341027-37-0Relevant academic research and scientific papers
Carboxylic acid isosteres improve the activity of ring-fused 2-pyridones that inhibit pilus biogenesis in E. coli
Aberg, Veronica,Das, Pralay,Chorell, Erik,Hedenstroem, Mattias,Pinkner, Jerome S.,Hultgren, Scott J.,Almqvist, Fredrik
supporting information; scheme or table, p. 3536 - 3540 (2009/04/05)
Ring-fused 2-pyridones, termed pilicides, are small synthetic compounds that inhibit pilus assembly in uropathogenic Escherichia coli. Their biological activity is clearly dependent upon a carboxylic acid functionality. Here, we present the synthesis and
Microwave-assisted decarboxylation of bicyclic 2-pyridone scaffolds and identification of Aβ-peptide aggregation inhibitors
Aberg, Veronica,Norman, Fredrik,Chorell, Erik,Westermark, Andreas,Olofsson, Anders,Elisabeth Sauer-Eriksson,Almqvist, Fredrik
, p. 2817 - 2823 (2007/10/03)
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°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 Aβ-peptide aggregation. Two out of the 21 2-pyridones described in this study inhibited amyloid formation of the Alzheimer Aβ(1-40) peptide. The effect was seen even at a 4: 1 ratio of 2-pyridone and monomeric Aβ-peptide. The Royal Society of Chemistry 2005.
