Potent In vitro methicillin-resistant Staphylococcus aureus activity of 2-(1 H-indol-3-yl)quinoline derivatives

A novel structural class of antibacterials, 2-(1 H-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 pot...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-12, Vol.10 (23), p.2675-2678
Hauptverfasser:	Hoemann, Michael Z., Kumaravel, G., Xie, Roger L., Rossi, Richard F., Meyer, Sylvia, Sidhu, Alban, Cuny, Gregory D., Hauske, James R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Combinatorial Chemistry Techniques Indoles - chemistry Indoles - pharmacology Medical sciences Methicillin Resistance Microbial Sensitivity Tests Pharmacology. Drug treatments Quinolines - chemistry Quinolines - pharmacology Staphylococcus aureus - drug effects Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	A novel structural class of antibacterials, 2-(1 H-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)
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00542-4