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

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

  • Eur J Med Chem. 2018 Jul 15:155:772-781. doi: 10.1016/j.ejmech.2018.06.028.
Hanane Kaoukabi 1,  Youssef Kabri 2,  Christophe Curti 2,  Moha Taourirte 3,  Juan C Rodriguez-Ubis 4,  Robert Snoeck 5,  Graciela Andrei 5,  Patrice Vanelle 6,  Hassan B Lazrek 7
Affiliations

Affiliations

  • 1 Laboratory of Bioorganic and Macromolecular Chemistry, Department of Chemistry, Faculty of Sciences and Technology, Gueliz (FSTG), Marrakesh, Morocco; Laboratory of Biomolecular and Medicinal Chemistry, Department of Chemistry, Faculty of Sciences Semlalia (FSSM), Marrakesh, Morocco.
  • 2 Aix Marseille University, Institut de Chimie Radicalaire ICR, UMR CNRS 7273, Laboratoire de Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, 27 Boulevard Jean Moulin-CS 30064, 13385, Marseille CEDEX 05, France.
  • 3 Laboratory of Bioorganic and Macromolecular Chemistry, Department of Chemistry, Faculty of Sciences and Technology, Gueliz (FSTG), Marrakesh, Morocco.
  • 4 Laboratory Organic-Inorganic Solids and Luminiscent Probes (M01-L207), Department of Organic Chemistry, Faculty of Sciences, University Autonoma, Madrid, Spain.
  • 5 Rega Institute for Medical Research, KU Leuven, Leuven, Belgium.
  • 6 Aix Marseille University, Institut de Chimie Radicalaire ICR, UMR CNRS 7273, Laboratoire de Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, 27 Boulevard Jean Moulin-CS 30064, 13385, Marseille CEDEX 05, France. Electronic address: patrice.vanelle@univ-amu.fr.
  • 7 Laboratory of Biomolecular and Medicinal Chemistry, Department of Chemistry, Faculty of Sciences Semlalia (FSSM), Marrakesh, Morocco. Electronic address: hblazrek@uca.ac.ma.
PMID: 29945100 DOI: 10.1016/j.ejmech.2018.06.028
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, 7ab, 6ba and 6da showed valuable Antiviral activities, with EC50 values ranging from 3.6 to 11.3 μM against TK+ and TK- VZV and without measurable cell-growth inhibition.

Keywords

1,2,3-Triazole; 1,3-Dipolar cycloaddition; Anti-VZV; Biginelli reaction; Hybrid molecules; Microwave.

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