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Open AccessCommunication

Novel Small-molecule Antibacterials against Gram-positive Pathogens of Staphylococcus and Enterococcus Species

Institute of Pharmacy, Martin-Luther-University Halle-Wittenberg, 06120 Halle, Germany
Institute of Molecular Infection Biology, Julius Maximilians University Würzburg, 97080 Würzburg, Germany
Institute of Biochemistry, Ernst-Moritz-Arndt-University Greifswald, 17489 Greifswald, Germany
Author to whom correspondence should be addressed.
Antibiotics 2019, 8(4), 210;
Received: 27 September 2019 / Revised: 22 October 2019 / Accepted: 30 October 2019 / Published: 2 November 2019
Defeat of the antibiotic resistance of pathogenic bacteria is one great challenge today and for the future. In the last century many classes of effective antibacterials have been developed, so that upcoming resistances could be met with novel drugs of various compound classes. Meanwhile, there is a certain lack of research of the pharmaceutical companies, and thus there are missing developments of novel antibiotics. Gram-positive bacteria are the most important cause of clinical infections. The number of novel antibacterials in clinical trials is strongly restricted. There is an urgent need to find novel antibacterials. We used synthetic chemistry to build completely novel hybrid molecules of substituted indoles and benzothiophene. In a simple one-pot reaction, two novel types of thienocarbazoles were yielded. Both indole substituted compound classes have been evaluated as completely novel antibacterials against the Staphylococcus and Enterococcus species. The evaluated partly promising activities depend on the indole substituent type. First lead compounds have been evaluated within in vivo studies. They confirmed the in vitro results for the new classes of small-molecule antibacterials. View Full-Text
Keywords: antibacterial activity; synthesis; substituent; structure-activity; inhibition antibacterial activity; synthesis; substituent; structure-activity; inhibition
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Seethaler, M.; Hertlein, T.; Wecklein, B.; Ymeraj, A.; Ohlsen, K.; Lalk, M.; Hilgeroth, A. Novel Small-molecule Antibacterials against Gram-positive Pathogens of Staphylococcus and Enterococcus Species. Antibiotics 2019, 8, 210.

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