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Piperonal, an important aromatic aldehyde containing the benzene ring fused to 1, 3- dioxolane moiety, widely occurred in nature and known for its fragrance similar to vanillin and cherry. Alterations in its structural features led to the access of a wide range of piperonal derivatives viz. pyrazolines, chalcones, benzothiazepines, benzoxazoles, triazoles etc. having remarkable pharmacological properties like antimicrobial, anticancer, antidiabetic, antitubercular activities, etc. Therefore, the present study has been designed to highlight the progress made in the area of piperonal and its derivatives till date with respect to their synthesis and pharmacological activities. This may facilitate the synthesis of more novel derivatives with improved biological activities. Various search engines like google, Pubmed, Scopus etc. were used to gather the related information using different keywords.

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