Abstract: The rapid development of antibiotic resistance among bacterial pathogens has threatened to take humans back to the "pre-antibiotic era". The New Delhi metallo-β-lactamase (NDM-1) hydrolyzes nearly all β-lactam antibiotics including carbapenems. Bacterial strains carrying blaNDM-1 gene are termed "superbugs" and clinical inhibitors of NDM-1 have not yet been identified. Discovery of novel NDM-1 inhibitors is a challenging but rewarding research area. This review focuses on the structural characteristics and catalytic mechanisms of NDM-1, and comprehensively summarizes the development of NDM-1 inhibitors in order to facilitate the further development of NDM-1 inhibitors.