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An updated patent review of therapeutic applications of chalcone derivatives (2014-present)

机译:氯酮衍生物治疗应用的更新专利综述(2014年至今)

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Introduction: Chalcone or benzylideneacetophenone or 1,3-diphenyl-2-propene-1-one is a natural product comprising of two aromatic rings connected together by a three-carbon alpha, beta unsaturated carbonyl bridge. It is one of the most privileged scaffolds in medicinal chemistry that can be synthesized in the laboratory and can be converted into several therapeutically active heterocyclic scaffolds. It exhibits multifarious pharmacological activities and also plays a key role in several non-pharmacological scientific applications. Areas covered: The present article comprehensively focuses on the approved patents during the time duration 2014-2018 on various chalcone molecules with diverse pharmacological activities. Expert opinion: The study puts forward the latest updated therapeutic applications of chalcone-based compounds as antiproliferative, antidiabetic, anti-infective, anti-inflammatory, antioxidant, antiaging, neuroprotective, and cardioprotective agents. The type, position, and the number of substituents present on the chalcone scaffold have been perceived to play an imperative function in interacting with molecular targets (receptor, enzyme, and/or channel) to express the biological responses. In the majority of the studies, the overall activity of the ligand administered as pharmaceutically acceptable salt is found to be better than that of standard marketed drug preparation. The article will certainly attract (medicinal)-chemists actively involved in the development of therapeutically active scaffolds.
机译:介绍:Chalcone或苄基苯二酮或1,3-二苯基-2-丙烯-1-1是包含由三碳α,β不饱和羰基桥连接在一起的两个芳环的天然产物。它是药物化学中最特权的支架之一,可以在实验室中合成,并且可以转化为几种治疗活性的杂环支架。它表现出多种的药理学活动,并在几种非药理学科学应用中起着关键作用。所涵盖的地区:本文在2014 - 2018年期间全面地专注于批准的专利,这些专利在各种药理学活动中的各种Chalcone分子上。专家意见:该研究提出了基于抗增殖,抗糖尿病,抗感染性,抗炎,抗氧化剂,抗衰老,神经保护剂和心脏保护剂的最新更新的疗效治疗应用。已经感知在Chalcone支架上存在的类型,位置和替代物的数量,以发挥与分子靶标(受体,酶和/或通道)相互作用以表达生物反应的命令函数。在大多数研究中,发现作为药学上可接受的盐的配体的总体活性比标准销售药物制剂更好。这篇文章肯定会吸引(药用) - 深思熟虑地参与治疗活性支架的发展。

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