期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 15, 页码 4294-4297出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.06.093
关键词
2-arylindoles; NorA efflux pump inhibitors; antibacterial
资金
- NIAID NIH HHS [R21 AI059483, R21 AI59483-01, R21 AI059483-02, R01 AI076372] Funding Source: Medline
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. (c) 2008 Elsevier Ltd. All rights reserved.
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