Potent in vitro methicillin-resistant Staphylococcus aureus activity of 2-(1H-indol-3-yl)tetrahydroquinoline derivatives.
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).
Hoemann
Michael Z
MZ
Sepracor Inc., 111 Locke Dr., Marlborough, MA 01752, USA. mhoemann@sepracor.com
Xie
Roger L
RL
Rossi
Richard F
RF
Meyer
Sylvia
S
Sidhu
Alban
A
Cuny
Gregory D
GD
Hauske
James R
JR
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D066298:In Vitro Techniques; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects*
C449665:2-(1H-indol-3-yl)tetrahydroquinoline; D000900:Anti-Bacterial Agents; D007211:Indoles; D011804:Quinolines