Discovery of bisindolyl-substituted cycloalkane-anellated indoles as novel class of antibacterial agents against S. aureus and MRSA. Issue 1 (1st January 2016)

• Record Type: Journal Article
• Authors: El-Sayed, Mardia Telep; Suzen, Sibel; Altanlar, Nurten; Ohlsen, Knut; Hilgeroth, Andreas
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 1(2016)
• Page Start: 218
• Page End: 221
• Publication Date: 2016-01-01
• Subjects: Cycloalkane indoles -- Antibacterial activity -- MRSA -- Structure–activity relationships; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.10.085
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.