Green Synthesis, derivatization and structure - activity relationships of bioactive compounds as potential antioxidants and enzyme inhibitors
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Date
2015-06
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Publisher
G.B. Pant University of Agriculture and Technology, Pantnagar-263145 (Uttarakhand)
Abstract
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.
Description
Thesis-PhD
Keywords
enzymes, inhibitors, antioxidants, biological activity, formamide, derivatives, catalysts, bioactive compounds