Abstract
Background: 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, it 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 crossresistance to other existing anti-influenza drugs.
Objective: To develop new analogs, a class of 1,3-oxathiolane nucleoside derivatives of T-705 was 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 µmol/L. Compound 1b showed weak activity against HIV with a viral suppression rate of 70-80% at 30 µmol/L.
Conclusion: A class of 1,3-oxathiolane nucleoside derivatives of T-705 was designed and synthesized, and one of them was identified as a novel scaffold against viral infection.
Keywords: Nucleotide analog, favipiravi, anti-influenza, anti-HIV, 1, 3-oxathiolane nucleoside, viral enzymes.
Graphical Abstract
Medicinal Chemistry
Title: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
Volume: 14 Issue: 6
Author(s): Mingming Han, Xu Zhao, Xuedong Wu, Wei Huang, Xingzhou Li*Fang Yu*
Affiliation:
- Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing 100850,China
- College of Chemistry, Chemical Engineering and Environmental Engineering, Liaoning Shihua University, Fushun 113001,China
Keywords: Nucleotide analog, favipiravi, anti-influenza, anti-HIV, 1, 3-oxathiolane nucleoside, viral enzymes.
Abstract: Background: 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, it 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 crossresistance to other existing anti-influenza drugs.
Objective: To develop new analogs, a class of 1,3-oxathiolane nucleoside derivatives of T-705 was 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 µmol/L. Compound 1b showed weak activity against HIV with a viral suppression rate of 70-80% at 30 µmol/L.
Conclusion: A class of 1,3-oxathiolane nucleoside derivatives of T-705 was designed and synthesized, and one of them was identified as a novel scaffold against viral infection.
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Cite this article as:
Han Mingming , Zhao Xu, Wu Xuedong, Huang Wei , Li Xingzhou*, Yu Fang *, 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, Medicinal Chemistry 2018; 14 (6) . https://dx.doi.org/10.2174/1573406414666180112102225
DOI https://dx.doi.org/10.2174/1573406414666180112102225 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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