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    Huprines as a new family of dual acting trypanocidal–antiplasmodial agents

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    Publication date
    2011
    Author
    Defaux, J.
    Sala, M.
    Formosa, X.
    Galdeano, C.
    Taylor, M.C.
    Kelly, J.M.
    Wright, Colin W.
    Camps, P.
    Muñoz-Torrero, D.
    Alobaid, Waleed A.A.
    Keyword
    Trypanocidal agents; Antimalarial agents; 4-Aminoquinolines; Huprines
    Peer-Reviewed
    Yes
    
    Metadata
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    Abstract
    A series of 19 huprines has been evaluated for their activity against cultured bloodstream forms of Trypanosoma brucei and Plasmodium falciparum. Moreover, cytotoxicity against rat myoblast L6 cells was assessed for selected huprines. All the tested huprines are moderately potent and selective trypanocidal agents, exhibiting IC50 values against T. brucei in the submicromolar to low micromolar range and selectivity indices for T. brucei over L6 cells of approximately 15, thus constituting interesting trypanocidal lead compounds. Two of these huprines were also found to be active against a chloroquine-resistant strain of P. falciparum, thus emerging as interesting trypanocidal–antiplasmodial dual acting compounds, but they exhibited little selectivity for P. falciparum over L6 cells.
    URI
    http://hdl.handle.net/10454/7468
    Version
    No full-text available in the repository
    Citation
    Defaux J, Sala M, Formosa X et al (2011) Huprines as a new family of dual acting trypanocidal-antiplasmodial agents. Bioorganic and Medicinal Chemistry. 19(5): 1702-1707.
    Link to publisher’s version
    http://dx.doi.org/10.1016/j.bmc.2011.01.028
    Type
    Article
    Collections
    Life Sciences Publications

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