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  • ThesisItemOpen Access
    Green Synthesis, derivatization and structure - activity relationships of bioactive compounds as potential antioxidants and enzyme inhibitors
    (G.B. Pant University of Agriculture and Technology, Pantnagar-263145 (Uttarakhand), 2015-06) Agarwal, Deepali; Kasana, Virendra
    Derivatives of formamide, α-aminophosphonate, 3,4-dihydropyrimidin-2(1H)- one and naphthoquinone were synthesised using green synthetic methods. Calcium chloride dihydrate supported on rice husk (RiH-CaCl2.2H2O) offers simple, efficient and economical solid support method for C-N bond formation for N-formylation of amines at room temperature. Natural acid catalysts, lemon juice (extracted from Citrus limonium) and yogurt (bacterial fermented milk), were developed for one pot synthesis of α-aminophosphonates and amino acid derivatives of α-aminophosphonate under solvent free condition. CaCl2.2H2O offers efficient method for direct carbon-carbon bond formation through soft enolization to promote the Biginelli three component condensation reaction from a diversity of aromatic aldehydes. N-formylated α- aminophosphonate and 3,4-dihydropyrimidin-2(1H)-one derivatives were synthesized using β-cyclodextrin in the presence of ionic liquid, TBAB, in good to excellent yield. Novel derivative of 1, 4-Naphthoquinone was synthesized in excellent yield as pH indicator and chemosensor for Sn2+, Hg2+ and Zn2+. Citrulline and tyrosine derivatives of α-aminophosphonate and compounds with -OH, -OCH3 substituent groups on benzene ring of α-aminophosphonates and 3,4-dihydropyrimidin-2(1H)-ones showed strong antioxidant and enzyme (tyrosinase, α-amylase and α-glucosidase) inhibition activity. N-formylation increased the antioxidant and enzyme inhibition activity of α- aminophosphonates and 3,4-dihydropyrimidin-2(1H)-ones with para -NO2 and -F groups on benzene ring. N-formylated 3,4-dihydropyrimidin-2(1H)-ones were found to increase the Fe2+ chelating activity.