Synthesis and antiviral activity of homodimers of 1,2,3-triazolyl nucleoside analogs

New homodimers of 1,2,3-triazolyl nucleoside analogs based on 6-methyluracil, which are linked by the polymethylene linker at the N(1) or N(3) atoms, were synthesized. Screening of in vitro antiviral activity against influenza A virus (H1N1) and Coxsackievirus B3 revealed the lead compound that in v...

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Veröffentlicht in:Russian chemical bulletin 2024-06, Vol.73 (6), p.1789-1800
Hauptverfasser: Andreeva, O. V., Shulaeva, M. M., Saifina, L. F., Garifullin, B. F., Belenok, M. G., Zarubaev, V. V., Slita, A. V., Semenov, V. E., Kataev, V. E.
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Sprache:eng
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Zusammenfassung:New homodimers of 1,2,3-triazolyl nucleoside analogs based on 6-methyluracil, which are linked by the polymethylene linker at the N(1) or N(3) atoms, were synthesized. Screening of in vitro antiviral activity against influenza A virus (H1N1) and Coxsackievirus B3 revealed the lead compound that in vitro inhibited the replication of Coxsackievirus B3 with a half-maximal inhibitory concentration (IC 50 ) and a half-maximal cytotoxic concentration (CC 50 ) of 30.1 and >374 µmol L −1 , respectively. A dependence of the antiviral activity on the length of the polymethylene linker connecting the 6-methyluracil and 1,2,3-triazolyl-β- d -ribofuranosyl fragments was found.
ISSN:1066-5285
1573-9171
DOI:10.1007/s11172-024-4296-5