Neuraminidase activity is essential for the infection and propagation of paramyxoviruses, including human parainfluenza viruses (hPIVs) and the Newcastle disease virus (NDV). Thus, many inhibitors have been developed based on the 2‐deoxy‐2,3‐didehydro‐d‐N‐acetylneuraminic acid inhibitor (DANA) backbone. Along this line, herein we report a series of neuraminidase inhibitors, having C4 (p‐toluenesulfonamido and azido substituents) and C5 (N‐perfluorinated chains) modifications to the DANA backbone, resulting in compounds with 5‐ to 15‐fold greater potency than the currently most active compound, the N‐trifluoroacetyl derivative of DANA (FANA), toward the NDV hemagglutinin‐neuraminidase (NDV‐HN). Remarkably, these inhibitors were found to be essentially inactive against the human sialidase NEU3, which is present on the outer layer of the cell membrane and is highly affected by the current NDV inhibitor FANA.

中文翻译：

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对新城疫病毒血凝素神经氨酸酶的有效抑制剂

神经氨酸酶活性对于副粘病毒（包括人副流感病毒（hPIV）和新城疫病毒（NDV））的感染和繁殖至关重要。因此，基于2-脱氧-2,3-二氢化二氢-d - N-乙酰神经氨酸抑制剂（DANA）骨架开发了许多抑制剂。沿此思路，我们在此报告了一系列神经氨酸酶抑制剂，它们对DANA主链进行了C4（对甲苯磺酰胺基和叠氮基取代基）和C5（N-全氟链）修饰，产生的化合物的效力比其高5至15倍目前活性最高的化合物NDANA的三氟乙酰基衍生物（FANA），用于NDV血凝素神经氨酸酶（NDV-HN）。值得注意的是，发现这些抑制剂对人唾液酸酶NEU3基本上是无活性的，人唾液酸酶NEU3存在于细胞膜的外层，并且受到当前NDV抑制剂FANA的高度影响。