The current trend of increasing infections by multidrug-resistant pathogens requires the discovery of novel antimicrobial agents with new target and selective toxicity towards pathogens. Menaquinone is a component of electron transport chains in a majority of anaerobic bacteria and Gram-positive bacteria. Due to its exclusivity in bacteria, menaquinone is thought to be a potential target for development of therapeutically effective antibacterial agents without side effects. In this review, we summarize inhibitors of menaquinone biosynthesis and antibiotics directly targeting menaquinone in bacteria.