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Article

Simplistic perylene-related compounds as inhibitors of tick-borne encephalitis virus reproduction

Bioorganic and Medicinal Chemistry Letters. 2020. Vol. 30. No. 10. P. 127100.
Slesarchuk N. A., Khvatov E. V., Chistov A. A., Proskurin G. V., Nikitin T. D., Lazarevich A. I., Ulanovskaya A. A., Ulashchik E. A., Orlov A. A., Jegorov A. V., Ustinov A. V., Tyurin Anton P., Shmanai V. V., Ishmukhametov A. A., Korshun V. A., Osolodkin D. I., Kozlovskaya L. I., Aralov A. V.

Rigid amphipathic fusion inhibitors are potent broad-spectrum antivirals based on the perylene scaffold, usually decorated with a hydrophylic group linked via ethynyl or triazole. We have sequentially simplified these structures by removing sugar moiety, then converting uridine to aniline, then moving to perylenylthiophenecarboxilic acids and to perylenylcarboxylic acid. All these polyaromatic compounds, as well as antibiotic heliomycin, still showed pronounced activity against tick-borne encephalitis virus (TBEV) with limited toxicity in porcine embryo kidney (PEK) cell line. 5-(Perylen-3-yl)-2-thiophenecarboxylic acid (5a) showed the highest antiviral activity with 50% effective concentration of approx. 1.6 nM.