Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Istanbul University, Istanbul, Turkey.
Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Istanbul University, Istanbul, Turkey.
Bioorg Chem. 2021 Jul;112:104958. doi: 10.1016/j.bioorg.2021.104958. Epub 2021 Apr 30.
A new series of N-(3-oxo-1-thia-4-azaspiro[4.5]decan-4-yl)carboxamides have been designed, synthesized and evaluated as antiviral agents. The compounds were prepared by condensation of 2-methylfuran-3-carbohydrazide, appropriate carbonyl compounds and sulfanyl acids. The new molecules were characterized by IR, H NMR, C NMR, mass spectrometry and elemental analysis. Six analogues proved to be active against influenza A/H3N2 virus, the two most protent analogues, 3c and 3d, having an EC value of about 1 µM. These findings help to define the SAR of spirothiazolidinone-based inhibitors of the influenza virus membrane fusion process.
设计、合成并评估了一系列新的 N-(3-氧代-1-硫杂-4-氮杂螺[4.5]癸烷-4-基)甲酰胺类化合物作为抗病毒药物。这些化合物是通过 2-甲基呋喃-3-甲酰肼、合适的羰基化合物和硫代酸缩合制备的。新分子通过 IR、H NMR、C NMR、质谱和元素分析进行了表征。6 种类似物被证明对甲型流感病毒 H3N2 具有活性，其中两个最有效的类似物 3c 和 3d 的 EC 值约为 1 µM。这些发现有助于确定基于螺噻唑烷酮的流感病毒膜融合抑制剂的 SAR。
