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

机译:查尔酮衍生物治疗应用的最新专利审查(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:简介:查尔酮或亚苄基苯乙酮或1,3-二苯基-2-丙烯-1-酮是一种天然产物,由两个通过三碳α,β不饱和羰基桥连接的芳环组成。它是医学化学中最优先的支架之一,可以在实验室中合成,并且可以转化为几种具有治疗活性的杂环支架。它具有多种药理活性,并且在几种非药理科学应用中也起着关键作用。涵盖领域:本文主要针对2014-2018年期间具有不同药理活性的各种查尔酮分子的已批准专利。专家意见:该研究提出了查尔酮类化合物的最新治疗应用,包括抗增殖,抗糖尿病,抗感染,抗炎,抗氧化剂,抗衰老,神经保护剂和心脏保护剂。查尔酮骨架上存在的取代基的类型,位置和数量被认为在与分子靶标(受体,酶和/或通道)相互作用以表达生物学反应中起着必不可少的作用。在大多数研究中,发现以药学上可接受的盐形式施用的配体的总体活性优于标准市售药物制剂的总体活性。本文肯定会吸引积极参与治疗活性支架开发的(药物)化学家。

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