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    Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 1. Sildenafil analogs

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    TbrPDEB - Sildenafil Paper_Revision_FINAL.pdf (107.5Kb)
    Date
    2012-01
    Author
    Wang, Cuihua  Concept link
    Ashton, Trent D.  Concept link
    Gustafson, Alden  Concept link
    Bland, Nicholas D.  Concept link
    Ochiana, Stefan O.  Concept link
    Campbell, Robert K.  Concept link
    Pollastri, Michael P.  Concept link
    Metadata
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    Citable URI
    https://hdl.handle.net/1912/5036
    As published
    https://doi.org/10.1016/j.bmcl.2012.01.119
    Keyword
     Neglected disease; Trypanosoma brucei; Target repurposing; Phosphodiesterase inhibitors; TbrPDEB1; PDE5; Sildenafil 
    Abstract
    Parasitic diseases, such as African sleeping sickness, have a significant impact on the health and well-being in the poorest regions of the world. Pragmatic drug discovery efforts are needed to find new therapeutic agents. In this report we describe target repurposing efforts focused on trypanosomal phosphodiesterases. We outline the synthesis and biological evaluation of analogs of sildenafil (1), a human PDE5 inhibitor, for activities against trypanosomal PDEB1 (TbrPDEB1). We find that, while low potency analogs can be prepared, this chemical class is a sub-optimal starting point for further development of TbrPDE inhibitors.
    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): 2579-2581, doi:10.1016/j.bmcl.2012.01.119.
    Collections
    • Josephine Bay Paul Center in Comparative Molecular Biology and Evolution
    Suggested Citation
    Preprint: Wang, Cuihua, Ashton, Trent D., Gustafson, Alden, Bland, Nicholas D., Ochiana, Stefan O., Campbell, Robert K., Pollastri, Michael P., "Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 1. Sildenafil analogs", 2012-01, https://doi.org/10.1016/j.bmcl.2012.01.119, https://hdl.handle.net/1912/5036
     

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