1,2,3-三唑基核苷类似物同二聚体的合成和抗病毒活性

IF 1.7 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Russian Chemical Bulletin Pub Date : 2024-07-26 DOI:10.1007/s11172-024-4296-5

O. V. Andreeva, M. M. Shulaeva, L. F. Saifina, B. F. Garifullin, M. G. Belenok, V. V. Zarubaev, A. V. Slita, V. E. Semenov, V. E. Kataev

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引用次数: 0

摘要

合成了基于 6-甲基尿嘧啶的 1,2,3-三唑基核苷类似物的新同源二聚体，这些类似物在 N(1) 或 N(3) 原子上由聚亚甲基连接体连接。通过对甲型 H1N1 流感病毒和柯萨奇病毒 B3 的体外抗病毒活性进行筛选，发现了一种体外抑制柯萨奇病毒 B3 复制的先导化合物，其半最大抑制浓度（IC50）和半最大细胞毒性浓度（CC50）分别为 30.1 µmol L-1 和 374 µmol L-1。研究发现，抗病毒活性取决于连接 6-甲基尿嘧啶和 1,2,3-三唑基-β-d-呋喃核糖基片段的聚亚甲基连接体的长度。

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Synthesis and antiviral activity of homodimers of 1,2,3-triazolyl nucleoside analogs

New homodimers of 1,2,3-triazolyl nucleoside analogs based on 6-methyluracil, which are linked by the polymethylene linker at the N(1) or N(3) atoms, were synthesized. Screening of in vitro antiviral activity against influenza A virus (H1N1) and Coxsackievirus B3 revealed the lead compound that in vitro inhibited the replication of Coxsackievirus B3 with a half-maximal inhibitory concentration (IC₅₀) and a half-maximal cytotoxic concentration (CC₅₀) of 30.1 and >374 µmol L⁻¹, respectively. A dependence of the antiviral activity on the length of the polymethylene linker connecting the 6-methyluracil and 1,2,3-triazolyl-β-d-ribofuranosyl fragments was found.

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来源期刊

Russian Chemical Bulletin 化学-化学综合

CiteScore

2.70

自引率

47.10%

发文量

257

审稿时长

3-8 weeks

期刊介绍： Publishing nearly 500 original articles a year, by leading Scientists from Russia and throughout the world, Russian Chemical Bulletin is a prominent international journal. The coverage of the journal spans practically all areas of fundamental chemical research and is presented in five sections: General and Inorganic Chemistry; Physical Chemistry; Organic Chemistry; Organometallic Chemistry; Chemistry of Natural Compounds and Bioorganic Chemistry.