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  • Evaluation of novel Hyphodermin derivatives as Glycogen Phosphorylase a inhibitors

    Author(s)
    Loughlin, Wendy A
    Pierens, Gregory K
    Petersson, Maria J
    Henderson, Luke C
    Healy, Peter C
    Griffith University Author(s)
    Healy, Peter C.
    Loughlin, Wendy A.
    Henderson, Luke
    Petersson, Maria J.
    Pierens, Gregory K.
    Year published
    2008
    Metadata
    Show full item record
    Abstract
    The lipophilicity, permeability, solubility, polar surface area and 'rule-of-five' properties were assessed, using QikProp v2.5 (Schr椩nger, Inc.) and ALOGPS 2.1 calculations, for 25 Hyphodermin derivatives. These compounds obeyed the 'rule of five', and the calculated physicochemical values were generally within desired limits. All compounds were tested against Glycogen Phosphorylase a (GPa). Four phenyl and benzyl substituted 2-oxo-hexahydro and tetrahydrobenzo[cd]indole carboxylic acids were identified as novel inhibitors of GPa with estimated IC50 values in the range 0.8-1.3 mM. Molecular modeling of these novel inhibitors ...
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    The lipophilicity, permeability, solubility, polar surface area and 'rule-of-five' properties were assessed, using QikProp v2.5 (Schr椩nger, Inc.) and ALOGPS 2.1 calculations, for 25 Hyphodermin derivatives. These compounds obeyed the 'rule of five', and the calculated physicochemical values were generally within desired limits. All compounds were tested against Glycogen Phosphorylase a (GPa). Four phenyl and benzyl substituted 2-oxo-hexahydro and tetrahydrobenzo[cd]indole carboxylic acids were identified as novel inhibitors of GPa with estimated IC50 values in the range 0.8-1.3 mM. Molecular modeling of these novel inhibitors was used to obtain the main structural features of this class of molecule for future structure-activity relationship studies.
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    Journal Title
    Bioorganic & Medicinal Chemistry
    Volume
    16
    Issue
    11
    DOI
    https://doi.org/10.1016/j.bmc.2008.04.047
    Subject
    Medicinal and biomolecular chemistry
    Organic chemistry
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/21673
    Collection
    • Journal articles

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