Benzimidazole scaffold has gained a great deal of attention in the last decades as they exhibit broad-spectrum antibacterial propensity and represent a privileged structure for several biological activities. This review clearly discusses all new approaches in benizmidazole derivatives fabrication and structure optimization to increase their mother nucleus potential applications as antibacterial agents. We discuss several synthetic methods comprising of conventional pathways, and a new paradigm as microwave assisted synthesis, green chemistry methods, and multicomponent reactions. We also discuss structure-activity relationship (SAR) studies focusing on the essential functional groups and structural variations responsible for antibacterial activity. In this review, we provide information about the potential therapeutic applications of these categories of benzimidazole derivatives which may work as a scaffold for the development of new antibacterial agents, and we also try to explain the molecular basis of antibacterial action of benzimidazole derivatives. The current review probes an imperative specter of novel synthesis approaches are reported for enhanced structure of benzimidazoles as antibacterial drug candidates.