Objective: The syntheses and biological activities of 8-thiosubstituted-1,3,7- trimethylxanthine derivatives bearing an aromatic hydrazide-hydrazone fragment in the side chain at C8 are described.

Methods: The chemical structures of the synthesized compounds 6a-m were confirmed based on their MS, FTIR, 1H NMR and 13C NMR analyses.

Results: The in vitro investigations of neuroprotective effects manifested on cellular (human neuroblastoma cell line SH-SY5Y) and sub-cellular (isolated rat brain synaptosomes) levels show that compounds 6g and 6i demonstrate statistically significant activity. The performed monoamine oxidase B (MAO-B) inhibition study in vitro show that compounds 6g and 6i possess a significant MAO-B inhibition activity close to L-deprenyl.

Conclusion: These results suggest that such compounds may be utilized for the development of new candidate MAO-B inhibitors for the treatment of Parkinson’s disease.

目的：描述了在C8侧链带有芳香酰肼-hydr片段的8-硫取代的1,3,7-三甲基黄嘌呤衍生物的合成和生物活性。

方法：根据合成化合物6a-m的MS，FTIR，1H NMR和13C NMR分析，确定其化学结构。

结果：对细胞（人成神经细胞瘤细胞系SH-SY5Y）和亚细胞（分离的大鼠脑突触体）水平表现出的神经保护作用的体外研究表明，化合物6g和6i具有统计学上的显着活性。体外进行的单胺氧化酶B（MAO-B）抑制研究表明，化合物6g和6i具有接近L-去异戊二烯基的重要MAO-B抑制活性。

结论：这些结果表明，此类化合物可用于开发新的候选MAO-B抑制剂，以治疗帕金森氏病。