Coumarin Derivatives as Potential Antibacterial Agents and Study of Structure-Activity Relationship against Gram-Negative Escherichia Coli: Mechanisms and Future Prospects

Abstract

Coumarin and its derivatives have garnered significant attention due to their diverse pharmacological properties, including potent antibacterial activity. This review focuses on the potential of coumarin derivatives as antibacterial agents, particularly against Gram-negative Escherichia coli (E. coli). E. coli is known for its resistance to conventional antibiotics, mainly due to its complex outer membrane structure and various resistance mechanisms. Coumarin derivatives have shown promising results in inhibiting E. coli, with several proposed mechanisms of action, including interference with bacterial DNA gyrase, cell membrane disruption, and inhibition of quorum sensing. Structure-activity relationship (SAR) studies reveal that modifications in the coumarin core, such as hydroxylation, halogenation, or alkylation, can significantly enhance antibacterial activity. Furthermore, combining coumarin derivatives with existing antibiotics could offer synergistic effects, helping to overcome bacterial resistance. While in vitro studies are encouraging, further research, including in vivo studies and clinical trials, is necessary to explore the therapeutic potential of coumarin-based drugs fully. Developing coumarin-loaded nanocarriers could also improve targeted drug delivery and efficacy, opening new avenues for treating antibiotic-resistant E. coli infections.

Conclusion:  The current research will aid in logically developing coumarin-bridging antibacterial medications for E. coli resistance.