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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Design, synthesis and biological evaluation of benzylisoquinoline derivatives as multifunctional agents against Alzheimer's disease
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Design, synthesis and biological evaluation of benzylisoquinoline derivatives as multifunctional agents against Alzheimer's disease

机译：苄基喹啉喹啉衍生物作为对阿尔茨海默病的多官能药物的设计，合成和生物学评价

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摘要

A novel series of benzylisoquinoline derivatives were designed, synthesized, and evaluated as multifunctional agents against Alzheimer's disease (AD). The screening results showed that most of the compounds significantly inhibited cholinesterases (ChEs), human cholinesterases (h-ChEs) and self-induced β-amyloid (Aβ) aggregation. In particular, compound 9k showed the strongest acetylcholinesterase (AChE) inhibitory activity, being 1000-fold and 3-fold more potent than its precursor benzylisoquinoline (10) and the positive control galanthamine, respectively. In addition, 9k was a moderately potent inhibitor for h-ChEs. Compared with precursor benzylisoquinoline (36.0% at 20 μM), 9k (78.4% at 20 μM) could further inhibit Aβ aggregation. Moreover, 9k showed low cell toxicity in human SH-SY5Y neuroblastoma cells. Therefore, compound 9k might be a promising lead compound for AD treatment.
机译：设计，合成并评估为针对阿尔茨海默病（AD）的多官能剂的新型苄基异喹啉衍生物。 筛选结果表明，大多数化合物显着抑制胆碱酯酶（CHE），人胆碱酯酶（H-CHES）和自诱导的β-淀粉样（Aβ）聚集。 特别地，化合物9K显示出最强的乙酰胆碱酯酶（ACHE）抑制活性，比其前体苄基异喹啉（10）和阳性对照Golanthamine分别为1000倍和3倍。 此外，9K是H-Ches的适度有效抑制剂。 与前体苄基异喹啉（36.0％在20μm）相比，9k（20μm处为78.4％）可以进一步抑制Aβ聚集。 此外，9K在人SH-SY5Y神经母细胞瘤细胞中显示出低细胞毒性。 因此，化合物9K可能是用于AD处理的有前途的铅化合物。

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