Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates.

نویسندگان

  • Willmen Youngsaye
  • Benjamin Vincent
  • Cathy L Hartland
  • Barbara J Morgan
  • Sara J Buhrlage
  • Stephen Johnston
  • Joshua A Bittker
  • Lawrence MacPherson
  • Sivaraman Dandapani
  • Michelle Palmer
  • Luke Whitesell
  • Susan Lindquist
  • Stuart L Schreiber
  • Benito Munoz
چکیده

The effectiveness of the potent antifungal drug fluconazole is being compromised by the rise of drug-resistant fungal pathogens. While inhibition of Hsp90 or calcineurin can reverse drug resistance in Candida, such inhibitors also impair the homologous human host protein and fungal-selective chemosensitizers remain rare. The MLPCN library was screened to identify compounds that selectively reverse fluconazole resistance in a Candida albicans clinical isolate, while having no antifungal activity when administered as a single agent. A piperazinyl quinoline was identified as a new small-molecule probe (ML189) satisfying these criteria.

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عنوان ژورنال:
  • Bioorganic & medicinal chemistry letters

دوره 21 18  شماره 

صفحات  -

تاریخ انتشار 2011