The domain of medicinal chemistry has witnessed a notable surge of interest in triazoles owing to their unique structural characteristics and wide range of applications. The versatility of their synthesis methods has facilitated the creation of compound libraries with remarkable pharmacological activities, including antiviral, antiepileptic, anxiolytic, hypnotic/sedatives anticancer, antifungal, and antidepressant activities. Several techniques have been documented in the literature for generating 1,2,4‐triazole derivatives. The mechanisms governing the pharmacological effects of the formulations containing 1,2,4‐triazoles were elucidated and made clear. In addition to reviewing existing marketed formulations, this review explores emerging trends and innovations in this field. This review offers a comprehensive perspective on the importance of triazoles for influencing contemporary research, fostering innovation, and driving technological progress.