Design, Synthesis and Activity Against Drug‐Resistant Bacteria Evaluation of 1H‐Pyrazole‐[3,4‐b] Pyridine Derivatives

Abstract

AbstractThe urgent need for novel antibiotics with potent activity against drug‐resistant bacteria is paramount in light of the escalating problem of antibiotic resistance. In this study, we evaluate the antibacterial efficacy of a series of newly designed and synthesized 1H pyrazole‐[3,4‐b]pyridine derivatives against various Gram‐positive and Gram‐negative bacterial strains. Among these derivatives, compound 15 q exhibits comparable antibacterial activity to the established medication Linezolid, demonstrating a minimum inhibitory concentration (MIC) value of 2 μg/mL against both the clinically resistant strain S. aureus M20 and the Gram‐positive bacterium S. aureus ATCC25923. Molecular docking analysis reveals that compound 15 q can interact with nucleotide residue G2505, providing initial insights into its underlying molecular mechanism responsible for its antibacterial activity. Therefore, compound 15 q holds great promise as a lead compound for potential therapeutic interventions against bacterial infections.