Benzoxazoles can be considered as structural isosteres of the naturally occurring nucleic bases adenine and guanine, which allow them to interact easily with polymers of living systems. Benzoxazole nucleus is present in compounds involved in research aimed at evaluating new products that possess interesting biological activities like antimicrobial, CNS activities, antihyperglycemic potentiating activity, analgesic and anti-inflammatory activity. Benzoxazole being a heterocyclic compound, finds use in research as a starting material for the synthesis of larger, usually bioactive structures. Modifications on the benzoxazole nucleus have resulted in a large number of compounds having diverse pharmacological activities. Benzoxazole derivatives have long been focus of research in the field of medicine, due to potential activities exhibited by them. The biological profiles of new generations of benzoxazoles represent much progress with regards to older compounds. Considering all these, we have synthesized and characterized some newer derivatives of benzoxazole and screened them for their biological activities.