Novel small-molecule antibacterials against Gram-positive pathogens of Staphylococcus and Enterococcus species

Please always quote using this URN: urn:nbn:de:bvb:20-opus-193130
  • Defeat of the antibiotic resistance of pathogenic bacteria is one great challenge today and for the future. In the last century many classes of effective antibacterials have been developed, so that upcoming resistances could be met with novel drugs of various compound classes. Meanwhile, there is a certain lack of research of the pharmaceutical companies, and thus there are missing developments of novel antibiotics. Gram-positive bacteria are the most important cause of clinical infections. The number of novel antibacterials in clinical trialsDefeat of the antibiotic resistance of pathogenic bacteria is one great challenge today and for the future. In the last century many classes of effective antibacterials have been developed, so that upcoming resistances could be met with novel drugs of various compound classes. Meanwhile, there is a certain lack of research of the pharmaceutical companies, and thus there are missing developments of novel antibiotics. Gram-positive bacteria are the most important cause of clinical infections. The number of novel antibacterials in clinical trials is strongly restricted. There is an urgent need to find novel antibacterials. We used synthetic chemistry to build completely novel hybrid molecules of substituted indoles and benzothiophene. In a simple one-pot reaction, two novel types of thienocarbazoles were yielded. Both indole substituted compound classes have been evaluated as completely novel antibacterials against the Staphylococcus and Enterococcus species. The evaluated partly promising activities depend on the indole substituent type. First lead compounds have been evaluated within in vivo studies. They confirmed the in vitro results for the new classes of small-molecule antibacterials.show moreshow less

Download full text files

Export metadata

Additional Services

Share in Twitter Search Google Scholar Statistics
Metadaten
Author: Marius Seethaler, Tobias Hertlein, Björn Wecklein, Alba Ymeraj, Knut Ohlsen, Michael Lalk, Andreas Hilgeroth
URN:urn:nbn:de:bvb:20-opus-193130
Document Type:Journal article
Faculties:Medizinische Fakultät / Institut für Molekulare Infektionsbiologie
Language:English
Parent Title (English):Antibiotics
ISSN:2079-6382
Year of Completion:2019
Volume:8
Issue:4
Article Number:210
Source:Antibiotics (2019) 8:4, 210. https://doi.org/10.3390/antibiotics8040210
DOI:https://doi.org/10.3390/antibiotics8040210
Dewey Decimal Classification:6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit
Tag:antibacterial activity; inhibition; structure-activity; substituent; synthesis
Release Date:2022/04/28
Date of first Publication:2019/11/02
Licence (German):License LogoCC BY: Creative-Commons-Lizenz: Namensnennung 4.0 International