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    Inhibition of noroviruses by piperazine derivatives

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    Groutas_2012a (7.046Kb)
    Date
    2012-01
    Author
    Dou, Dengfeng
    He, Guijia
    Mandadapu, Sivakoteswara Rao
    Aravapalli, Sridhar
    Kim, Yunjeong
    Chang, Kyeong-Ok
    Groutas, William C.
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    Citation
    Dou, D., G. He, S.R. Mandadapu, S. Aravapalli, Y. Kim, K.O. Chang, and W.C. Groutas. 2012. "Inhibition of noroviruses by piperazine derivatives". Bioorganic & Medicinal Chemistry Letters. 22 (1): 377-379.
    Abstract
    There is currently an unmet need for the development of small-molecule therapeutics for norovirus infection. The piperazine scaffold, a privileged structure embodied in many pharmacological agents, was used to synthesize an array of structurally-diverse derivatives which were screened for anti-norovius activity in a cell-based replicon system. The studies described herein demonstrate for the first time that functionalized piperazine derivatives possess anti-norovirus activity. Furthermore, these studies have led to the identification of two promising compounds (6a and 9I) that can be used as a launching pad for the optimization of potency, cytotoxicity, and drug-like characteristics.
    Description
    Click on the DOI link below to access the article (may not be free).
    URI
    http://hdl.handle.net/10057/4488
    http://dx.doi.org/10.1016/j.bmcl.2011.10.122
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