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Antiadenovirus Activity of New Fluorine-containing Polypeptides Mimetics
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1  D.K. Zabolotny Institute of Microbiology and Virology of the NAS of Ukraine

Published: 01 November 2017 by MDPI in 3rd International Electronic Conference on Medicinal Chemistry session ECMC-3

 More than 60 serotypes cause a variety of courses and severe clinical signs of infectious diseases. However, there is no specific drug for the treatment of adenoviral diseases. Fluorinated nucleoside sugars chemistry became the basis for the development of promising chemotherapeutic agents with antitumor and antiviral effects. Based on the purine and pyrimidine nucleotide analogs and fluorinated heterocycle molecules a new generation of drugs with anticancer effect was developed.

The reference strain of human adenovirus serotype 5 and monolayer cell line MDBK were used in the experiment. We studied new fluorine-containing compounds 10S-25 (1-S-thio-(1-methylsulfonyl-2-difluoromethyl-vinyl)-2,3,4,6,-tetra-O-acetyl-β-D-glucopyranose), 10S-26 ((S)-2-(ethoxydifluoromethyl)-pyrrolidine hydrochloride), 10S-27(1-(β-D-glucopyranosyl)-4-(hexafluoropropyl)-5-tosyl-1H-1,2,3-triazole),  10S-28 (Dimethyl N,N'-(2,2-difluoropropanedithioyl)bis(L-alaninate)), synthesized in Institute of Organic Chemistry of the NAS of  Ukraine. Antiviral activity and the effect on adenovirus synthesized de novo were investigated.

Cytotoxicity of experimental compounds was within 16 - 637 μg/ml. Antiviral activity was maximal for compound 10S-27 in the concentration of 16 μg/ml (36%). Other experimental compounds had less antiviral activity at all concentrations. However, they had a significant influence on the synthesis of viral offspring. The percentage of virus inhibition titer was in the range of 65-92%. Consequently, the experimental compounds affected the formation of the infectious viral offspring.

Keywords: adenovirus, fluorine-containing compounds, antiviral activity