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  • The synthesis, antimalarial activity and CoMFA analysis of novel aminoalkylated quercetin analogs

    Author(s)
    Helgren, Travis R
    Sciotti, Richard J
    Lee, Patricia
    Duffy, Sandra
    Avery, Vicky M
    Igbinoba, Osayawemwen
    Akoto, Matthew
    Hagen, Timothy J
    Griffith University Author(s)
    Duffy, Sandra
    Avery, Vicky M.
    Year published
    2015
    Metadata
    Show full item record
    Abstract
    A series of novel aminoalkylated quercetin analogs, prepared via the Mannich reaction of various primary and secondary amines with formaldehyde, were tested for antimalarial activity. The compounds were screened against three drug resistant malarial strains (D6, C235 and W2) and were found to exhibit sub-micromolar activity across all three strains (0.065–13.0 μM). The structure–activity relationship determined from the antimalarial activity data suggests the inclusion of phenethyl amine sidechains on the quercetin scaffolding is necessary for potent activity. Additionally, the most active compounds ((5) and (6)) were tested ...
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    A series of novel aminoalkylated quercetin analogs, prepared via the Mannich reaction of various primary and secondary amines with formaldehyde, were tested for antimalarial activity. The compounds were screened against three drug resistant malarial strains (D6, C235 and W2) and were found to exhibit sub-micromolar activity across all three strains (0.065–13.0 μM). The structure–activity relationship determined from the antimalarial activity data suggests the inclusion of phenethyl amine sidechains on the quercetin scaffolding is necessary for potent activity. Additionally, the most active compounds ((5) and (6)) were tested for both early and late stage anti-gametocytocidal activity. Finally, the antimalarial activity data were utilized to construct comparative molecular field analysis (CoMFA) models to be used for further compound refinement.
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    Journal Title
    Bioorganic and Medicinal Chemistry Letters
    Volume
    25
    Issue
    2
    DOI
    https://doi.org/10.1016/j.bmcl.2014.11.039
    Subject
    Medicinal and biomolecular chemistry
    Medicinal and biomolecular chemistry not elsewhere classified
    Organic chemistry
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/101303
    Collection
    • Journal articles

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