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Novel Effective Fluorinated Benzothiophene-Indole Hybrid Antibacterials against S. aureus and MRSA Strains
- 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 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.
Author: | Marius Seethaler, Tobias Hertlein, Elisa Hopke, Paul Köhling, Knut Ohlsen, Michael LalkORCiD, Andreas Hilgeroth |
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URN: | urn:nbn:de:gbv:9-opus-75401 |
DOI: | https://doi.org/10.3390/ph15091138 |
ISSN: | 1424-8247 |
Parent Title (English): | Pharmaceuticals |
Publisher: | MDPI |
Place of publication: | Basel |
Editor: | Fiorella Meneghetti, Daniela Barlocco |
Document Type: | Article |
Language: | English |
Date of first Publication: | 2022/09/13 |
Release Date: | 2022/11/14 |
Tag: | antibacterial drug resistance; inhibition; structure activity; substituent; synthesis |
GND Keyword: | - |
Volume: | 15 |
Issue: | 9 |
Article Number: | 1138 |
Page Number: | 15 |
Faculties: | Mathematisch-Naturwissenschaftliche Fakultät / Institut für Biochemie |
Licence (German): | Creative Commons - Namensnennung |