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Novel 2-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole and 3-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole derivatives as dengue virus inhibitors targeting NS5 polymerase

Abstract : Using a functional high-throughput screening (HTS) and subsequent SAR studies, we have discovered a novel series of non-nucleoside dengue viral polymerase inhibitors. We report the elaboration of SAR around hit compound 1 as well as the synthesis and antiviral evaluation of 3-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole and 5-phenyl-2-[2-(2-thienyl)ethenyl]-1,3,4-oxadiazole analogues derived from a rapid and easily accessible chemical pathway. A large number of compounds prepared by this method were shown to possess in vitro activity against the polymerase of dengue virus. The most potent inhibitors were tested against Dengue virus clinical isolates on infected cells model and exhibit submicromolar activity on the four dengue virus serotypes.
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https://hal-amu.archives-ouvertes.fr/hal-02061730
Contributor : Karine Barral <>
Submitted on : Friday, March 8, 2019 - 12:14:14 PM
Last modification on : Tuesday, August 25, 2020 - 1:22:01 PM

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Fatiha Benmansour, Cecilia Eydoux, Gilles Querat, Xavier de Lamballerie, Bruno Canard, et al.. Novel 2-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole and 3-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole derivatives as dengue virus inhibitors targeting NS5 polymerase. European Journal of Medicinal Chemistry, Elsevier, 2016, 109, pp.146-156. ⟨10.1016/j.ejmech.2015.12.046⟩. ⟨hal-02061730⟩

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