Double‐pronged Antimicrobial Agents based on a Donor‐π‐Acceptor Type Aggregation‐Induced Emission Luminogen

Abstract Novel antibacterial agents are urgently needed to control the infections induced by multidrug‐resistant (MDR) bacteria. Herein, we rationally designed and facilely synthesized a new D‐π‐A type luminogen with strong red/near‐infrared fluorescence emission, great aggregation‐induced emission (AIE) features, and excellent reactive oxygen species (ROS) production. The newly developed molecule TTTh killed the methicillin‐resistant Staphylococcus aureus (MRSA) by triggering the ROS accumulation in bacteria and interrupting the membrane integrity. Moreover, TTTh specifically targeted the lysosomes and potentiated their maturation to accelerate the clearance of intracellular bacteria. Additionally, reduced bacterial burden and improved healing were observed in TTTh‐treated wounds with negligible side effects. Our study expands the biological design and application of AIE luminogens (AIEgens), and provides new insights into discovering novel antibacterial targets and agents.