A series of analogues of potent antiviral perylene nucleoside dUY11 with methylthiomethyl (MTM), azidomethyl (AZM) and HO-C_1–4-alkyl-1,2,3-triazol-1,4-diyl groups at 3′-O-position as well as the two products of copper-free alkyne-azide cycloaddition of the AZM derivative were prepared and evaluated against tick-borne encephalitis virus (TBEV). Four compounds (4, 6, 8a, 8b) showed EC₅₀ ≤ 10 nM, thus appearing the most potent TBEV inhibitors to date. Moreover, these nucleosides have higher lipophilicity (clogP) and increased solubility in aq. DMSO vs. parent compound dUY11.

中文翻译：

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3'- ø -取代5-（perylen -3-基乙炔基）-2'- deoxyuridines如蜱传脑炎病毒的繁殖抑制剂

一系列有效的抗病毒的核苷苝的类似物dUY11与甲硫基甲基（MTM），叠氮基甲基（AZM）和HO-C _1-4在3'-烷基-1,2,3-三唑-1,4-二基ø -制备了AZM衍生物的位置以及两种无铜炔-叠氮化物环加成的产物，并针对tick传播性脑炎病毒（TBEV）进行了评估。四种化合物（4，6，图8A，图8B）显示EC ₅₀  ≤10nm时，由此出现的最有效的抑制剂TBEV迄今。此外，这些核苷具有更高的亲脂性（clogP），并在水溶液中具有更高的溶解度。DMSO与母体化合物dUY11。