Design and evaluation of analogues of the bacterial cell-wall peptidoglycan motif L-Lys-D-Ala-D-Ala for use in a vancomycin biosensor.

نویسندگان

  • Olivier Hernout
  • Karine Berthoin
  • Isabelle Delattre
  • Paul M Tulkens
  • Stéphane Carryn
  • Jacqueline Marchand-Brynaert
چکیده

Four small molecular receptors of vancomycin have been designed to make part of a novel biosensor device based on the FTIR-ATR detection: N-Boc (2a) or N-Ac (2b)-6-aminocaproyl-D-Ala-D-Ala and N-Boc (3a) or N-Ac (3b)-6-aminocaproyl-D-Ala-d-Ser. Using an original microbiological approach to assess the competition of compounds with the natural target of vancomycin in bacteria, EC(50) values of 6.3-8.0 x 10(-5)M (2a-b) and 7.1-9.3 x 10(-4)M (3a-b) were determined. Vancomycin:2b complex was characterized by MS.

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عنوان ژورنال:
  • Bioorganic & medicinal chemistry letters

دوره 17 21  شماره 

صفحات  -

تاریخ انتشار 2007