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Design, synthesis, and antiviral activity of novel ribonucleosides of 1,2,3-triazolylbenzyl-aminophosphonates

机译:1,2,3-三唑基苄基氨基膦酸酯的新型核糖核苷的设计,合成和抗病毒活性

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摘要

A novel series of ribonucleosides of 1,2,3-triazolylbenzyl-aminophosphonates was synthesized through the Kabachnik-Fields reaction using I2 as catalyst followed by copper-catalyzed cycloaddition of the azide-alkyne reaction (CuAAC). All structures of the newly prepared compounds were characterized by (1) H NMR, (13) C NMR, and HRMS spectra. The structures of 2e, 2f, 3d, and 3g were further confirmed by X-ray diffraction analysis. These compounds were tested against various strains of DNA and RNA viruses; compounds 4b and 4c showed a modest inhibitory activity against respiratory syncytial virus (RSV) and compound 4h displayed modest inhibitory activity against Coxsackie virus B4.
机译:通过Kabachnik-Fields反应,使用I 2作为催化剂,然后通过铜催化的叠氮化物-炔反应(CuAAC)的环加成反应,合成了一系列1,2,3-三唑基苄基-氨基膦酸酯的核糖核苷。通过(1)1 H NMR,(13)C NMR和HRMS光谱表征新制备的化合物的所有结构。通过X射线衍射分析进一步证实了2e,2f,3d和3g的结构。测试了这些化合物对各种DNA和RNA病毒的抵抗力;化合物4b和4c显示对呼吸道合胞病毒(RSV)的适度抑制活性,化合物4h显示对柯萨奇病毒B4的适度抑制活性。

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