEMISTRY, MULTIDISCIPLINARY
S. Roopan, Mohamed Sulthan Hasan Fathima Afridha, Kathar Aazath, Sagayaraj Jane Anto Simplica
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引用次数: 1

Abstract

The wide pharmaceutical activity of the bioactive heterocycles, which include nitrogen, oxygen, and sulphur and comprise five- and six-membered rings, has drawn the attention of medicinal chemists for several years. The therapeutic potential of bioactive heterocycles for a variety of disorders lies in their medicinal effects. The most prominent of them is Alzheimer's disease (AD), a neurodegenerative disorder that impairs memory and causes other psychiatric problems. Globally, there are around 54 million cases, and by 2050, that number is predicted to rise by 131 million. So far, donepezil, galantamine, and rivastigmine have indeed received FDA approval for use in the treatment of AD. In this regard, the pharmacophoric properties of heterocycle molecules are equivalent to those of galantamine mimics. Therefore, it is beneficial to create novel compounds containing these moieties and test their ability to inhibit acetyl and butyl cholinesterase. Diverse heterocyclic scaffolds may now have therapeutic potential for Alzheimer's disease. Recently, greener and more expeditious synthesis of bioactive heterocycles has drawn much attention because of the utilisation of environmentally benign protocols, thereby diminishing the usage of hazardous chemicals. In this review, we discuss the most pertinent findings about the "green" synthesis of heterocycles and their possible anti-activity against Alzheimer's.
生物活性杂环化合物的绿色合成及其抗阿尔茨海默病活性
生物活性杂环包括氮、氧和硫,由五元环和六元环组成,其广泛的药物活性多年来引起了药物化学家的注意。生物活性杂环化合物对多种疾病的治疗潜力在于其药物作用。其中最突出的是阿尔茨海默病(AD),这是一种神经退行性疾病,会损害记忆并导致其他精神问题。全球约有5400万病例,到2050年,这一数字预计将增加1.31亿。到目前为止,多奈哌齐、加兰他明和利瓦斯汀确实已获得FDA批准用于治疗阿尔茨海默病。在这方面,杂环分子的药效性质与加兰他明模拟物相当。因此,建立含有这些部分的新化合物并测试其抑制乙酰胆碱酯酶和丁基胆碱酯酶的能力是有益的。多种杂环支架现在可能具有治疗阿尔茨海默病的潜力。最近,由于采用无害环境的方案,更绿色和更快速的生物活性杂环合成引起了广泛关注,从而减少了有害化学品的使用。本文就杂环类化合物的“绿色”合成及其可能的抗阿尔茨海默病活性研究进展作一综述。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Current Green Chemistry
Current Green Chemistry CHEMISTRY, MULTIDISCIPLINARY-
CiteScore
4.30
自引率
13.60%
发文量
6
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