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Design, Synthesis and Discovery of N,N’ ‐Carbazoyl‐aryl‐urea Inhibitors of Zika NS5 Methyltransferase and Virus Replication

Abstract : The recent outbreaks of Zika virus (ZIKV) infection worldwide make the discovery of novel antivirals against flaviviruses a research priority. This work describes the identification of novel inhibitors of ZIKV through a structure-based virtual screening approach using the ZIKV NS5-MTase. A novel series of molecules with a carbazoyl-aryl-urea structure has been discovered and a library of analogues has been synthesized. The new compounds inhibit ZIKV MTase with IC 50 between 23-48 μM. In addition, carbazoyl-aryl-ureas also proved to inhibit ZIKV replication activity at micromolar concentration.
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https://hal.archives-ouvertes.fr/hal-02890596
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Submitted on : Tuesday, July 7, 2020 - 8:35:37 AM
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Long-term archiving on: : Friday, November 27, 2020 - 12:03:30 PM

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Sharon Spizzichino, Giulio Mattedi, Kate Lauder, Coralie Valle, Wahiba Aouadi, et al.. Design, Synthesis and Discovery of N,N’ ‐Carbazoyl‐aryl‐urea Inhibitors of Zika NS5 Methyltransferase and Virus Replication. ChemMedChem, Wiley-VCH Verlag, 2020, 15 (4), pp.385-390. ⟨10.1002/cmdc.201900533⟩. ⟨hal-02890596⟩

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