The globally growing antimicrobial resistance seriously threatens human health, increasing efforts have been devoting to the development of novel antibiotics. Naphthalimides contain a special skeleton of cyclic double imides and the naphthalene framework, this unique structure can exert multitargeting abilities which are helpful to overcome the escalating issue of resistance. Therefore, research in connection with the development of naphthalimides as novel antimicrobial agents is becoming progressively active. It has been revealed that naphthalimides as novel structural skeleton of multitargeting promising antibiotics could not only target DNAs and enzymes, disturb membrane, produce reactive oxygen species,