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    Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds 
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    Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds

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    Accepted version (423.8Kb)
    Volume
    117
    Pagination
    179 - 186 (8)
    Publisher
    Elsevier
    Publisher URL
    http://dx.doi.org/10.1016/j.ejmech.2016.04.010
    DOI
    10.1016/j.ejmech.2016.04.010
    Journal
    European Journal of Medicinal Chemistry
    ISSN
    0223-5234
    Metadata
    Show full item record
    Abstract
    A small series of 5-nitro-2-aminothiazole-based amides containing arylpiperazine-, biphenyl- or aryloxyphenyl groups in their core were synthesized and evaluated as anti-trypanosomatid agents. All tested compounds were active or moderately active against Trypanosoma cruzi amastigotes in infected L6 cells and Trypanosoma brucei brucei, four were moderately active against Leishmania donovani axenic parasites while none were deemed active against Trypanosoma brucei rhodesiense. For the most active/moderately active compounds a moderate selectivity against the human infectious parasites was observed. There was a good correlation between lipophilicity (clogP value) versus antileishmanial activity and mammalian cell toxicity with a similar correlation also noted between clogP values and IC50 values against T. cruzi in structurally related subgroups of compounds. Three compounds were more potent as antichagasic agents than benznidazole.
    Authors
    Papadopoulou, MV; Bloomer, WD; Rosenzweig, HS; WILKINSON, SR; Szular, J; Kaiser, M
    URI
    http://qmro.qmul.ac.uk/xmlui/handle/123456789/11848
    Collections
    • Cell and Molecular Biology [192]
    Licence information
    © 2016. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
    Copyright statements
    Copyright © 2016 Published by Elsevier Masson SAS
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