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    Synthesis, biological profiling and mechanistic studies of 4-aminoquinoline-based heterodimeric compounds with dual trypanocidal–antiplasmodial activity.

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    Wright_Bioorganic_and_Medicinal_Chemistry.pdf (796.8Kb)
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    Publication date
    2015-08
    Author
    Sola, I.
    Castellà, S.
    Viayna, E.
    Galdeano, C.
    Taylor, M.C.
    Gbedema, Stephen Y.
    Pérez, B.
    Clos, M.V.
    Jones, D.C.
    Fairlamb, A.H.
    Wright, Colin W.
    Kelly, J.M.
    Muñoz-Torrero, D.
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    Keyword
    Molecular hybridization; Trypanocidal agents; Antimalarial agents; Trypanothione reductase inhibitors; Inhibitors of β-haematin formation; Brain permeability
    Rights
    © 2015 Elsevier. Reproduced in accordance with the publisher's self-archiving policy. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
    Peer-Reviewed
    yes
    
    Metadata
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    Abstract
    Dual submicromolar trypanocidal–antiplasmodial compounds have been identified by screening and chemical synthesis of 4-aminoquinoline-based heterodimeric compounds of three different structural classes. In Trypanosoma brucei, inhibition of the enzyme trypanothione reductase seems to be involved in the potent trypanocidal activity of these heterodimers, although it is probably not the main biological target. Regarding antiplasmodial activity, the heterodimers seem to share the mode of action of the antimalarial drug chloroquine, which involves inhibition of the haem detoxification process. Interestingly, all of these heterodimers display good brain permeabilities, thereby being potentially useful for late stage human African trypanosomiasis. Future optimization of these compounds should focus mainly on decreasing cytotoxicity and acetylcholinesterase inhibitory activity.
    URI
    http://hdl.handle.net/10454/7485
    Version
    Accepted Manuscript
    Citation
    Sola I, Castella S, Viayna E et al (2015) Synthesis, biological profiling and mechanistic studies of 4-amonoquinoline-based heterodimeric compounds with dual trypanocidal-antiplasmodial activity. Bioorganic and Medicinal Chemistry. 23(16): 5156-5167.
    Link to publisher’s version
    http://dx.doi.org/10.1016/j.bmc.2015.01.031
    Type
    Article
    Collections
    Life Sciences Publications

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