Potent in vitro methicillin-resistant Staphylococcus aureus activity of 2-(1H-indol-3-yl)quinoline derivatives |
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| Authors: | Hoemann M Z Kumaravel G Xie R L Rossi R F Meyer S Sidhu A Cuny G D Hauske J R |
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| Institution: | Sepracor Inc., Marlborough, MA 01752, USA. |
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| Abstract: | A novel structural class of antibacterials, 2-(1H-indol-3-yl)quinolines, effective against methicillin-resistant Staphylococcus aureus (MRSA), was discovered from a combinatorial library. A structure-activity relationship (SAR) study was conducted to determine the pharmacophore and increase the potency of these compounds. Compounds were prepared that had minimum inhibitory concentrations (MICs) < 1.0 microg/mL against MRSA and retained activity against two strains of glycopeptide intermediate-resistant S. aureus (GISA). |
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