Identification of novel small-molecule inhibitors of Zika virus infection

[Display omitted] The recent re-emergence of Zika virus (ZIKV), a member of the Flaviviridae family, has become a global emergency and a serious public health threat worldwide. ZIKV infection causes severe neuroimmunopathology and is particularly harmful to the developing fetuses of infected pregnan...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2018-02, Vol.28 (3), p.452-458
Main Authors: Micewicz, Ewa D., Khachatoorian, Ronik, French, Samuel W., Ruchala, Piotr
Format: Article
Language:English
Subjects:
Antivirals
Plaque assay
Screening
Zika inhibitors
Zika virus
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Summary:[Display omitted] The recent re-emergence of Zika virus (ZIKV), a member of the Flaviviridae family, has become a global emergency and a serious public health threat worldwide. ZIKV infection causes severe neuroimmunopathology and is particularly harmful to the developing fetuses of infected pregnant women causing various developmental abnormalities. Currently, there are no effective methods of preventing or treating ZIKV infection, and new treatment options are urgently needed. Therefore, we have used an in vitro plaque assay to screen a limited proprietary library of small organic compounds and identified highly bioactive leads, with the most active analogs showing activity in low picomolar range. Identified “hits” possess certain common structural features that can be used in the design of the next generation(s) of ZIKV inhibitors. Collectively, our findings suggest that identified compounds represent excellent template(s) for the development of inexpensive and orally available anti-Zika drugs.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2017.12.019