二氢嘧啶酮/1,2,3-三唑杂合分子的合成及抗水痘带状疱疹病毒（VZV）活性评价。
Dihydropyrimidinone/1,2,3-triazole hybrid molecules: Synthesis and anti-varicella-zoster virus (VZV) evaluation.
机构信息
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.
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.
出版信息
Eur J Med Chem. 2018 Jul 15;155:772-781. doi: 10.1016/j.ejmech.2018.06.028. Epub 2018 Jun 13.
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 EC values ranging from 3.6 to 11.3 μM against TK+ and TK- VZV and without measurable cell-growth inhibition.
通过结合二氢嘧啶酮和 1,2,3-三唑杂环的结构特征，使用简单方便的方法合成了新型杂合化合物。通过微波辐射下铜催化的叠氮-炔环加成反应（CuAAC）合成了一系列新型单和双 1,2,3-三唑。新合成的化合物被评估了其对水痘带状疱疹病毒（VZV）的抗病毒活性。化合物 6aa、7ab、6ba 和 6da 表现出有价值的抗病毒活性，对 TK+和 TK- VZV 的 EC 值范围为 3.6 至 11.3 μM，且没有可测量的细胞生长抑制作用。
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