@article{SeethalerHertleinHopkeetal.2022,
  author    = {Seethaler, Marius and Hertlein, Tobias and Hopke, Elisa and K{\"o}hling, Paul and Ohlsen, Knut and Lalk, Michael and Hilgeroth, Andreas},
  title     = {Novel effective fluorinated benzothiophene-indole hybrid antibacterials against S. aureus and MRSA strains},
  series = {Pharmaceuticals},
  volume    = {15},
  journal   = {Pharmaceuticals},
  number    = {9},
  issn      = {1424-8247},
  doi       = {10.3390/ph15091138},
  url       = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-288253},
  year      = {2022},
  abstract  = {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.},
  language  = {en}
}
@article{SeethalerHertleinWeckleinetal.2019,
  author    = {Seethaler, Marius and Hertlein, Tobias and Wecklein, Bj{\"o}rn and Ymeraj, Alba and Ohlsen, Knut and Lalk, Michael and Hilgeroth, Andreas},
  title     = {Novel small-molecule antibacterials against Gram-positive pathogens of Staphylococcus and Enterococcus species},
  series = {Antibiotics},
  volume    = {8},
  journal   = {Antibiotics},
  number    = {4},
  issn      = {2079-6382},
  doi       = {10.3390/antibiotics8040210},
  url       = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-193130},
  year      = {2019},
  abstract  = {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 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.},
  language  = {en}
}