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Novel influenza polymerase PB2 inhibitors for the treatment of influenza A infection

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  • Novel influenza polymerase PB2 inhibitors for the treatment of influenza A infection

    Bioorg Med Chem Lett. 2019 Aug 24:126639. doi: 10.1016/j.bmcl.2019.126639. [Epub ahead of print]
    Novel influenza polymerase PB2 inhibitors for the treatment of influenza A infection.

    Zhang H1, Zhou L1, Amichai S1, Zandi K1, Cox B1, Schinazi R1, Amblard F2.
    Author information

    1 Center for AIDS Research, Global Virus Network, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA. 2 Center for AIDS Research, Global Virus Network, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA. Electronic address: famblar@emory.edu.

    Abstract

    Exploration of the chemical space of known influenza polymerase PB2 inhibitor Pimodivir, was performed by our group. We synthesized and identified compounds 16a and 16b, two novel thienopyrimidine derivatives displaying anti-influenza A activity in the single digit nanomolar range in cell culture. Binding of these unique compounds in the influenza polymerase PB2 pocket was also determined using molecular modeling.
    Copyright 2019 Elsevier Ltd. All rights reserved.


    KEYWORDS:

    Antiviral; Flu; Influenza A; Virus

    PMID: 31493987 DOI: 10.1016/j.bmcl.2019.126639
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