Bacterial resistance against antibiotics is a growing threat to the society. Various approaches are used for the development of new resistance-free antibiotics. As an important and growing field is antibacterial prodrugs. Prodrugs, being inactive against bacteria, undergo chemical modification or activation within target bacteria to release the active form of the drug. In this chapter, we summarize common strategies for the development of antibacterial prodrugs including β-lactamase-activated prodrugs, Cephalosporin-3′-diazeniumdiolate prodrugs, glycoside-based prodrugs, pyrimidine nucleoside derivative prodrugs, Carvacrol prodrugs, and antimicrobial peptides-based prodrugs. Short clinical and preclinical advances are highlighted.