Title

Structure-activity relationships of 2-aryl-1H-indole inhibitors of the NorA efflux pump in Staphylococcus aureus

RIS ID

24974

Publication Details

Ambrus, J. I., Kelso, M. J., Bremner, J. B., Ball, A. R., Casadei, G. & Lewis, K. (2008). Structure-activity relationships of 2-aryl-1H-indole inhibitors of the NorA efflux pump in Staphylococcus aureus. Bioorganic and Medicinal Chemistry Letters, 18 (15), 4294-4297.

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 the lead INF55. A promising new antibacterial lead compound against S. aureus (2-phenyl-1H-indol-5-yl)-methanol, was also found.

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Link to publisher version (DOI)

http://dx.doi.org/10.1016/j.bmcl.2008.06.093