| Autor: |
Garifullin BF; Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.; Kazan National Research Technological University, Kazan, Russian Federation., Khabibulina LR; Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation.; Kazan National Research Technological University, Kazan, Russian Federation., Belenok MG; Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation., Saifina LF; Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation., Zarubaev VV; Pasteur Institute of Epidemiology and Microbiology, Saint Petersberg, Russian Federation., Slita AV; Pasteur Institute of Epidemiology and Microbiology, Saint Petersberg, Russian Federation., Volobueva AS; Pasteur Institute of Epidemiology and Microbiology, Saint Petersberg, Russian Federation., Semenov VE; Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation., Kataev VE; Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russian Federation. |
| Abstrakt: |
A series of 1,2,3-triazolyl nucleoside analogues bearing N -acetyl-D-glucosamine residue was synthesized by the copper-catalyzed alkyne-azide cycloaddition (CuAAC) reaction of N 1-ω-alkynyl derivatives of uracil, 6-methyluracil, thymine and 3,4,6-tri- O -acetyl-2-deoxy-2-acetamido-β-D-glucopyranosyl azide. Antiviral assays revealed the lead compound 3f which showed both the same activity against the influenza virus A H1N1 (IC 50 =70.7 µM) as the antiviral drug Rimantadine in control (IC 50 =77 µM) and good activity against Coxsackievirus B3 (IC 50 =13.9 µM) which was one and a half times higher than the activity of the antiviral drug Pleconaril in control (IC 50 =21.6 µM). According to molecular docking simulations, the antiviral activity of the lead compound 3f against Coxsackie B3 virus can be explained by its binding to a key fragment of the capsid surface of this virus. |
