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含 1,2,3-三唑的杂合体作为药物化学中的先导化合物:最新概述。

1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview.

机构信息

Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, 40-1 South Beijing Rd, Urumqi 830011, PR China; Institute of the Chemistry of Plant Substances, Academy of Sciences of Uzbekistan, Mirzo Ulugbek Str. 77, Tashkent 100170, Uzbekistan.

Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, 40-1 South Beijing Rd, Urumqi 830011, PR China.

出版信息

Bioorg Med Chem. 2019 Aug 15;27(16):3511-3531. doi: 10.1016/j.bmc.2019.07.005. Epub 2019 Jul 4.

Abstract

The 1,2,3-triazole ring is a major pharmacophore system among nitrogen-containing heterocycles. These five-membered heterocyclic motifs with three nitrogen heteroatoms can be prepared easily using 'click' chemistry with copper- or ruthenium-catalysed azide-alkyne cycloaddition reactions. Recently, the 'linker' property of 1,2,3-triazoles was demonstrated, and a novel class of 1,2,3-triazole-containing hybrids and conjugates was synthesised and evaluated as lead compounds for diverse biological targets. These lead compounds have been demonstrated as anticancer, antimicrobial, anti-tubercular, antiviral, antidiabetic, antimalarial, anti-leishmanial, and neuroprotective agents. The present review summarises advances in lead compounds of 1,2,3-triazole-containing hybrids, conjugates, and their related heterocycles in medicinal chemistry published in 2018. This review will be useful to scientists in research fields of organic synthesis, medicinal chemistry, phytochemistry, and pharmacology.

摘要

1,2,3-三氮唑环是含氮杂环中主要的药效团系统。这些具有三个氮杂原子的五元杂环可以通过铜或钌催化的叠氮-炔烃环加成反应的“点击”化学轻松制备。最近,1,2,3-三唑的“连接子”性质得到了证明,并合成了一类新型的含 1,2,3-三唑的杂合体和缀合物,并将其作为针对各种生物靶标的先导化合物进行了评估。这些先导化合物已被证明具有抗癌、抗菌、抗结核、抗病毒、抗糖尿病、抗疟疾、抗利什曼病和神经保护作用。本综述总结了 2018 年在药物化学中发表的含 1,2,3-三唑的杂合体、缀合物及其相关杂环的先导化合物的进展。这篇综述将对有机合成、药物化学、植物化学和药理学等研究领域的科学家有用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/91d4/7185471/821038ed7715/ga1_lrg.jpg

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