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 IC50 between 23–48 μM. In addition, carbazoyl‐aryl‐ureas also proved to inhibit ZIKV replication activity at micromolar concentration.
Highlights
The recent outbreaks of Zika virus (ZIKV) infection worldwide make the discovery of novel antivirals against flaviviruses a research priority
Zika virus (ZIKV)[1,2] is a single positive-strand RNA mosquitoborne pathogen belonging to the family of Flaviviridae, genus
Was declared by the World Health Organization (WHO) as a Public Health Emergency of International Concern (PHEIC) and the first case of sexually-transmitted ZIKV was reported in USA
Summary
To cite this version: 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. Sharon Spizzichino,[a, b] Giulio Mattedi,[a] Kate Lauder,[a] Coralie Valle,[c] Wahiba Aouadi,[c]. The recent outbreaks of Zika virus (ZIKV) infection worldwide make the discovery of novel antivirals against flaviviruses a research priority. Carbazoyl-aryl-ureas proved to inhibit ZIKV replication activity at micromolar concentration. Zika virus (ZIKV)[1,2] is a single positive-strand RNA mosquitoborne pathogen belonging to the family of Flaviviridae, genus. Flavivirus and it causes mild-severe diseases in humans and animals.
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