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

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发表日期：

2024年6月1日

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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

摘要

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.