One of the triazole tautomers, 1,2,4‐triazole derivatives, has a wide range of biological activities that suggest its potential therapeutic utility in medicinal chemistry. These actions include anti‐inflammatory, anti‐cancer, anti‐bacterial, anti‐tuberculosis, and anti‐diabetic effects. The review highlights anti‐inflammatory effect of 1,2,4‐triazoles in relation to their ability to disrupt significant inflammatory mediators and pathways. We present in‐silico data that illuminate the triazoles capacity to inhibit cell division, encourage apoptosis, and stop metastasis in a range of cancer models. This review looks at the bactericidal and bacteriostatic properties of 1,2,4‐triazole derivatives, with a focus on their potential efficacy against multi‐drug resistant bacterial infections and their usage in tuberculosis therapy. In order to better understand these substances' potential anti‐diabetic benefits, this review also looks at how they affect glucose metabolism regulation and insulin responsiveness. Based on information provided, it can be concluded that 1,2,4‐triazole derivatives are a promising class of diverse therapeutic agents with potential utility in a range of disorders. Their development and improvement might herald a new era of medical care that will be immensely advantageous to both patients and medical community as a whole. Additionally, this study encourages more research into these substances and their enhancement for use in pharmaceutical development.