Oxadiazole, a heterocyclic nucleus has attracted a wide attention of the chemist in search for the new therapeutic molecules. Out of its four possible isomers, 1, 3, 4-oxadiazole is widely exploited for various applications. A numbers of therapeutic agents such as HIV-integrase inhibitor raltagravir, a nitrofuran antibacterial furamizole, a potent PDF inhibitor BB-83698, antihypertensive agents tiodazosin and nesapidil are based on 1,3,4-oxadiazole moiety. The 1, 3, 4-oxadiazole undergoes number of reactions including electrophillic substitution, nucleophilic substitution, thermal and photochemical. The present review attempts to summarize the various routes of synthesis and the reactions of 1, 3, 4-oxadiazole and its derivatives and focus on their biological potential.