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Molecules 2017, 22(12), 2193; https://doi.org/10.3390/molecules22122193

Novel Effective Small-Molecule Antibacterials against Enterococcus Strains

1
Institute of Pharmacy, Martin-Luther-University Halle-Wittenberg, 06120 Halle, Germany
2
Institute of Molecular Infection Biology, Julius-Maximilians-University Wuerzburg, 97080 Wuerzburg, Germany
3
Institute of Biochemistry, Ernst-Moritz-Arndt-University Greifswald, 17489 Greifswald, Germany
*
Author to whom correspondence should be addressed.
Received: 1 November 2017 / Revised: 24 November 2017 / Accepted: 29 November 2017 / Published: 10 December 2017
(This article belongs to the Special Issue Emerging Drug Discovery Approaches against Infectious Diseases)
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Abstract

Enterococcus species cause increasing numbers of infections in hospitals. They contribute to the increasing mortality rates, mostly in patients with comorbidities, who suffer from severe diseases. Enterococcus resistances against most antibiotics have been described, including novel antibiotics. Therefore, there is an ongoing demand for novel types of antibiotics that may overcome bacterial resistances. We discovered a novel class of antibiotics resulting from a simple one-pot reaction of indole and o-phthaldialdehyde. Differently substituted indolyl benzocarbazoles were yielded. Both the indole substitution and the positioning at the molecular scaffold influence the antibacterial activity towards the various strains of Enterococcus species with the highest relevance to nosocomial infections. Structure-activity relationships are discussed, and the first lead compounds were identified as also being effective in the case of a vancomycin resistance. View Full-Text
Keywords: antibacterial activity; synthesis; derivatives; structure-activity; lead structure antibacterial activity; synthesis; derivatives; structure-activity; lead structure
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Ashraf, K.; Yasrebi, K.; Hertlein, T.; Ohlsen, K.; Lalk, M.; Hilgeroth, A. Novel Effective Small-Molecule Antibacterials against Enterococcus Strains. Molecules 2017, 22, 2193.

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