4.7 Article

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

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 155, Issue -, Pages 772-781

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.06.028

Keywords

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

Funding

  1. ERASMUS program (University Autonoma, laboratory Organic-Inorganic Solids and Luminiscent Probes, Madrid, Spain) [M01-L207]

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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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