Provided is the use of a rifamycin-quinolizidone coupling molecule as shown in I and a pharmaceutically acceptable salt thereof in the preparation of a drug for treating or preventing infections caused by methicillin-resistant, quinolone-resistant, and methicillin and quinolone-multi-resistant Staphylococcus aureus. The rifamycin-quinolizidone coupling molecule and the pharmaceutically acceptable salt thereof provided by the present invention can effectively treat or prevent bacterial infections and diseases caused by methicillin-resistant, quinolone-resistant, and methicillin and quinolone-multi-resistant Staphylococcus aureus; and compared with a pharmaceutical combination of rifamycin and quinolone, the frequency of spontaneous drug resistance occurring is reduced.
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