Infectious illnesses resulting from antibiotic resistance are the primary contributor to global mortality. The escalating morbidity and mortality associated with bacterial resistance to antibiotics poses a significant challenge to global public health. Hence, there exists a pressing requirement to formulate innovative antimicrobial agents. From this standpoint, the study demonstrates the synthesis and characterization of a novel set of ligands known as Pyridine-2,6-dicarboxamides, along with their corresponding complexes involving Cu(II) and Zn(II) ions. The synthesized compounds were subjected to screening against five bacterial strains, namely Acinetobacter baumannii, Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, and Klebsiella pneumoniae. The ligands, along with their Cu(II) and Zn(II) complexes, exhibited significant efficacy against S. aureus, with minimum inhibitory concentrations (MICs) ranging from 2-16 μg/mL and 4-64 μg/mL, respectively. Furthermore, these compounds shown little hemolytic and cytotoxic effects. The main cause of bacterial cell death has been substantiated by SEM and AFM imaging experiments to be the breakdown of the cell wall. Furthermore, the docking outcomes were consistent with the findings of the biological investigation, suggesting that the antibacterial efficacy of L¹¹ can be ascribed to its interaction with the S. aureus MurB enzyme located in the cell wall. The lead drug exhibited significant efficacy against Methicillin-resistant S. aureus and Vancomycin-resistant S. aureus clinical isolates, as evidenced by minimum inhibitory concentration (MIC) values ranging from 2 to 4 μg/mL. The utilization of in-vivo rodent models to study dental biofilm has demonstrated enhanced oral hygiene through the suppression of biofilm development upon treatment with L¹¹ and CuL¹¹. Collectively, the research provided insights into a category of highly effective antibacterial and antibiofilm substances that can be utilized to battle infections caused by S. aureus.

Kajal Chaudhary

Indian Institute of Technology Kanpur, India

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