The significant step in antiviral therapy development was the introduction of ribavirin ({1-(β-D-ribofuranosyl)-1H-1,2,4 -triazole-3-carboxamide}) into medical practice. This small and simple, from structural point of view, molecule appeared to have extremely wide antiviral activity spectrum, both in relation to DNA-viruses [1, 2] and RNA-viruses [3-8]. It is known, that ribavirin influences the activeness of many enzymes, like inosine monophosphate dehydrogenases and viral RNA-polymerases [9, 10]. The inhibition of these enzymes causes blocking viral replication. It was obvious that 1,2,4-triazole scaffold, contained in the molecule, influences pharmacological properties of ribavirin. The result of the above observation was numerous research concerning the use of triazole structure in other antiviral drugs [11-13]. 

General structure of synthesized compounds

Taking into consideration the pharmacological usefulness of 1,2,4-triazole moiety for antiviral activity, we decided to investigate the antiviral properties of our newly-synthesized compounds in relation to DNA-virus (Adenovirus-5) and RNA-virus (ECHO-9-virus).Antiviral and virucidal activity of the title compounds was examined only at concentrations that were non-toxic for HEK-293 and GMK cells. Evaluation of virucidal activity showed that only compound without substituents at amide nitrogen was totally inactive against human adenovirus type 5. Other compounds caused the decrease in the titres of viruses by 0.44-1.56 log (24%-48%). All the tested triazole derivatives affirmed virucidal activity towards ECHO-9 virus.

[1] R. W. Sidwell, J. H. Huffman, G. P. Khare, L. B. Allen, J. T. Witkowski, R. K. Robins, Science 177 (1972) 705-706. [2] W. Markland, T. J. McQuaid, J. Jain, A. D. Kwong, Antimicrob. Agents Chemother. 44 (2000) 859-866.[3] J. F. Hruska, J. M. Bernstein, R. G. Jr. Douglas, C. B. Hall, Antimicrob. Agents Chemother. 17 (1980) 770-775.[4] J. Neyts, A. Meerbach, P. McKenna, E. De Clercq, Antiviral Res. 30 (1996) 125-132.[5] I. Jordan, T. Briese, N. Fischer, J. Y. Lau, W. I. Lipkin, J. Infect. Dis. 182 (2000) 1214-1217.[6] S. Crotty, D. Maag, J. J. Arnold, W. Zhong, J. Y. Lau, Z. Hong, R. Andino, C. E. Cameron, Nat. Med. 6 (2000) 1375-1379.[7] J. S. Oxford, Gen. Virol. 28 (1975) 409-414.[8] G. Andrei, E. De Clercq, Antiviral Res. 14 (1990) 287-299.[9] S. Crotty, C. Cameron, R. Andino, J. Mol. Med. 80 (2002) 86-95.[10] W. B. Parker, Virus Res. 107 (2005) 165-171.[11] R. Zhu, M. Wang, Y. Xia, F. Qu, J. Neyts, L. Peng, Bioorg. Med. Chem. Lett. 18 (2008) 3321-3327.[12] T. A. Kirschberg, M. Balakrishnan, N. Huang, R. Hluhanich, N. Kutty, A. C. Liclican, D. J. McColl,N. H. Squires, E. B. Lansdon, Bioorg. Med. Chem. Lett. 18 (2008) 1131-1134.[13] I. Küçükgüzel, E. Tatar, Ş. G. Küçükgüzel, S. Rollas, E. De Clercq, Eur. J. Med. Chem. 43 (2008) 381-392.

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