title: Potent in vitro methicillin-resistant Staphylococcus aureus activity of 2-(1H-indol-3-yl)tetrahydroquinoline derivatives.
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).
authors.affiliation: Sepracor Inc., 111 Locke Dr., Marlborough, MA 01752, USA. mhoemann@sepracor.com
authors.forename: Michael Z
authors.initials: MZ
authors.lastname: Hoemann
authors.forename: Roger L
authors.initials: RL
authors.lastname: Xie
authors.forename: Richard F
authors.initials: RF
authors.lastname: Rossi
authors.forename: Sylvia
authors.initials: S
authors.lastname: Meyer
authors.forename: Alban
authors.initials: A
authors.lastname: Sidhu
authors.forename: Gregory D
authors.initials: GD
authors.lastname: Cuny
authors.forename: James R
authors.initials: JR
authors.lastname: Hauske
mesh_terms: 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*
chemical_list: C449665:2-(1H-indol-3-yl)tetrahydroquinoline; D000900:Anti-Bacterial Agents; D007211:Indoles; D011804:Quinolines