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

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

Risultato della ricerca: Contributo in rivistaArticolo in rivistapeer review

15 Citazioni (Scopus)

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.
Lingua originaleEnglish
pagine (da-a)227-243
Numero di pagine17
RivistaEuropean Journal of Medicinal Chemistry
Volume120
DOI
Stato di pubblicazionePubblicato - 2016

Keywords

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

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