In this study, forty-four chiral triazole derivatives have been prepared via asymmetric synthesis, and which has been successfully characterized by typical spectroscopic techniques including ¹H NMR, ¹³C NMR, EI-MS, elemental analysis and optical rotations. Their in vitro antiviral activities against EV71 and CVB3 were fully investigated in cell-based assays. It was observed that 13 synthetic triazole derivatives inhibited the CPE of EV71 on RD cells, with EC_50S in the 5.3–15.9 μg/ml range and corresponding SIs of 4.0–27.6, while 17 triazole derivatives showed antiviral activities against CVB3, with EC_50S in the 4.7–15.1 μg/ml range and the corresponding SIs of 3.7–14.5. In addition, in some cases, the respective enantiomers showed significantly selective inhibitory effect against EV71, most notably for the enantiomers 9(R) and 10(S), 42(R) and 43(S), which presented an obvious activity difference. The most potential molecules are the compounds 10 and 43 with S-configuration, and which exhibit good SI values compared with the control Ribavirin.

在这项研究中，通过不对称合成制备了四十四种手性三唑衍生物，并已通过典型的光谱技术成功表征，包括¹ H NMR，¹³ C NMR，EI-MS，元素分析和旋光性。在基于细胞的测定中，已充分研究了它们对EV71和CVB3的体外抗病毒活性。据观察，有13种合成的三唑衍生物抑制RD71 EV71的CPE，EC _50S在5.3-15.9μg/ ml范围内，相应的SI值为4.0-27.6，而17种三唑衍生物对CVB3表现出抗病毒活性，EC _50S在4.7–15.1μg/ ml范围内，相应的SI在3.7–14.5之间。此外，在某些情况下，各个对映体对EV71表现出明显的选择性抑制作用，最显着的是对映体9（R）和10（S），42（R）和43（S），表现出明显的活性差异。最有潜力的分子是具有S-构型的化合物10和43，与对照利巴韦林相比，它们具有良好的SI值。