Thiazolo[3,2-b][1,2,4]triazole derivatives have emerged as a promising class of fused heterocyclic scaffolds in medicinal chemistry. Over the past decade, this class of compounds has attracted considerable attention as potential leads for developing therapeutically relevant agents. Owing to the remarkable therapeutic profile of this scaffold, in the present review, we aim to provide a comprehensive overview of the biological significance of thiazolo[3,2-b][1,2,4]triazole derivatives reported between 2015 and 2026, emphasizing anticancer, antimicrobial, antiviral, analgesic, anti-inflammatory, and enzyme-inhibitory activities. To get insights into the structural features and modifications essential for the activity, detailed structure-activity relationship (SAR) studies are carried out. Additionally, to better understand the binding mechanism and to support the in vitro results, molecular docking studies are discussed. The present review may help researchers working in the field of medicinal chemistry for designing highly potent, novel, multifunctional derivatives that exhibit excellent target selectivity and drug-like characteristics.
