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Spectrum of antiviral activity of 4-aminopyrimidine N-oxides against a broad panel of tick-borne encephalitis virus strains.


ABSTRACT: Tick-borne encephalitis is an important human arbovirus neuroinfection spread across the Northern Eurasia. Inhibitors of tick-borne encephalitis virus (TBEV) strain Absettarov, presumably targeting E protein n-octyl-?-d-glucoside (?-OG) pocket, were reported earlier. In this work, these inhibitors were tested in vitro against seven strains representing three main TBEV subtypes. The most potent compound, 2-[(2-methyl-1-oxido-5,6,7,8-tetrahydroquinazolin-4-yl)amino]-phenol, showed EC50 values lower than 22?µM against all the tested strains. Nevertheless, EC50 values for virus samples of certain strains demonstrated a substantial variation, which appeared to be consistent with the presence of E protein not only in infectious virions, but also in non-infectious and immature virus particles, protein aggregates, and membrane complexes.

SUBMITTER: Dueva EV 

PROVIDER: S-EPMC7545520 | biostudies-literature | 2020 Jan-Dec

REPOSITORIES: biostudies-literature

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Spectrum of antiviral activity of 4-aminopyrimidine <i>N</i>-oxides against a broad panel of tick-borne encephalitis virus strains.

Dueva Evgenia V EV   Tuchynskaya Ksenia K KK   Kozlovskaya Liubov I LI   Osolodkin Dmitry I DI   Sedenkova Kseniya N KN   Averina Elena B EB   Palyulin Vladimir A VA   Karganova Galina G GG  

Antiviral chemistry & chemotherapy 20200101


Tick-borne encephalitis is an important human arbovirus neuroinfection spread across the Northern Eurasia. Inhibitors of tick-borne encephalitis virus (TBEV) strain Absettarov, presumably targeting E protein <i>n</i>-octyl-β-d-glucoside (β-OG) pocket, were reported earlier. In this work, these inhibitors were tested <i>in vitro</i> against seven strains representing three main TBEV subtypes. The most potent compound, 2-[(2-methyl-1-oxido-5,6,7,8-tetrahydroquinazolin-4-yl)amino]-phenol, showed EC  ...[more]

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