M. C. R. Silva, A. F. Vilela, C. Cardoso, R. Pilli
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引用次数: 1
Abstract
In this work, twelve analogues of piperidine alkaloids (-)-cassine and (-)-spectaline were synthesized, as well as the racemic forms of these natural products. The compounds were evaluated for their inhibition of electric eel acetylcholinesterase (AChEee) and human butyrylcholinesterase (BChEhu) by on-flow mass-spectrometry-based dual-enzyme assay, and the inhibition mechanisms for the most potent analogues were also determined. Our results showed a preference for BChEhu inhibition with compounds 10c (Ki = 5.24 μM), 12b (Ki = 17.4 μM), 13a (Ki = 13.2 μM) and 3 (Ki = 11.3 μM) displaying the best inhibitory activities.
本文合成了十二种胡椒碱类生物碱(-)-卡西因和(-)-谱碱的类似物，以及这些天然产物的外消旋形式。采用流动质谱双酶法测定了化合物对电鳗乙酰胆碱酯酶(AChEee)和人丁基胆碱酯酶(BChEhu)的抑制作用，并确定了最有效的类似物的抑制机制。结果表明，化合物10c (Ki = 5.24 μM)、12b (Ki = 17.4 μM)、13a (Ki = 13.2 μM)和3 (Ki = 11.3 μM)对BChEhu具有较强的抑制作用。
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