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以吖啶和苄胺为关键片段,通过不同长度的碳链连接,合成了9个乙酰胆碱酯酶(AChE)抑制剂,并经核磁共振和高分辨质谱分析确证结构。测试了目标化合物对AChE的体外抑制活性。结果显示,目标化合物对AChE的抑制活性随着连接链长度的增加而提高;六碳链化合物的活性最佳(IC_(50)=17.19 nmol/L)。本研究还通过计算机模拟对接分析,对活性测试结果进行了解析。
Using acridine and benzylamine as the key fragments, nine acetylcholinesterase (AChE) inhibitors were synthesized by carbon chain of different lengths and confirmed by 1H NMR and MS-MS. The target compounds were tested for in vitro inhibitory activity against AChE. The results showed that the inhibitory activity of the target compound on AChE increased with the length of the linked chain; the activity of the six-carbon chain compound was the best (IC 50 = 17.19 nmol / L). In this study, the results of the activity test were also analyzed by computer simulation docking analysis.