Aryldiketo acids have antibacterial activity against MDR Staphylococcus aureus strains: structural insights based on similarity and molecular interaction fields.

نویسندگان

  • Branko J Drakulić
  • Michael Stavri
  • Simon Gibbons
  • Zeljko S Zizak
  • Tatjana Z Verbić
  • Ivan O Juranić
  • Mire Zloh
چکیده

Staphylococcus aureus is a major communityand hospitalacquired pathogen. Reports of resistance to antibiotics, including the fluoroquinolone class, have placed a greater emphasis on the development of new drugs for the treatment of both methicillin(MRSA) and multidrug-resistant (MDR) S. aureus strains. Recently, mixed quinolonediketo acid derivatives, which are based on the scaffold of fluoroquinolone antibiotics, were shown to exert significant anti-HIV-1 potency. The g-diketo moiety is also found in tetracycline, and is therefore potentially important for antibacterial activity. GS-9137 (elvitegravir, CAS 697761-98-1), a 4-quinolone-3-carboxylic acidbased HIV-1 integrase inhibitor is presently in phase III clinical trials. The similarity between these two scaffolds (Figure 1),

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عنوان ژورنال:
  • ChemMedChem

دوره 4 12  شماره 

صفحات  -

تاریخ انتشار 2009