Organo‐Ptii Complexes for Potent Photodynamic Inactivation of Multi‐Drug Resistant Bacteria and the Influence of Configuration

Abstract Pt II based organometallic photosensitizers (PSs) have emerged as novel potent photodynamic inactivation (PDI) reagents through their enhanced intersystem crossing (ISC) processes. Currently, few Pt II PSs have been investigated as antibacterial materials, with relatively poor performances reported and with structure‐activity relationships not well described. Herein, a pair of configurational isomers are reported of Bis‐BODIPY (4,4‐difluoro‐boradizaindacene) embedded Pt II PSs. The cis ‐isomer ( cis ‐BBP) displayed enhanced 1 O 2 generation and better bacterial membrane anchoring capability as compared to the trans‐isomer (trans‐BBP). The effective PDI concentrations (efficiency > 99.9%) for cis‐BBP in Acinetobacter baumannii (multi‐drug resistant (MDR)) and Staphylococcus aureus are 400 nM (12 J cm −2 ) and 100 nM (18 J cm −2 ), respectively; corresponding concentrations and light doses for trans ‐BBP in the two bacteria are 2.50 µM (30 J cm −2 ) and 1.50 µM (18 J cm −2 ), respectively. The 50% and 90% minimum inhibitory concentration (MIC 50 and MIC 90 ) ratio of trans‐BBP to cis ‐BBP is 22.22 and 24.02 in A. baumannii (MDR); 21.29 and 22.36 in methicillin resistant S. aureus (MRSA), respectively. Furthermore, cis ‐BBP displays superior in vivo antibacterial performance, with acceptable dark and photoinduced cytotoxicity. These results demonstrate cis ‐BBP is a robust light‐assisted antibacterial reagent at sub‐micromolecular concentrations. More importantly, configuration of Pt II PSs should be an important issue to be considered in further PDI reagents design.