Novel effective small-molecule antibacterials against \(Enterococcus\) strains
Please always quote using this URN: urn:nbn:de:bvb:20-opus-172628
- \(Enterococcus\) 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\(Enterococcus\) 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.…
Author: | Kerolos Ashraf, Kaveh Yasrebi, Tobias Hertlein, Knut Ohlsen, Michael Lalk, Andreas Hilgeroth |
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URN: | urn:nbn:de:bvb:20-opus-172628 |
Document Type: | Journal article |
Faculties: | Medizinische Fakultät / Institut für Molekulare Infektionsbiologie |
Language: | English |
Parent Title (English): | Molecules |
Year of Completion: | 2017 |
Volume: | 22 |
Issue: | 12 |
Article Number: | 2193 |
Source: | Molecules (2017) 22(12):2193. https://doi.org/10.3390/molecules22122193 |
DOI: | https://doi.org/10.3390/molecules22122193 |
Dewey Decimal Classification: | 6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit |
Tag: | antibacterial activity; derivatives; lead structure; medicine; structure-activity; synthesis |
Release Date: | 2021/03/17 |
Licence (German): | CC BY: Creative-Commons-Lizenz: Namensnennung 4.0 International |