Bacterial infections are account for the majority of hospital-acquired and community-acquired infections. The emergency and widespread of drug-resistant pathogens has further worsened the situation. In recent years, various isatin derivatives have been screened for their anti-bacterial activities, and some of them demonstrated promising in?vitro and in?vivo potency. This review covers the recent advances of isatin derivatives including isatin-azole, isatin-quinoline/quinolone, isatin-furan/coumarin, isatin-hydrazone/(thio)semicarbazone, isatin dimers and isatin-indole hybrids as potential anti-bacterial agents. The enriched structure-activity relationship may pave the way for further rational development of isatin derivatives with broader spectrum, higher potency, lower toxicity and multiple mechanisms of action.