Creating an Antibacterial with in Vivo Efficacy: Synthesis and Characterization of Potent Inhibitors of the Bacterial Cell Division Protein FtsZ with Improved Pharmaceutical Properties

نویسندگان

  • David J. Haydon
  • James M. Bennett
  • David Brown
  • Ian Collins
  • Greta Galbraith
  • Paul Lancett
  • Rebecca Macdonald
  • Neil R. Stokes
  • Pramod K. Chauhan
  • Jignesh K. Sutariya
  • Narendra Nayal
  • Anil Srivastava
  • Joy Beanland
  • Robin Hall
  • Vincent Henstock
  • Caterina Noula
  • Chris Rockley
  • Lloyd Czaplewski
چکیده

3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the structure-activity relationships of analogues of these inhibitors led to the identification of potent antistaphylococcal compounds with improved pharmaceutical properties.

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عنوان ژورنال:

دوره 53  شماره 

صفحات  -

تاریخ انتشار 2010