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Med Chem. 2018 Jan 11. doi: 10.2174/1573406414666180112102225. [Epub ahead of print]
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.
Han M1, Zhao X2, Wu X3, Huang W1, Li X2, Yu F1.
Author information
Abstract
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.
OBJECTIVE:
To develop new analogs, a class of 1,3-oxathiolane nucleoside derivatives of T-705 were designed and synthesized in this work.
RESULTS:
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.
CONCLUSION:
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.
KEYWORDS:
1; 3-oxathiolane nucleoside.; Nucleotide analog; anti-HIV; anti-influenza; favipiravi
PMID: 29332597 DOI: 10.2174/1573406414666180112102225
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.
Han M1, Zhao X2, Wu X3, Huang W1, Li X2, Yu F1.
Author information
Abstract
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.
OBJECTIVE:
To develop new analogs, a class of 1,3-oxathiolane nucleoside derivatives of T-705 were designed and synthesized in this work.
RESULTS:
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.
CONCLUSION:
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.
KEYWORDS:
1; 3-oxathiolane nucleoside.; Nucleotide analog; anti-HIV; anti-influenza; favipiravi
PMID: 29332597 DOI: 10.2174/1573406414666180112102225