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Potent in vitro methicillin-resistant Staphylococcus aureus activity of 2-(1H-indol-3-yl)tetrahydroquinoline
Michael Z Hoemann1, Roger L Xie, Richard F Rossi
1Sepracor Inc., 111 Locke Dr., Marlborough, MA 01752, USA. mhoemann@sepracor.com
Bioorganic & Medicinal Chemistry Letters
|January 5, 2002
Abstract:
Novel antibacterials agents, 2-(1H-indol-3-yl)tetrahydroquinolines, were prepared using hetero Diels-Alder chemistry and found to be effective in vitro against methicillin-resistant Staphylococcus aureus (MRSA). A structure-activity relationship (SAR) study was conducted to determine the important features of this series and to increase the potency of these compounds. Compounds were prepared that had minimum inhibitory concentrations (MIC's) < 1.0 microg/mL against MRSA, but had no activity versus vancomycin-resistant Enterococcus (VRE).