具有乙酰胆碱酯酶和单胺氧化酶抑制活性的新型他克林-司来吉兰杂合体用于治疗老年痴呆症。
A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease.
机构信息
Institute of Drug Synthesis and Pharmaceutical Processing, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
出版信息
Eur J Med Chem. 2013 Apr;62:745-53. doi: 10.1016/j.ejmech.2013.01.039. Epub 2013 Feb 8.
A novel series of tacrine-selegiline hybrids was synthesised and evaluated for application as inhibitors of cholinesterase (AChE/BuChE) and monoamine oxidase (MAO-A/B). The results demonstrate that most of the synthesised compounds exhibit high inhibitory activity. Among these compounds, compound 8g provided a good balance of activity towards all targets (with IC50 values of 22.6 nM, 9.37 nM, 0.3724 μM, and 0.1810 μM for AChE, BuChE, MAO-A and MAO-B, respectively). These results indicated that 8g has the potential to be a multi-functional candidate for Alzheimer's disease.
合成了一系列新型他克林-司来吉兰杂合体，并评估其作为乙酰胆碱酯酶（AChE/BuChE）和单胺氧化酶（MAO-A/B）抑制剂的应用。结果表明，大多数合成的化合物表现出高抑制活性。在这些化合物中，化合物 8g 对所有靶点均具有良好的活性平衡（对 AChE、BuChE、MAO-A 和 MAO-B 的 IC50 值分别为 22.6 nM、9.37 nM、0.3724 μM 和 0.1810 μM）。这些结果表明，8g 有可能成为治疗阿尔茨海默病的多功能候选药物。
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