Design, synthesis, and biological evaluation of BODIPY®–erythromycin probes for bacterial ribosomes

BODIPY®–erythromycin probes of bacterial ribosomes were designed and synthesized by attaching a BODIPY® fluorophore to the 4″- and 9-positions of the erythromycin structure. The probes exhibited excellent binding affinity to bacterial ribosomes and competed with erythromycin and other drugs whose binding sites are in the same vicinity of the 50S subunit. The synthetic fluorescent probe 5 was successfully adapted in our ultra high-throughput screening (uHTS) to identify novel ribosome inhibitors.

Graphical abstractBODIPY®–erythromycin probes of bacterial ribosomes were designed, synthesized, and evaluated. The synthetic fluorescent probe 5 was successfully adapted in our ultra high-throughput screening (uHTS) for identifying novel ribosome inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide