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The global threat of infectious diseases has been aggravated by the emergence of bacterial resistance to antibiotics. To combat the situation, 1,2,4-triazoles and their derivatives have a distinct role in the field of medicinal and pharmaceutical chemistry. The 1,2,4-triazole scaffold has emerged as a privileged structure in medicinal chemistry due to its broad spectrum of biological activities, particularly its potent antibacterial properties. Over the years, extensive research has been conducted to explore synthetic strategies for 1,2,4-triazole derivatives and evaluate their antibacterial potential. This review comprehensively summarizes recent advances in synthetic methodologies, including conventional, green, and catalysed approaches, as well as innovations in functional group modifications that emphasize their antibacterial properties from 2009 to the present. This review provides a critical appraisal of the progress made in the field and identifies challenges and opportunities for the future development of 1,2,4-triazole derivatives as antibacterial agents. The findings aim to guide researchers in designing novel derivatives with enhanced potency, selectivity, and pharmacokinetic profiles.
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