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With the development of antimicrobial agents, researchers have developed new strategies through key regulatory systems to block the expression of virulence genes without affecting bacterial growth. This strategy can minimize the selective pressure that leads to the emergence of resistance. Quorum sensing (QS) is an intercellular communication system that plays a key role in the regulation of bacterial virulence and biofilm formation. Studies have revealed that the QS system controls 4–6% of the total number of <i>P. aeruginosa</i> genes, and quorum sensing inhibitors (QSIs) could be a promising target for developing new prevention and treatment strategies against <i>P. aeruginosa</i> infection. In this study, four series of phenyloxadiazole and phenyltetrazole sulfoxide derivatives were synthesized and evaluated for their inhibitory effects on <i>P. aeruginosa</i> PAO1 biofilm formation. Our results showed that <b>5b</b> had biofilm inhibitory activity and reduced the production of QS-regulated virulence factors in <i>P. aeruginosa</i>. In addition, silico molecular docking studies have shown that <b>5b</b> binds to the <i>P. aeruginosa</i> QS receptor protein LasR through hydrogen bond interaction. Preliminary structure–activity relationship and docking studies show that <b>5b</b> has broad application prospects as an anti-biofilm compound, and further research will be carried out in the future to solve the problem of microbial resistance.