Benzoxazole nucleus is one of the most important heterocyclic compounds exhibiting remarkable pharmacological activities. Benzoxazole constitute an important class of therapeutic compounds and efforts were made to synthesize varied derivatives in order to claim their potential biological profiles. Variety of substituted benzoxazole derivatives that have shown various considerable biological activities such as antimicrobial, antiinflammatory, analgesic, antifungal, herbicidal, antiplatelets, anticonvulsants, antitumor, anticancer, anti-alzheimer's, antihyperglycemic, melatoninergic ligands, antitubercular, anti-HIV, anthelmintic, DNA topoisomerase inhibitor, cholesterol ester transfer protein inhibitor and miscellaneous activities. Although benzoxazoles are very common heterocyclic compounds now a day, but still the results shown by previous studies emerge the fascination about the molecule. The review focuses out various important synthetic derivatives of benzoxazole and their associated pharmacological profiles which may in turn helpful to the information seekers to develop some novel derivatives of medicinal interest. The review provides a broad overview of the synthesis and pharmacological 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.