This review constitutes a methods of preparation and biological activities of some substituted benzoxazoles. Benzoxazole moieties have attracted special attention in chemistry and biochemistry because of their structural similarity with nucleic bases, such as adenine and guanine, which allows their easy interaction with the biopolymers in living system. These compounds possess a wide range of biological activities such as antibacterial, antifungal, antiviral, anticancer activities and various other activities. This review may help medicinal chemists to develop newer compounds possessing benzoxazole moiety that could be better agents in term of efficacy and safety.