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    Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 2CL Protease

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    Mehzabeen_2016.pdf (1.555Mb)
    Issue Date
    2016-03-10
    Author
    Damalanka, Vishnu C.
    Kim, Yunjeong
    Alliston, Kevin R.
    Weerawarna, Pathum M.
    Kankanamalage, Anushka C. Galasiti
    Lushington, Gerald H.
    Mehzabeen, Nurjahan
    Battaile, Kevin P.
    Lovell, Scott
    Chang, Kyeong-Ok
    Groutas, William C.
    Publisher
    American Chemical Society
    Type
    Article
    Article Version
    Scholarly/refereed, author accepted manuscript
    Rights
    This document is the Accepted Manuscript version of a Published Work that appeared in final form in the Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/acs.jmedchem.5b01464.
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    Abstract
    Human noroviruses are the primary causative agents of acute gastroenteritis and a pressing public health burden worldwide. There are currently no vaccines or small molecule therapeutics available for the treatment or prophylaxis of norovirus infections. Norovirus 3CL protease plays a vital role in viral replication by generating structural and nonstructural proteins via the cleavage of the viral polyprotein. Thus, molecules that inhibit the viral protease may have potential therapeutic value. We describe herein the structure-based design, synthesis, and in vitro and cell-based evaluation of the first class of oxadiazole-based, permeable macrocyclic inhibitors of norovirus 3CL protease.
    URI
    http://hdl.handle.net/1808/23729
    DOI
    https://doi.org/10.1021/acs.jmedchem.5b01464
    Collections
    • Higuchi Biosciences Center Scholarly Works [54]
    Citation
    Damalanka, V. C., Kim, Y., Alliston, K. R., Weerawarna, P. M., Galasiti Kankanamalage, A. C., Lushington, G. H., … Groutas, W. C. (2016). Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 3CL Protease. Journal of Medicinal Chemistry, 59(5), 1899–1913. http://doi.org/10.1021/acs.jmedchem.5b01464

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    Contact KU ScholarWorks
    785-864-8983
    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    785-864-8983

    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    Image Credits
     

     

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