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

Research output: Contribution to journalArticle

Original languageEnglish
Pages (from-to)385-390
Number of pages6
JournalChemmedchem
Volume15
Issue number4
DOIs
Accepted/In press5 Dec 2019
Published17 Feb 2020

Documents

  • Final draft_0411

    Final_draft_0411.docx, 22 MB, application/vnd.openxmlformats-officedocument.wordprocessingml.document

    Uploaded date:06 Dec 2019

    Version:Accepted author manuscript

King's Authors

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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