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Discovery of antipsychotic loxapine derivatives against intracellular multidrug-resistant bacteria†
Hsueh-Chun Lin,Yi-Lun Wu,Cheng-Yun Hsu,Man-Yi Lin,Ling-Han Chen,Chung-Wai Shiau
RSC Medicinal Chemistry Pub Date : 08/11/2022 00:00:00 , DOI:10.1039/D2MD00182A
Abstract

The emergence and spread of multidrug-resistant bacteria highlight the need for new antibacterial interventions. A screening of 24 newly synthesized dibenzoxazepines identified a small molecule compound, SW14, with potent inhibitory activity against intracellular multidrug-resistant and fluoroquinolone-resistant strains of S. typhimurium in macrophages and epithelial cells. Moreover, intra-macrophagic Salmonella typhi, Yersinia enterocolitica, and Listeria monocytogenes and methicillin-resistant Staphylococcus aureus are also susceptible to SW14. Overall, our findings suggest that SW14 has a broad-spectrum activity against intracellular bacteria.

Graphical abstract: Discovery of antipsychotic loxapine derivatives against intracellular multidrug-resistant bacteria
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