2. Academic Validation
  3. Discovery of new dibenzodiazepine derivatives as antibacterials against intracellular bacteria

Discovery of new dibenzodiazepine derivatives as antibacterials against intracellular bacteria

  • RSC Med Chem. 2023 Dec 11;15(1):283-292. doi: 10.1039/d3md00418j.
Ling-Han Chen 1,  Man-Yi Lin 2,  Hsueh-Chun Lin 1,  Fan-Wei Yang 3,  Hsiao-Wei Liao 3,  Chung-Wai Shiau 2,  Hao-Chieh Chiu 1 4,  Jung-Chen Su 3
Affiliations

Affiliations

  • 1 Department of Clinical Laboratory Sciences and Medical Biotechnology, College of Medicine, National Taiwan University Taipei 10048 Taiwan [email protected] (+886) 22371-1574 (+886) 22312-3456 ext 66902.
  • 2 Institute of Biopharmaceutical Sciences, National Yang Ming Chiao Tung University Taipei 11221 Taiwan.
  • 3 Department of Pharmacy, National Yang Ming Chiao Tung University Taipei 11221 Taiwan [email protected] (+886) 22826-7000 ext 66401.
  • 4 Department of Laboratory Medicine, National Taiwan University Hospital, College of Medicine, National Taiwan University Taipei 10021 Taiwan.
PMID: 38283231 DOI: 10.1039/d3md00418j
Abstract

The emergence and spread of multidrug-resistant bacteria underscore the critical need for novel Antibacterial interventions. In our screening of 12 synthesized thienobenzodiazepines, pyridobenzodiazepines, and dibenzodiazepines, we successfully identified a small molecule compound SW33. Notably, SW33 demonstrated potent inhibitory activity against intracellular multidrug-resistant and fluoroquinolone-resistant strains of S. typhimurium in both macrophages and epithelial cells. Furthermore, SW33 was also effective against intramacrophagic Salmonella typhi, Yersinia enterocolitica, and Listeria monocytogenes. These significant findings suggest that SW33 possesses broad-spectrum activity against intracellular bacteria.

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