Countless bioactive compounds are having the oxadiazole nucleus showing clinical and biological applications. Oxadiazole is a heterocyclic compound of the azole family that has gained increasing attention due to its wide therapeutic potential. Many significant synthetic medicinal compounds have the oxadiazole scaffold, which provided a good treatment idea and binds with high affinity to a variety of receptors to aid in the development of novel beneficial derivatives. Numerous researchers have worked to create novel oxadiazole compounds and evaluate them for how they affect inflammation, tumor, epilepsy, microbial infections, and analgesic properties. The present review article summarizes some of the oxadiazole derivatives synthesized and their biological activities and can be a useful guide for researchers working on this scaffold.