Novel small-molecule hybrid-antibacterial agents against S. aureus and MRSA strains

Please always quote using this URN: urn:nbn:de:bvb:20-opus-252371
  • Ongoing resistance developments against antibiotics that also affect last-resort antibiotics require novel antibacterial compounds. Strategies to discover such novel structures have been dimerization or hybridization of known antibacterial agents. We found novel antibacterial agents by dimerization of indols and hybridization with carbazoles. They were obtained in a simple one-pot reaction as bisindole tetrahydrocarbazoles. Further oxidation led to bisindole carbazoles with varied substitutions of both the indole and the carbazole scaffold.Ongoing resistance developments against antibiotics that also affect last-resort antibiotics require novel antibacterial compounds. Strategies to discover such novel structures have been dimerization or hybridization of known antibacterial agents. We found novel antibacterial agents by dimerization of indols and hybridization with carbazoles. They were obtained in a simple one-pot reaction as bisindole tetrahydrocarbazoles. Further oxidation led to bisindole carbazoles with varied substitutions of both the indole and the carbazole scaffold. Both the tetrahydrocarbazoles and the carbazoles have been evaluated in various S. aureus strains, including MRSA strains. Those 5-cyano substituted derivatives showed best activities as determined by MIC values. The tetrahydrocarbazoles partly exceed the activity of the carbazole compounds and thus the activity of the used standard antibiotics. Thus, promising lead compounds could be identified for further studies.show moreshow less

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Metadaten
Author: Robin Gehrmann, Tobias Hertlein, Elisa Hopke, Knut Ohlsen, Michael Lalk, Andreas Hilgeroth
URN:urn:nbn:de:bvb:20-opus-252371
Document Type:Journal article
Faculties:Medizinische Fakultät / Institut für Molekulare Infektionsbiologie
Language:English
Parent Title (English):Molecules
ISSN:1420-3049
Year of Completion:2021
Volume:27
Issue:1
Article Number:61
Source:Molecules (2022) 27:1, 61. https://doi.org/10.3390/molecules27010061
DOI:https://doi.org/10.3390/molecules27010061
Dewey Decimal Classification:5 Naturwissenschaften und Mathematik / 54 Chemie / 540 Chemie und zugeordnete Wissenschaften
6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit
Tag:antibacterial activity; inhibition; structure–activity; substituent; synthesis
Release Date:2022/11/17
Date of first Publication:2021/12/23
Licence (German):License LogoCC BY: Creative-Commons-Lizenz: Namensnennung 4.0 International