Potent in vitro methicillin-resistant Staphylococcus aureus activity of 2-(1H-indol-3-yl)quinoline derivatives.
A novel structural class of antibacterials, 2-(1H-indol-3-yl)quinolines, effective against methicillin-resistant Staphylococcus aureus (MRSA), was discovered from a combinatorial library. A structure-activity relationship (SAR) study was conducted to determine the pharmacophore and increase the potency of these compounds. Compounds were prepared that had minimum inhibitory concentrations (MICs) < 1.0 microg/mL against MRSA and retained activity against two strains of glycopeptide intermediate-resistant S. aureus (GISA).
Hoemann
M Z
MZ
Sepracor Inc., Marlborough, MA 01752, USA.
Kumaravel
G
G
Xie
R L
RL
Rossi
R F
RF
Meyer
S
S
Sidhu
A
A
Cuny
G D
GD
Hauske
J R
JR
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D007211:Indoles; D011804:Quinolines