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Synthesis of a Novel Class of 1,3-oxathiolane Nucleoside Derivatives of T-705 and Evaluation of Their Anti-influenza A Virus and Anti-HIV Activity

tetano

Editor, Senior Moderator
Med Chem. 2018 Jan 11. doi: 10.2174/1573406414666180112102225. [Epub ahead of print]
[h=1]Synthesis of a Novel Class of 1,3-oxathiolane Nucleoside Derivatives of T-705 and Evaluation of Their Anti-influenza A Virus and Anti-HIV Activity.[/h] Han M[SUP]1[/SUP], Zhao X[SUP]2[/SUP], Wu X[SUP]3[/SUP], Huang W[SUP]1[/SUP], Li X[SUP]2[/SUP], Yu F[SUP]1[/SUP].
[h=3]Author information[/h]

[h=3]Abstract[/h] Backgroud: T-705 (Favipiravir) is a broad spectrum antiviral agent approved for stockpiling in Japan and currently in Phase 3 testing in the United States. Against influenza acts as a prodrug, converted intracellularly to selectively inhibit viral RNA-dependent RNA polymerase or similar enzymes. This is regarded as a novel antiviral mechanism of action, reducing cross-resistance to other existing anti-influenza drugs.
[h=4]OBJECTIVE:[/h] To develop new analogs, a class of 1,3-oxathiolane nucleoside derivatives of T-705 were designed and synthesized in this work.
[h=4]RESULTS:[/h] Anti-influenza activity and Anti-HIV activity of these compounds were evaluated. Compound 1a displayed activity against A H1N1 with an IC50 of 40.4 ?mol/L. Compound 1b showed weak activity against HIV with a viral suppression rate of 70-80% at 30 ?mol/L.
[h=4]CONCLUSION:[/h] A class of 1,3-oxathiolane nucleoside derivatives of T-705 were designed and synthesized, one of them was identified as a novel scaffold against viral infection.
Copyright? Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.


[h=4]KEYWORDS:[/h] 1; 3-oxathiolane nucleoside.; Nucleotide analog; anti-HIV; anti-influenza; favipiravi

PMID: 29332597 DOI: 10.2174/1573406414666180112102225
 
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