title: Discovery of bisindolyl-substituted cycloalkane-anellated indoles as novel class of antibacterial agents against S. aureus and MRSA.
abstract: Antibiotic resistance is an ongoing problem in the treatment of bacterial diseases. Among the various antibacterial infections Staphylococcus aureus infections remain critical due to the increasing resistances, especially against the methicillin-resistant S. aureus (MRSA). We discovered novel antibacterial compounds with activities against both S. aureus and MRSA types. Structure-activity relationships (SAR) are discussed and show that the activity depends on the ring size of the anellated cycloalkane. Moreover, first substituent effects have been investigated for both the cycloalkane and the indole residues.
authors.affiliation: Institute of Pharmacy, Martin-Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany.
authors.forename: Mardia Telep
authors.initials: MT
authors.lastname: El-Sayed
authors.affiliation: Faculty of Pharmacy, Ankara University, Tandogan, Department of Pharmaceutical Chemistry, Tandogan, 06100 Ankara, Turkey.
authors.forename: Sibel
authors.initials: S
authors.lastname: Suzen
authors.affiliation: Faculty of Pharmacy, Ankara University, Tandogan, Department of Pharmaceutical Microbiology, Tandogan, 06100 Ankara, Turkey.
authors.forename: Nurten
authors.initials: N
authors.lastname: Altanlar
authors.affiliation: Institute of Molecular Infection Biology, Julius-Maximilian University Würzburg, 97080 Würzburg, Germany.
authors.forename: Knut
authors.initials: K
authors.lastname: Ohlsen
authors.affiliation: Institute of Pharmacy, Martin-Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany. Electronic address: andreas.hilgeroth@pharmazie.uni-halle.de.
authors.forename: Andreas
authors.initials: A
authors.lastname: Hilgeroth
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D003516:Cycloparaffins / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D015394:Molecular Structure; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D003516:Cycloparaffins; D007211:Indoles
keywords: Antibacterial activity; Cycloalkane indoles; MRSA; Structure–activity relationships