5-O-methylglovanon (5-O-MG) is a bioactive compound that was first isolated and characterized from Glycosmis plants. In this study, we found that chemically synthesized 5-O-MG has antimicrobial ability against eleven clinical ampicillin resistant Staphylococcus aureus and S. epidermidis isolates. The MICs of 5-O-MG against the S. aureus and S. epidermidis isolates were $12.5-50{mu}g/mL$ and $25-50{mu}g/mL$, respectively. In combination with ampicillin, a synergistic interaction between 5-O-MG and ampicillin against the eleven resistant Staphylococcus isolates was observed, with fractional inhibitory concentration indices of 0.03-0125. Moreover, the anti-staphylococcal activity of 5-O-MG in combination with ampicillin was comparable with that of clavulanic acid in combination with ampicillin. The drug combination had no antagonistic effects when tested against any of the strains. Time-killing assays confirmed the synergy between 5-O-MG and ampicillin (p < 0.01). The combination of these two agents yielded greater than a 2 $log_{10}$ cfu/mL decrease in comparison with 5-O-MG or ampicillin alone. These findings suggest that 5-O-MG is a promising compound with the potential for future anti-staphylococcal drug development.