Novel effective fluorinated benzothiophene-indole hybrid antibacterials against S. aureus and MRSA strains
Zitieren Sie bitte immer diese URN: urn:nbn:de:bvb:20-opus-288253
- Increasing antibacterial drug resistance threatens global health, unfortunately, however, efforts to find novel antibacterial agents have been scaled back by the pharmaceutical industry due to concerns about a poor return on investment. Nevertheless, there is an urgent need to find novel antibacterial compounds to combat antibacterial drug resistance. The synthesis of novel drugs from natural sources is mostly cost-intensive due to those drugs’ complicated structures. Therefore, it is necessary to find novel antibacterials by simple synthesisIncreasing antibacterial drug resistance threatens global health, unfortunately, however, efforts to find novel antibacterial agents have been scaled back by the pharmaceutical industry due to concerns about a poor return on investment. Nevertheless, there is an urgent need to find novel antibacterial compounds to combat antibacterial drug resistance. The synthesis of novel drugs from natural sources is mostly cost-intensive due to those drugs’ complicated structures. Therefore, it is necessary to find novel antibacterials by simple synthesis to become more attractive for industrial production. We succeeded in the discovery of four antibacterial compound (sub)classes accessible in a simple one-pot reaction based on fluorinated benzothiophene-indole hybrids. They have been evaluated against various S. aureus and MRSA strains. Structure- and substituent-dependent activities have been found within the (sub)classes and promising lead compounds have been identified. In addition, bacterial pyruvate kinase was found to be the molecular target of the active compounds. In conclusion, simple one-pot synthesis of benzothiophene-indoles represents a promising strategy for the search of novel antimicrobial compounds.…
Autor(en): | Marius Seethaler, Tobias Hertlein, Elisa Hopke, Paul Köhling, Knut Ohlsen, Michael Lalk, Andreas Hilgeroth |
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URN: | urn:nbn:de:bvb:20-opus-288253 |
Dokumentart: | Artikel / Aufsatz in einer Zeitschrift |
Institute der Universität: | Medizinische Fakultät / Institut für Molekulare Infektionsbiologie |
Sprache der Veröffentlichung: | Englisch |
Titel des übergeordneten Werkes / der Zeitschrift (Englisch): | Pharmaceuticals |
ISSN: | 1424-8247 |
Erscheinungsjahr: | 2022 |
Band / Jahrgang: | 15 |
Heft / Ausgabe: | 9 |
Aufsatznummer: | 1138 |
Originalveröffentlichung / Quelle: | Pharmaceuticals (2022) 15:9, 1138. https://doi.org/10.3390/ph15091138 |
DOI: | https://doi.org/10.3390/ph15091138 |
Allgemeine fachliche Zuordnung (DDC-Klassifikation): | 6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit |
Freie Schlagwort(e): | antibacterial drug resistance; inhibition; structure activity; substituent; synthesis |
Datum der Freischaltung: | 08.09.2023 |
Datum der Erstveröffentlichung: | 13.09.2022 |
Lizenz (Deutsch): | CC BY: Creative-Commons-Lizenz: Namensnennung 4.0 International |