Structure–activity relationships of 2-aryl-1H-indole inhibitors of the NorA efflux pump in Staphylococcus aureus
…, MJ Kelso, JB Bremner, AR Ball, G Casadei…
Index: Ambrus, Joseph I.; Kelso, Michael J.; Bremner, John B.; Ball, Anthony R.; Casadei, Gabriele; Lewis, Kim Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 15 p. 4294 - 4297
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Citation Number: 51
Abstract
The synthesis of 22 2-aryl-1H-indoles, including 12 new compounds, has been achieved via Pd-or Rh-mediated methodologies, or selective electrophilic substitution. All three methods were based on elaborations from simple indole precursors. SAR studies on these indoles and 2-phenyl-1H-indole in Staphylococcus aureus as NorA efflux pump inhibitors indicated 5-nitro-2-(3-methoxycarbonyl) phenyl-1H-indole was a slightly more potent inhibitor than ...
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