新型1,2,4-三唑衍生物中不同功能取代基对化合物生物学性质影响的研究综述

М. В. Оглобліна, І. В. Бушуєва, В. В. Парченко
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引用次数: 0

摘要

目前,1,2,4-三唑衍生物是一类很有前途的有机化合物。这首先是由于典型药效团的加入可能导致1,2,4-三唑片段发生各种化学修饰,这有助于扩大新分子的武器库。大量1,2,4-三唑衍生物显示出生物学特性,这对最有希望的物质的进一步引入产生了积极的影响。本研究的目的是分析1,2,4-三唑类新衍生物的各种功能取代基对上述化合物生物活性指标的影响。含有1,2,4-三唑类新衍生物的各种功能取代基对这些化合物生物活性指标影响的文献来源成为研究材料。工作中采用的方法有:分析法、文献语义信息检索法、泛化法。三唑及其杂环类似物是在其组成中含有一定量的氮原子的化合物,具有典型的药效团的性质。它们的衍生物很容易合成,并可转化为各种生物活性分子。本文对1,2,4-三唑衍生物的化学模型进行了分析和总结,该模型允许有目的地获得具有必要生物学特性的化合物,同时考虑到新分子的毒性指标。作者已经证明,在1,2,4-三唑衍生物分子中逐渐和预期地引入各种取代基,导致新的生物活性类型的出现,在某些情况下,它使已有的活性指标增加。由于取代基在1,2,4-三唑片段周围的变化而引起的化合物的修饰从根本上改变了新分子的生物活性类型。这种方法被大多数科学家认为是在1,2,4-三唑衍生物中寻找新的生物活性物质的一种有希望的方法。这些研究的优先性、相关性和前景不仅得到了国内科学家团队的证明。近年来,来自土耳其、印度、韩国、中国、埃及等国的研究人员在1,2,4-三唑类衍生物中积极寻找新的生物活性物质。通过对现代文献资料对新型1,2,4-三唑衍生物生物活性研究的分析,确立了各种功能取代基对生物活性类型影响的某些特征,并有力地证明了该化合物指定系列的进一步合成试验的前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Review of the research on the influence of different functional substituents of new 1,2,4-triazole derivatives on the compounds biological properties
Today, 1,2,4-triazole derivatives are a promising class of organic compounds. This is caused, first of all, by the possibility of various chemical modifications of the 1,2,4-triazole fragment due to the addition of typical pharmacophores, which contributes to the expansion of the new molecules’ arsenal. A significant number of the 1,2,4-triazole derivatives show biological properties, that postively affects the further process of the most promising substances’ introduction. The aim of the work was to analyze the influence of various functional substituents of the new 1,2,4-triazole derivatives on the indicators of the mentioned compounds’ biological activity. Literature sources containing information on the influence of various functional substituents of the new 1,2,4-triazole derivatives on the indicators of these compounds’ biological activity became the research materials. Methods were used in the work: analytical, bibliosemantic information search, generalization. Triazoles and their heterocyclic analogues are compounds that contain a certain amount of Nitrogen atoms in their composition, showing the properties of typical pharmacophores. Their derivatives are easily synthesized and can be transformed into various biologically active molecules. Information on the 1,2,4-triazole derivatives’ chemical modeling, which allows for purposefully obtaining compounds with the necessary biological properties, taking into account the toxicity indicators of new molecules, has been analyzed and summarized. The authors have proved, that the gradual and predicted introduction of various substituents into the molecule of 1,2,4-triazole derivatives leads to the appearance of new types of biological activity, in some cases it gives an increase in already existing activity indicators. Chemical compounds’ modification due to the substituents’ changing around the 1,2,4-triazole fragment fundamentally changes the type of biological activity of new molecules. This approach was chosen by the majority of scientists as promising one for the new biologically active substances’ search among the 1,2,4-triazole derivatives. The priority, relevance and perspective of such researches have been proved by not only domestic scientists’ teams. Recently, foreign investigators from Turkey, India, Korea, China, Egypt, etc. have been actively searching for new biologically active substances among the 1,2,4-triazole derivatives. The analysis of modern literary sources on the study of the new 1,2,4-triazole derivatives’ biological activity allows us to establish certain features of the various functional substituents’ influence on the types of biological activity and convincingly proves the outlook of further synthetic tests in the compounds’ specified series.
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