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    Glycosylated metal chelators as anti-parasitic agents with tunable selectivity


    Reddy, Andrew and Sangenito, Leandro Stefano and Guedes, Arthur de Azevedo and Branguinha, Marta Helena and Kavanagh, Kevin and McGinley, John and Souza dos Santos, André Luis and Velasco-Torrijos, Trinidad (2017) Glycosylated metal chelators as anti-parasitic agents with tunable selectivity. Dalton Transactions, 46 (16). p. 5297. ISSN 1477-9226

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    Abstract

    Trypanosoma cruzi and Leishmania amazonensis are the causative agents of Chagas’ disease and leishmaniasis, respectively. These conditions affect millions of people worldwide, especially in developing countries. As such, there is an urgent need for novel, efficient and cost-effective treatments for these diseases, given the growing resistance and side-effects of current therapies. This work details the synthesis and evaluation of the anti-parasitic activity of novel amino- and iminopyridyl metal chelators, their glycosylated derivatives and some of their metal complexes. Our results revealed the potent and metal-dependent activity for the aminopyridyl compounds: Cu(II) complexes were most effective against T. cruzi trypomastigotes, while Zn(II) complexes presented excellent activity against L. amazonensis promastigotes. In addition, the compounds showed excellent selectivity indexes and very low relative toxicity as judged by in vitro and in vivo studies, respectively, using RAW macrophages and Galleria mellonella larvae model.

    Item Type: Article
    Keywords: Glycosylated metal chelators; anti-parasitic agents; tunable selectivity;
    Academic Unit: Faculty of Science and Engineering > Biology
    Item ID: 11075
    Depositing User: Dr. Kevin Kavanagh
    Date Deposited: 23 Sep 2019 13:53
    Journal or Publication Title: Dalton Transactions
    Publisher: Royal Society of Chemistry
    Refereed: Yes
    URI:

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