Presently, antimicrobial resistance (AMR) is a major global problem, aggravated by the mismanagement of available antibiotics. This not only makes the treatment of patients difficult but also leads to longer hospital stays and increased mortality. Many available antibiotics have lost their efficacy due to excessive and uncontrolled use on plants and animals. Therefore, it is desirable to develop a new generation of antibiotic drugs that can effectively cure diseases and provide rapid relief to patients. The 1,3,4- oxadiazole moiety, which exhibits various biological activities, including antifungal, antibacterial, anticancer, anti-inflammatory, and analgesic, has attracted the attention of medicinal chemists for developing novel drugs to address AMR. This review paper aims to provide a valuable resource for investigators interested in this area of research and is divided into two sections based on the medicinal features of 1,3,4-oxadiazole. The first section covers various synthetic procedures for preparing derivatives of heterocyclic compounds containing a 1,3,4-oxadiazole core, and the second section focuses on the antibacterial activity of the synthesized compounds.