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

Zitieren Sie bitte immer diese 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.zeige mehrzeige weniger

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Autor(en): Marius Seethaler, Tobias Hertlein, Björn Wecklein, Alba Ymeraj, Knut Ohlsen, Michael Lalk, Andreas Hilgeroth
URN:urn:nbn:de:bvb:20-opus-193130
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):Antibiotics
ISSN:2079-6382
Erscheinungsjahr:2019
Band / Jahrgang:8
Heft / Ausgabe:4
Aufsatznummer:210
Originalveröffentlichung / Quelle:Antibiotics (2019) 8:4, 210. https://doi.org/10.3390/antibiotics8040210
DOI:https://doi.org/10.3390/antibiotics8040210
Allgemeine fachliche Zuordnung (DDC-Klassifikation):6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit
Freie Schlagwort(e):antibacterial activity; inhibition; structure-activity; substituent; synthesis
Datum der Freischaltung:28.04.2022
Datum der Erstveröffentlichung:02.11.2019
Lizenz (Deutsch):License LogoCC BY: Creative-Commons-Lizenz: Namensnennung 4.0 International