State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang, China.
Molecules. 2010 Jul 29;15(8):5112-23. doi: 10.3390/molecules15085112.
A series of novel chiral thioureas 3a-n bearing leucine and phosphonate moieties were synthesized in excellent yields. The structures of the compounds were completely characterized by elemental analysis, IR, 1H-, 13C-, 31P- and 19F-NMR spectral data. A half-leaf method was used to determine the in vivo protective and curative efficacies of the title products against tobacco mosaic virus (TMV). The compounds 3l and 3n displayed good in vivo protection and curative effects against TMV with inhibitory rates of 60.1, 62.8% (protection) and 56.7, 53.6% (curative) at 0.5 mg/mL, respectively. To the best of our knowledge, this is the first report on the antiviral activity of chiral thioureas containing leucine and phosphonate moieties.
一系列新型手性硫脲 3a-n 含有亮氨酸和膦酸酯部分，以优异的产率合成。通过元素分析、IR、1H-、13C-、31P-和 19F-NMR 光谱数据完全表征了化合物的结构。采用半叶法测定了标题产物对烟草花叶病毒（TMV）的体内保护和治疗功效。化合物 3l 和 3n 在 0.5mg/mL 时对 TMV 表现出良好的体内保护和治疗效果，抑制率分别为 60.1%、62.8%（保护）和 56.7%、53.6%（治疗）。据我们所知，这是首例关于含有亮氨酸和膦酸酯部分的手性硫脲的抗病毒活性的报道。
