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    Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 2. Tadalafil analogs

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    Pollastri_TbrPDE_Tadalafil_Revision_02022012.pdf (104.1Kb)
    Date
    2012-02-02
    Author
    Ochiana, Stefan O.  Concept link
    Gustafson, Alden  Concept link
    Bland, Nicholas D.  Concept link
    Wang, Cuihua  Concept link
    Russo, Michael J.  Concept link
    Campbell, Robert K.  Concept link
    Pollastri, Michael P.  Concept link
    Metadata
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    Citable URI
    https://hdl.handle.net/1912/5037
    As published
    https://doi.org/10.1016/j.bmcl.2012.01.118
    Keyword
     Neglected disease; Trypanosoma brucei; Target repurposing; Phosphodiesterase inhibitors; TbrPDEB1; PDE5; Tadalafil 
    Abstract
    In this report we describe our ongoing target repurposing efforts focused on discovery of inhibitors of the essential trypanosomal phosphodiesterase TbrPDEB1. This enzyme has been implicated in virulence of Trypanosoma brucei, the causative agent of human African trypanosomiasis (HAT). We outline the synthesis and biological evaluation of analogs of tadalafil, a human PDE5 inhibitor currently utilized for treatment of erectile dysfunction, and report that these analogs are weak inhibitors of TbrPDEB1.
    Description
    Author Posting. © The Author(s), 2012. This is the author's version of the work. It is posted here by permission of Elsevier B.V. for personal use, not for redistribution. The definitive version was published in Bioorganic & Medicinal Chemistry Letters 22 (2012): 2582-2584, doi:10.1016/j.bmcl.2012.01.118.
    Collections
    • Josephine Bay Paul Center in Comparative Molecular Biology and Evolution
    Suggested Citation
    Preprint: Ochiana, Stefan O., Gustafson, Alden, Bland, Nicholas D., Wang, Cuihua, Russo, Michael J., Campbell, Robert K., Pollastri, Michael P., "Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 2. Tadalafil analogs", 2012-02-02, https://doi.org/10.1016/j.bmcl.2012.01.118, https://hdl.handle.net/1912/5037
     

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