Abstract
Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attentionbecause of its unique bioisosteric properties and an unusually wide spectrum of biological activities.Thus, it is a perfect framework for the novel drug development. After a century since the1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists'attention, leading to the discovery of a few presently accessible drugs containing 1,2,4-oxadiazoleunit. It is worth noting that the interest in a 1,2,4-oxadiazoles' biological application has been doubledin the last fifteen years. Herein, after a concise historical introduction, we present a comprehensiveoverview of the recent achievements in the synthesis of 1,2,4-oxadiazole-based compounds and themajor advances in their biological applications in the period of the last five years as well as briefremarks on prospects for further development.