Abstract: OBJECTIVE To study the quantitative structure-activity relationship of the antibiotic properties of a series of pyrolines. METHODS Pyroline was acted as a lead compound and new twelve hydroquine compounds were synthesized. Combined with clinic practice, staphylococcus was selected as a pathogenic bacterium by which effective coefficients were measured. RESULTS It followed: Hansch QSAR equation was lg1/MIC=0.035 0π-0.015 3π2+0.178 4σ+0.002 0 MR-1.621 3 I+ 4.441 5, n=13, r=0.808 9, F=2.65(α=0.05). When iso-propylhydroquinone were used to prove the equation, there were some certain effective significance for its equation forecasting compounds' activity. Through selecting significant action parameters, it was followed that there was 58% correlation between indicator variance (I) and antibacterial activity. Therefore, antibacterial mechanism of hydroquinones was carried out by oxidization and reduction reaction. CONCLUSION The experiment provides some certain clue and basis for finding farther effective pyrolines and explaining its action mechanism.