Synthesis and Comparative Study of Anti-Adenoviral Activity of 6-Azacytidine and Its Analogues |
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| Authors: | Inna Alexeeva Lydia Nosach Larisa Palchykovska Lyubov Usenko Olga Povnitsa |
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| Affiliation: | 1. Institute of Molecular Biology and Genetics, National Academy of Sciences, Kyiv, Ukraine i.v.alexeeva@imbg.org.ua;3. D.K. Zabolotny Institute of Microbiology and Virology, National Academy of Sciences, Kyiv, Ukraine;4. Institute of Molecular Biology and Genetics, National Academy of Sciences, Kyiv, Ukraine |
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| Abstract: | This paper presents the results of synthesis and study of cytotoxicity and the anti-adenoviral activity of new N4-derivatives of 6-azacytidine and its α-L-glycopyranosyl analogues obtained by the simplified one-pot version of the silyl condensation method. The resulting acylated 4-methylmercapto-1,2,4-triazin-3(2Н)-one glycosides then underwent the amination and/or ammonolysis to provide 6-azacytidine glycoside analogues (2–6, 12, 15, 17) and compounds with modifications at both base and sugar fragments (11, 15). The evaluation of cytotoxicity and antiviral activity of new compounds against AdV5 showed high selectivity indexes for N4-methyl-6-azacytidine (2) and N,O-tetraacetyl-6-azacytidine (8). High anti-adenoviral activity of N4-methyl-6-azacytidine as well as very low cytotoxicity may suggest its further investigation as potential compound for the therapy of AdV infection. |
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| Keywords: | 6-azacytidine nucleoside analogues human adenovirus antiviral agents |
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