As we know that, Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring and is derived from furan by substitution of two methylene groups (=CH) with two pyridine type nitrogen (-N=) [1,2]. There are three known isomers that is 1,2,4-oxadiazole, 1,2,3-oxadiazole and 1,2,5-oxadiazole (Figure 1.0). However, 1,3,4-oxadiazole and 1,2,4-oxadiazole are better known, and more widely studied by researchers because of their many important chemical and biological properties. Among heterocyclic compounds, 1,3,4-oxadiazole has become an important construction motif for the development of new drugs. Compounds containing 1,3,4-oxadiazole cores have a broad biological activity spectrum including antibacterial, antifungal, analgesic, anti-inflammatory, antiviral, anticancer, antihypertensive, anticonvulsant, and anti-diabetic properties. They have also attracted interest in medicinal chemistry as surrogates (bioisosteres) for carboxylic acids, esters and carboxamides. The ability of 1,3,4-oxadiazole heterocyclic compounds to undergo various chemical reactions has made them important for molecule planning because of their privileged structure, which has enormous biological potential. Some examples of compounds containing the 1,3,4-oxadiazole unit currently used in clinical medicine are: Raltegravir as an antiretroviral drug and Zibotentan as an anticancer agent. They possesses various other biological activities and having various synthetic approaches, some of them are presented here in the aritcle. Keywords: Oxadiazoles synthetic approaches, biologically active ozadiazoles, oxadiazoles as anticancers etc.