title: Novel inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase.
abstract: Novel bisindolyl-cycloalkane indoles resulted from the reaction of aliphatic dialdehydes and indole. As bisindolyl-natural alkaloid compounds have recently been reported as inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase (PK), we tested our novel compounds as MRSA PK inhibitors and now report first inhibiting activities. We discuss structure-activity relationships of structurally varied compounds. Activity influencing substituents have been characterized and relations to antibacterial activities of the most active compounds have been proved.
authors.affiliation: a Department of Pharmaceutical Chemistry , Institute of Pharmacy, Martin Luther University , Halle , Germany .
authors.forename: Mardia Telep
authors.initials: MT
authors.lastname: El-Sayed
authors.affiliation: b Department of Medicine, Division of Infectious Diseases , University of British Columbia , Vancouver , BC , Canada .
authors.forename: Roya
authors.initials: R
authors.lastname: Zoraghi
authors.affiliation: b Department of Medicine, Division of Infectious Diseases , University of British Columbia , Vancouver , BC , Canada .
authors.forename: Neil
authors.initials: N
authors.lastname: Reiner
authors.affiliation: c Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Ankara University , Ankara , Turkey .
authors.forename: Sibel
authors.initials: S
authors.lastname: Suzen
authors.affiliation: d Institute for Molecular Biology of Infections, Julius Schneider University Würzburg , Würzburg , Germany .
authors.forename: Knut
authors.initials: K
authors.lastname: Ohlsen
authors.affiliation: e Institute of Biochemistry, Ernst Moritz Arndt University Greifswald , Greifswald , Germany , and.
authors.forename: Michael
authors.initials: M
authors.lastname: Lalk
authors.affiliation: f Department of Pharmaceutical Microbiology, Faculty of Pharmacy , Ankara University , Ankara , Turkey.
authors.forename: Nurten
authors.initials: N
authors.lastname: Altanlar
authors.affiliation: a Department of Pharmaceutical Chemistry , Institute of Pharmacy, Martin Luther University , Halle , Germany .
authors.forename: Andreas
authors.initials: A
authors.lastname: Hilgeroth
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects / Q000201:enzymology*; D011770:Pyruvate Kinase / Q000037:antagonists & inhibitors*; D013057:Spectrum Analysis / Q000379:methods
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D011770:Pyruvate Kinase
keywords: Antimicrobial compounds; biological activity; indolyl-derived compounds