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    Cyclosulfamide-based derivatives as inhibitors of noroviruses

    Date
    2011-10-20
    Author
    Dou, Dengfeng
    Mandadapu, Sivakoteswara Rao
    Alliston, Kevin R.
    Kim, Yunjeong
    Chang, Kyeong-Ok
    Groutas, William C.
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    Citation
    European journal of medicinal chemistry. 2011 Oct 20. [Epub ahead of print]
    Abstract
    An optimization campaign focused on improving pharmacological activity and physicochemical properties of a recently-identified class of cyclosulfamide-based norovirus inhibitors has been carried out. Dimeric compound 4 was found to be a ~10-fold more potent norovirus inhibitor (ED(50) 0.4 µM) compared to the original hit, however, isonipecotic acid ester derivatives 7e and 10a were shown to have superior therapeutic indices.
    Description
    Click on the DOI link below to access the article (may not be free).
    URI
    http://dx.doi.org/10.1016/j.ejmech.2011.10.019
    http://hdl.handle.net/10057/4365
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