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


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.

SUBMITTER: Zhang H 

PROVIDER: S-EPMC7732027 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature

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

Zhang Hongwang H   Zhou Longhu L   Amichai Sarah S   Zandi Keivan K   Cox Bryan B   Schinazi Raymond R   Amblard Franck F  

Bioorganic & medicinal chemistry letters 20190824 20


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. ...[more]

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