Influenza A viruses have caused worldwide epidemics and pandemics by reassortment and generation of drug-resistant mutants, which leads to an urgent need to develop novel antivirals. In this study, a series of sulfonyl piperazine nucleozin derivatives were designed and synthesized, and their in vitro anti-influenza activity was evaluated. Many of these compounds exhibited moderate to good anti-influenza activity against influenza A. Among these, 6d, 6g, 6h, 6i, and 6j exhibited better activity than ribavirin. 2,3-dichlorobenzene substituted analogue 6i displayed the most remarkable in vitro activity against Influenza A. All the derivatives show no obvious cellular growth inhibition against MDCK cells. This study reported a new series of nucleoprotein inhibitors with a good selectivity window and potential for further development as novel anti-influenza agents.

中文翻译：

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核苷磺酰哌嗪衍生物抗甲型流感病毒抑制剂的设计、合成及生物学评价

甲型流感病毒通过重组和耐药突变体的产生引起了世界范围内的流行和大流行，这导致迫切需要开发新型抗病毒药物。本研究设计合成了一系列磺酰基哌嗪核苷衍生物，并对其体外抗流感活性进行了评价。许多这些化合物对甲型流感病毒表现出中等至良好的抗流感活性。其中，6d、6g、6h、6i 和 6j 表现出比利巴韦林更好的活性。2,3-二氯苯取代的类似物6i显示出最显着的体外抗甲型流感活性。所有衍生物对MDCK细胞均无明显的细胞生长抑制作用。