2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion

نویسندگان

  • James R. Sayer
  • Karin Walldén
  • Thomas Pesnot
  • Frederick Campbell
  • Paul J. Gane
  • Michela Simone
  • Hans Koss
  • Floris Buelens
  • Timothy P. Boyle
  • David L. Selwood
  • Gabriel Waksman
  • Alethea B. Tabor
چکیده

A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a]pyrazines has been used to probe the structure-activity relationships of these inhibitors, which show potential as antibacterial agents.

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عنوان ژورنال:

دوره 22  شماره 

صفحات  -

تاریخ انتشار 2014