Chen Ling-Han, Lin Man-Yi, Lin Hsueh-Chun, Yang Fan-Wei, Liao Hsiao-Wei, Shiau Chung-Wai, Chiu Hao-Chieh, Su Jung-Chen
Department of Clinical Laboratory Sciences and Medical Biotechnology, College of Medicine, National Taiwan University Taipei 10048 Taiwan
Institute of Biopharmaceutical Sciences, National Yang Ming Chiao Tung University Taipei 11221 Taiwan.
RSC Med Chem. 2023 Dec 11;15(1):283-292. doi: 10.1039/d3md00418j. eCollection 2024 Jan 25.
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 in both macrophages and epithelial cells. Furthermore, SW33 was also effective against intramacrophagic , , and . These significant findings suggest that SW33 possesses broad-spectrum activity against intracellular bacteria.
多重耐药菌的出现和传播凸显了新型抗菌干预措施的迫切需求。在我们对12种合成的噻吩并苯二氮䓬、吡啶并苯二氮䓬和二苯并氮䓬进行的筛选中，我们成功鉴定出一种小分子化合物SW33。值得注意的是，SW33在巨噬细胞和上皮细胞中均表现出对细胞内多重耐药和耐氟喹诺酮菌株的强效抑制活性。此外，SW33对巨噬细胞内的 、 和 也有效。这些重要发现表明，SW33对细胞内细菌具有广谱活性。
