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Dihydropyrimidinone/1,2,3-triazole hybrid molecules: Synthesis and anti-varicella-zoster virus (VZV) evaluation

Hanane Kaoukabi 1 Youssef Kabri 2 Christophe Curti 2 Moha Taourirte 1 Juan C. Rodriguez-Ubis 3 Robert Snoeck 4 Graciela Andrei 4 Patrice Vanelle 2 Hassan B. Lazrek 5
1 Laboratory of Bioorganic and Macromolecular Chemistry
2 ICR - Institut de Chimie Radicalaire
3 Autonoma University
4 Rega Institute for Medical Research [Leuven, België]
5 URAC 16 - Laboratoire de Chimie Biomoléculaire Substances Naturelles et Réactivité
Abstract : By combining the structural features of dihydropyrimidinone and 1,2,3-triazole heterocycles, novel hybrid compounds were synthesized using a simple and convenient method. A series of novel mono and bis 1,2,3-triazole was synthesized via copper-catalyzed Huisgen azide-alkyne cycloadditions (CuAAC) under microwave irradiation. The newly synthesized compounds were evaluated for their antiviral activity against varicella-zoster virus (VZV). Compounds 6aa, lab, 6ba and 6da showed valuable antiviral activities, with EC50 values ranging from 3.6 to 11.3 mu M against TK+ and TK- VZV and without measurable cell-growth inhibition. (C) 2018 Elsevier Masson SAS. All rights reserved.
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https://hal-amu.archives-ouvertes.fr/hal-02091894
Contributor : Didier Gigmes <>
Submitted on : Saturday, April 6, 2019 - 5:17:21 PM
Last modification on : Tuesday, July 7, 2020 - 4:22:05 PM

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Hanane Kaoukabi, Youssef Kabri, Christophe Curti, Moha Taourirte, Juan C. Rodriguez-Ubis, et al.. Dihydropyrimidinone/1,2,3-triazole hybrid molecules: Synthesis and anti-varicella-zoster virus (VZV) evaluation. European Journal of Medicinal Chemistry, Elsevier, 2018, 155, pp.772--781. ⟨10.1016/j.ejmech.2018.06.028⟩. ⟨hal-02091894⟩

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