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.show moreshow less

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Metadaten
Author: Kerolos Ashraf, Kaveh Yasrebi, Tobias Hertlein, Knut Ohlsen, Michael Lalk, Andreas Hilgeroth
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):License LogoCC BY: Creative-Commons-Lizenz: Namensnennung 4.0 International