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Bioorg Med Chem Lett. 2016 Jan 1;26(1):218-21. doi: 10.1016/j.bmcl.2015.10.085. Epub 2015 Oct 29.

Discovery of bisindolyl-substituted cycloalkane-anellated indoles as novel class of antibacterial agents against S. aureus and MRSA.

Author information

1
Institute of Pharmacy, Martin-Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany.
2
Faculty of Pharmacy, Ankara University, Tandogan, Department of Pharmaceutical Chemistry, Tandogan, 06100 Ankara, Turkey.
3
Faculty of Pharmacy, Ankara University, Tandogan, Department of Pharmaceutical Microbiology, Tandogan, 06100 Ankara, Turkey.
4
Institute of Molecular Infection Biology, Julius-Maximilian University Würzburg, 97080 Würzburg, Germany.
5
Institute of Pharmacy, Martin-Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120 Halle, Germany. Electronic address: andreas.hilgeroth@pharmazie.uni-halle.de.

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.

KEYWORDS:

Antibacterial activity; Cycloalkane indoles; MRSA; Structure–activity relationships

PMID:
26590101
DOI:
10.1016/j.bmcl.2015.10.085
[Indexed for MEDLINE]

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