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3-(Benzodioxan-2-ylmethoxy)-2,6-difluorobenzamides bearing hydrophobic substituents at the 7-position of the benzodioxane nucleus potently inhibit methicillin-resistant Sa and Mtb cell division

  • Valentina Straniero
  • , Marco Pallavicini
  • , Giuseppe Chiodini
  • , Carlo Zanotto
  • , Luca Volontè
  • , Antonia Radaelli
  • , Cristiano Bolchi
  • , Laura Fumagalli
  • , Maurizio Sanguinetti
  • , Giulia Menchinelli
  • , Giovanni Delogu
  • , Basem Battah
  • , Carlo De Giuli Morghen
  • , Ermanno Valoti
  • University of Milan

Research output: Contribution to journal › Article › peer-review

Abstract

Lipophilic substituents at benzodioxane C (7) of 3-(benzodioxan-2-ylmethoxy)-2,6-difluorobenzamide improve the antibacterial activity against methicillin-resistant Staphylococcus aureus strains to MIC values in the range of 0.2-2.5 μg/mL, whereas hydrophilic substituents at the same position and modifications at the benzodioxane substructure, excepting for replacement with 2-cromanyl, are deleterious. Some of the lead compounds also exhibit good activity against Mtb. Parallel SARs to those of 3-(2-benzothiazol-2-ylmethoxy)-2,6-difluorobenzamide, well known FtsZ inhibitor, and cells alterations typical of FtsZ inhibition indicate such a protein as the target of these potent antibacterial benzodioxane-benzamides.
Original languageEnglish
Pages (from-to)227-243
Number of pages17
JournalEuropean Journal of Medicinal Chemistry
Volume120
DOIs
Publication statusPublished - 2016

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

Keywords

  • 2,6-Difluorobenzamide
  • Antibacterial activity
  • Benzodioxane
  • FtsZ
  • Methicillin resistance
  • Mycobacterium tuberculosis
  • Staphylococcus aureus

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