کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1394034 | 1501124 | 2015 | 8 صفحه PDF | دانلود رایگان |
• Acridone linked to 1,2,3-triazole derivatives have been synthesized.
• All compounds were evaluated for AChE and BChE inhibitory activities.
• Compound 9g depicted the most potent anti-AChE activity (IC50 = 7.31 μM).
A novel series of acridone linked to 1,2,3-triazole derivatives have been synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. The synthetic approach was started from the reaction of 2-bromobenzoic acid with aniline derivatives and subsequent cyclization reaction to give acridone derivatives. Then, reaction of the later compounds with propargyl bromide followed by azide–alkyne cycloaddition reaction (click reaction) led to the formation of the title compounds in good yields. Among the synthesized compounds, 10-((1-(4-chlorobenzyl)-1H-1,2,3-triazol-4-yl)methyl)-2-methoxyacridin-9(10H)-one 9g, depicted the most potent anti-AChE activity (IC50 = 7.31 μM). Also, docking study confirmed the results obtained through in vitro experiments and predicted possible binding conformation.
A novel series of acridone linked to 1,2,3-triazole derivatives have been synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 92, 6 March 2015, Pages 799–806