STUDY OF ANTIADENOVIRALACTIVITY OF NEW FLUORINECONTAINING HETEROCYCLIC COMPOUNDS

Abstract

Purpose: To study the cytotoxic action and antiviral activity of new fluorinated nucleoside compounds on human adenovirus model and the role of individual molecular fragments in their activity. Methods. Cytotoxic activity of the compounds was determined by the MTT method. Antiviral activity of substances was studied using cyto-morphological method with acridine orange dye. The virus-specific intranuclear inclusions were determined. Results. In present study the cytotoxicity of 2N-substituted-4-tosyl-5-polyfluoroalkyl-1,2,3-triazoles for Hep-2 and Hela cell lines were studied. The dependence of cytotoxicity on the compounds in the structure of substituents in the aromatic rings of the molecules was defined. Combination of residues of 3-hlorotetrahydropyran, 3-chloro-dihydrofuran tetrahydrofuran in a glycosidic moiety with trifluoromethyl or perfluoropropyl in a triazole ring were more toxic. Antiviral activity of 3 compounds (G7, G8 and G10) against HAdV5 in vitro was revealed. The effective antiviral concentrations (EC50) for them were 16, 70 and 186 mg/ml, and the selectivity indexes were equal to 91, 8 and 4, respectively. Conclusions. High rates of antiviral activity and low cytotoxicity of G8 compound make it perspective for development antiviral agents.

Keywords

• фторовмісні нуклеозиди
• аденовірус
• антивірусна активність