Bacterial and parasitic infections rank as the second leading cause of death globally. The persistent rise in antibiotic resistance, particularly against β-lactams, vancomycinand methicillin, poses a significant challenge to public health. The World Health Organization (WHO) has prioritized the fight against antibiotic resistance, recognizing the urgent need for new targets and the development of novel antibiotics. Given that many potential drugs focus on pathogens prioritized by the WHO, which often share characteristics with existing antibiotic classes, fostering resistance, there is an imperative requirement to identify new targets and develop agents that specifically address these challenges. Bacterial peptidoglycan, with its specificity for bacteria and essential role in their survival, has become a focal point of research. Due to the enzymes involved in peptidoglycan biosynthesis being exclusive to bacteria, they represent ideal targets for the discovery of new antimicrobials. Inhibiting these enzymes offers an optimal inhibition profile, where the inhibitors are inactive towards eukaryotic cells but effectively combat bacterial infections. The aim of this review is to introduce the advancements in the synthesis of a series of inhibitors targeting the bacterial transferase MraY, which catalyzes the first membrane-bound step in peptidoglycan biosynthesis. Currently, there are no antibiotics in clinical use that target MraY. By inhibiting MraY, the hope is to mitigate the development of resistance. Natural inhibitors of MraY, based on the aminoarabinosyluridine scaffold, have been known for their biological activity. However, due to their limited antibacterial efficacy, several research groups have embarked on the development of simplified analogues to enhance their therapeutic potential.