Benzoxazine and its derivatives are used in organic synthesis for building natural and designed synthetic compounds and they have been frequently utilized as suitable skeletons for the design of biologically active compound. This review covers updated information on the most active benzoxazine derivatives that have been reported to show considerable pharmacological actions such as antimicrobial, antimycobacterial, anti-diabetic, antihypolipidaemic, and antidepressant. It can act as an important tool for chemists to develop newer benzoxazine derivatives that may prove to be better agents in terms of efficacy and safety.