A library of 24 glycoconjugates related to glycosylated b-amino acid derivative (I) was been prepared and screened against DNA topoisomerase-II of the filarial parasite S. cervi. Among these, compound 6 was found to be a potent inhibitor of DNA topoisomerase-II with 95percent inhibition at 1.0?mM. Furthermore, compound 6 was at least three times more potent than the lead compound, glycosylated b-amino acid derivative I.
Keywords: DNA Topoisomerase II, filarial parasites, nalidixic acid, Fmoc-protected amino acids, propanoyl Sieber Amide Resin, negative ninhydrin test, Cys-Gly adornment
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Published on: 01 March, 2012
Page: [237 - 244]