Abstract:Pathogens exhibit strong antibiotic resistance, a major cause of which is biofilm (BF) formation. The eradication of bacteria is extremely difficult once biofilms have formed as biofilms can lead to persistent infections in patients and trigger a variety of chronic diseases, which cause a heavy burden on the global healthcare system. Pillararenes are novel macrocyclic compounds with unique pillar-shaped architectures, which have attracted wide attention owing to their potential applications in the development of functionalized and bioactive materials. In addition, they have broad application prospects in the prevention and control of antibiotic resistance. This article reviewed the activities and mechanisms of pillar[5]arene derivatives against bacterial pathogens, especially the inhibitory effect on biofilms. On this basis, researchers can explore new antibacterial and bactericidal strategies and employ non-traditional methods to solve antibiotic resistance. This review is expected to provide a theoretical basis for the development of new agents to control biofilm or treat bacterial infections.