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  • Pyridyl Benzamides as a Novel Class of Potent Inhibitors for the Kinetoplastid Trypanosoma brucei

    Author(s)
    Ferrins, Lori
    Gazdik, Michelle
    Rahmani, Raphael
    Varghese, Swapna
    Sykes, Melissa L
    Jones, Amy J
    Avery, Vicky M
    White, Karen L
    Ryan, Eileen
    Charman, Susan A
    Kaiser, Marcel
    Bergstroem, Christel AS
    Baell, Jonathan B
    Griffith University Author(s)
    Sykes, Melissa L.
    Avery, Vicky M.
    Jones, Amy J.
    Year published
    2014
    Metadata
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    Abstract
    A whole-organism screen of approximately 87000 compounds against Trypanosoma brucei brucei identified a number of promising compounds for medicinal chemistry optimization. One of these classes of compounds we termed the pyridyl benzamides. While the initial hit had an IC50 of 12 μM, it was small enough to be attractive for further optimization, and we utilized three parallel approaches to develop the structure–activity relationships. We determined that the physicochemical properties for this class are generally favorable with particular positions identified that appear to block metabolism when substituted and others that ...
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    A whole-organism screen of approximately 87000 compounds against Trypanosoma brucei brucei identified a number of promising compounds for medicinal chemistry optimization. One of these classes of compounds we termed the pyridyl benzamides. While the initial hit had an IC50 of 12 μM, it was small enough to be attractive for further optimization, and we utilized three parallel approaches to develop the structure–activity relationships. We determined that the physicochemical properties for this class are generally favorable with particular positions identified that appear to block metabolism when substituted and others that modulate solubility. Our most active compound is 79, which has an IC50 of 0.045 μM against the human pathogenic strain Trypanosoma brucei rhodesiense and is more than 4000 times less active against the mammalian L6 cell line.
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    Journal Title
    Journal of Medicinal Chemistry
    Volume
    57
    DOI
    https://doi.org/10.1021/jm500191u
    Subject
    Medicinal and Biomolecular Chemistry not elsewhere classified
    Medicinal and Biomolecular Chemistry
    Organic Chemistry
    Pharmacology and Pharmaceutical Sciences
    Publication URI
    http://hdl.handle.net/10072/140923
    Collection
    • Journal articles

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