Oxadiazoles and their derivatives represent a significant class of organic compounds, wielding profound implications in both the realms of medicinal science and heterocyclic rings housing oxygen and nitrogen atoms, has garnered attention owing to their multifaceted. Pharmacological potential. The diverse array of biological activities exhibited by oxadiazole derivatives spans antimicrobial, anti-inflammatory, anti-cancer and anti-viral effects. Beyond medicinal applications, these compounds showcase utility in agriculture, with their herbicidal, insecticidal and fungicidal properties enabling their role as effective plant protection agents. Researchers have been focusing on the synthesis and exploration of these compounds for their potential in drug development. This review article is an in-depth exploration of diverse synthetic methodologies for oxadiazole and its derivatives while highlighting their associated pharmacological activities. It offers valuable insights into this class of compounds’ versatile chemistry and potential therapeutic applications.