Potent Acetylcholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Docking Study of Acridone Linked to 1,2,3-Triazole Derivatives

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Potent Acetylcholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Docking Study of Acridone Linked to 1,2,3-Triazole Derivatives Publisher Pubmed

Mohammadikhanaposhtani M¹ ; Saeedi M² ; Zafarghandi NS¹ ; Mahdavi M³ ; Sabourian R⁴ ; Razkenari EK⁴ ; Alinezhad H⁵ ; Khanavi M⁶ ; Foroumadi A³ ; Shafiee A³ ; Akbarzadeh T^{1, 4}

Source: European Journal of Medicinal Chemistry Published:2015

Abstract

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 Combining double low line 7.31 μ1/4M). Also, docking study confirmed the results obtained through in vitro experiments and predicted possible binding conformation. © 2015 Elsevier Masson SAS.

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Style	Citing Format
MLA	Mohammadikhanaposhtani M, et al.. "Potent Acetylcholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Docking Study of Acridone Linked to 1,2,3-Triazole Derivatives." European Journal of Medicinal Chemistry, vol. 92, no. , 2015, pp. 799-806.
APA	Mohammadikhanaposhtani M, Saeedi M, Zafarghandi NS, Mahdavi M, Sabourian R, Razkenari EK, Alinezhad H, Khanavi M, Foroumadi A, Shafiee A, Akbarzadeh T (2015). Potent Acetylcholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Docking Study of Acridone Linked to 1,2,3-Triazole Derivatives. European Journal of Medicinal Chemistry, 92(), 799-806.
Chicago	Mohammadikhanaposhtani M, Saeedi M, Zafarghandi NS, Mahdavi M, Sabourian R, Razkenari EK, Alinezhad H, et al.. "Potent Acetylcholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Docking Study of Acridone Linked to 1,2,3-Triazole Derivatives." European Journal of Medicinal Chemistry 92, no. (2015): 799-806.
Harvard	Mohammadikhanaposhtani M et al. (2015) 'Potent Acetylcholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Docking Study of Acridone Linked to 1,2,3-Triazole Derivatives', European Journal of Medicinal Chemistry, 92(), pp. 799-806.
Vancouver	Mohammadikhanaposhtani M, Saeedi M, Zafarghandi NS, Mahdavi M, Sabourian R, Razkenari EK, et al.. Potent Acetylcholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Docking Study of Acridone Linked to 1,2,3-Triazole Derivatives. European Journal of Medicinal Chemistry. 2015;92():799-806.
BibTex	@article{ author = {Mohammadikhanaposhtani M and Saeedi M and Zafarghandi NS and Mahdavi M and Sabourian R and Razkenari EK and Alinezhad H and Khanavi M and Foroumadi A and Shafiee A and Akbarzadeh T}, title = {Potent Acetylcholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Docking Study of Acridone Linked to 1,2,3-Triazole Derivatives}, journal = {European Journal of Medicinal Chemistry}, volume = {92}, number = {}, pages = {799-806}, year = {2015} }
RIS	TY - JOUR AU - Mohammadikhanaposhtani M AU - Saeedi M AU - Zafarghandi NS AU - Mahdavi M AU - Sabourian R AU - Razkenari EK AU - Alinezhad H AU - Khanavi M AU - Foroumadi A AU - Shafiee A AU - Akbarzadeh T TI - Potent Acetylcholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Docking Study of Acridone Linked to 1,2,3-Triazole Derivatives JO - European Journal of Medicinal Chemistry VL - 92 IS - SP - 799 EP - 806 PY - 2015 ER -

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