Furanyl-rhodanines are unattractive drug candidates for development as inhibitors of bacterial RNA polymerase.

نویسندگان

  • Katherine R Mariner
  • Rachel Trowbridge
  • Anil K Agarwal
  • Keith Miller
  • Alex J O'Neill
  • Colin W G Fishwick
  • Ian Chopra
چکیده

Previous studies suggest that furanyl-rhodanines might specifically inhibit bacterial RNA polymerase (RNAP). We further explored three compounds from this class. Although they inhibited RNAP, each compound also inhibited malate dehydrogenase and chymotrypsin. Using biosensors responsive to inhibition of macromolecular synthesis and membrane damaging assays, we concluded that in bacteria, one compound inhibited DNA synthesis and another caused membrane damage. The third rhodanine lacked antibacterial activity. We consider furanyl-rhodanines to be unattractive RNAP inhibitor drug candidates.

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عنوان ژورنال:
  • Antimicrobial agents and chemotherapy

دوره 54 10  شماره 

صفحات  -

تاریخ انتشار 2010