Acetoxy drug: Protein transacetylase catalyses the transfer of acetyl groups from acetylated polyphenolic peracetates (PAs) to the receptor proteins and modulates the activity of proteins and alters the effect of various enzymes like Glutathione S-transferase, NADPH Cytochrome c Reductase and Nitric Oxide Synthase (NOS). Accordingly, Polyphenolic acetates were found effective in the inhibition of ADP induced platelet aggregation, because of which, the acetoxy derivatives of several classes of polyphenols were found to be the substrates of TAase. Our group has synthesized a number of heterocyclic compounds e.g. benzofurans and quinolones etc. These compounds were screened for various biological activities e.g. antioxidant, antiplatelet aggregation, and antimicrobial activities.