Nitroreductase‐Responsive Photosensitizers for Selective Imaging and Photo‐Inactivation of Intracellular Bacteria

Abstract Intracellular Staphylococcus aureus ( S. aureus ), especially the methicillin resistant staphylococcus aureus (MRSA), are difficult to detect and eradicate due to the protection by the host cells. Antibacterial photodynamic therapy (aPDT) offers promise in treating intracellular bacteria, provided that selective damage to the bacteria ranther than host cells can be realized. According to the different nitroreductase (NTR) levels in mammalian cells and S. aureus , herein NTR‐responsive photosensitizers (PSs) (T)CyI−NO 2 were designed and synthesized. The emission and 1 O 2 generation of (T)CyI−NO 2 are quenched by the 4‐nitrobenzyl group, but can be specifically switched on by bacterial NTR. Therefore, selective imaging and photo‐inactivation of intracellular S. aureus and MRSA were achieved. Our findings may pave the way for the development of more efficient and selective aPDT agents to combat intractable intracellular infections.