Microwave-assisted decarboxylation of bicyclic 2-pyridone scaffolds and identification of Aβ-peptide aggregation inhibitors
Microwave-assisted decarboxylation of bicyclic 2-pyridone scaffolds and identification of Aβ-peptide aggregation inhibitors
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DOI：
10.1039/b503294f
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发表时间：
2005-01-01
影响因子：
3.2
通讯作者：
Almqvist, F
中科院分区：
文献类型：
--
作者：
Åberg, V;Norman, F;Almqvist, F
研究了一种无试剂微波辅助下羧酸官能化双环2-吡啶酮的脱羧反应。这种新方法基于在N-甲基吡咯烷酮（NMP）中在220摄氏度下微波加热600秒，被证明是实用且非常有效的，以接近定量的产率产生脱羧的2-吡啶酮。筛选羧酸甲酯和羧酸形式的脱羧产物和中间体2-吡啶酮对A β-肽聚集的影响。在这项研究中描述的21种2-吡啶酮中有两种抑制阿尔茨海默A β（1-40）肽的淀粉样蛋白形成。甚至在2-吡啶酮和单体A β-肽的比例为4：1时也观察到该效果。
A reagent-free microwave-assisted decarboxylation procedure for carboxylic acid functionalized bicyclic 2-pyridones has been developed. This new method, based on microwave heating at 220 degrees C for 600 seconds in N-methyl pyrrolidone (NMP), proved to be practical and very efficient, resulting in decarboxylated 2-pyridones in near-quantitative yields. The decarboxylated products and the intermediate 2-pyridones in the form of carboxylic acid methyl esters and carboxylic acids were screened for their effect on A beta-peptide aggregation. Two out of the 21 2-pyridones described in this study inhibited amyloid formation of the Alzheimer A beta(1-40) peptide. The effect was seen even at a 4 : 1 ratio of 2-pyridone and monomeric A beta-peptide.