Background: Benzoxazine is one of the most important privileged scaffolds in medicinal chemistry. Compounds bearing benzoxazine moiety usually have a variety of biological activities, such as anti-inflammatory, anti-microbial, anti-tuberculosis, anti-oxidant and anti-cancer activities. The fascinating bioactivity profile of benzoxazine scaffold in various fields has prompted medicinal chemists to design and discover novel benzoxazine derivatives as potential therapeutic candidates with the desired biological properties. Objective: This review aimed to provide a comprehensive elucidation on the recent advances of benzoxazine derivatives in medicinal chemistry. Method: We have searched the recent literatures about benzoxazine derivatives from the online resources and databases, such as pubmed, scifinder and google scholar. Conclusion: Benzoxazine is a versatile structure and building block in medicinal chemistry. Benzoxazine derivatives have gained considerable attention from medicinal chemists due to their various pharmacological properties and multiple modification sites. This review might help medicinal chemists to seek for new drug candidates with better bioactivities and pharmacokinetics properties.

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