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

作者：Kaoukabi Hanane; Kabri Youssef; Curti Christophe; Taourirte Moha; Rodriguez Ubis Juan C; Snoeck Robert; Andrei Graciela; Vanelle Patrice^*; Lazrek Hassan B^*

来源：European Journal of Medicinal Chemistry, 2018, 155: 772-781.

DOI：10.1016/j.ejmech.2018.06.028

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

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.

• 出版日期2018-7-15