Synthesis and Antiviral Activity of Homodimers of 1,2,3-Triazolyl Nucleoside Analogues Based on Quinazoline-2,4-dione

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发表日期：

2024年5月1日

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

摘要

Abstract

By covalent binding of 1,2,3-triazolyl nucleoside analogues by a polymethylene chain at the N³ atoms, a series of homodimers was synthesized, in which nucleic bases are replaced by quinazoline-2,4-dione moieties connected to the β-D-ribofuranose residues by 1,2,3-triazolylbutyl linkers. Screening of in vitro antiviral activity against influenza A (H1N1) and Coxsackie B3 viruses revealed a lead compound that showed high antiviral activity (IC₅₀ = 11.6 μM) against influenza A/Puerto Rico/8/34 (H1N1) virus and a lead compound that exhibited high antiviral activity (IC₅₀ = 12.2 μM) against enterovirus Coxsackie B3.