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Design Synthesis and Antiviral Activity of Novel Ribonucleosides of 123‐Triazolylbenzyl‐aminophosphonates

机译:123-三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 1H NMR, 13C 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:通过使用I2作为催化剂的Kabachnik-Fields反应,然后通过铜催化的叠氮化物-炔烃反应(CuAAC),合成了一系列新的1,2,3-三唑基苄基氨基膦酸酯核糖核苷。新制备的化合物的所有结构均通过 1 1 H NMR, 13 C NMR和HRMS光谱表征。 X射线衍射分析进一步确定了> 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 对呼吸道合胞病毒(RSV)表现出适度的抑制活性,化合物> 4h 对柯萨奇病毒B4表现出适度的抑制活性。

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