Benzofuran-Derived Benzylpyridinium Bromides As Potent Acetylcholinesterase Inhibitors

Benzofuran-Derived Benzylpyridinium Bromides As Potent Acetylcholinesterase Inhibitors Publisher Pubmed

Baharloo F¹ ; Moslemin MH¹ ; Nadri H² ; Asadipour A³ ; Mahdavi M⁴ ; Emami S⁵ ; Firoozpour L⁶ ; Mohebat R¹ ; Shafiee A⁴ ; Foroumadi A^{3, 4}

Show Affiliations

1. Department of Chemistry, Faculty of Chemistry, Islamic Azad University, Yazd, Iran
2. Department of Medicinal Chemistry, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran
3. Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medicinal Sciences, Kerman, Iran
4. Department of Medicinal Chemistry, Pharmaceutical Sciences Research Center, Tehran University of Medicinal Sciences, Tehran, Iran
5. Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
6. Drug Design and Development Research Center, Tehran University of Medicinal Sciences, Tehran, Iran

Source: European Journal of Medicinal Chemistry Published:2015

Abstract

A series of benzofuran-based N-benzylpyridinium derivatives 5a-o were designed and synthesized as novel AChE inhibitors. The synthetic pathway of the compounds involved the preparation of 4-(benzofuran-2-yl)pyridine intermediates via the reaction of different salicylaldehyde derivatives and 4-(bromomethyl)pyridine, followed by intramolecular cyclization. Subsequently, the 4-(benzofuran-2-yl)pyridines were N-benzylated by using appropriate benzyl bromide to afford the final product 5a-o. The results of in vitro AChE activity evaluation of synthesized compounds revealed that all compound had potent anti-AChE activity comparable or more potent than standard drug donepezil. The N-(3,5-dimethylbenzyl) derivative 5e with IC50 value of 4.1 nM was the most active compound, being 7-fold more potent than donepezil. © 2015 Elsevier Masson SAS.

Style	Citing Format
MLA	Baharloo F, et al.. "Benzofuran-Derived Benzylpyridinium Bromides As Potent Acetylcholinesterase Inhibitors." European Journal of Medicinal Chemistry, vol. 93, no. , 2015, pp. 196-201.
APA	Baharloo F, Moslemin MH, Nadri H, Asadipour A, Mahdavi M, Emami S, Firoozpour L, Mohebat R, Shafiee A, Foroumadi A (2015). Benzofuran-Derived Benzylpyridinium Bromides As Potent Acetylcholinesterase Inhibitors. European Journal of Medicinal Chemistry, 93(), 196-201.
Chicago	Baharloo F, Moslemin MH, Nadri H, Asadipour A, Mahdavi M, Emami S, Firoozpour L, Mohebat R, Shafiee A, Foroumadi A. "Benzofuran-Derived Benzylpyridinium Bromides As Potent Acetylcholinesterase Inhibitors." European Journal of Medicinal Chemistry 93, no. (2015): 196-201.
Harvard	Baharloo F et al. (2015) 'Benzofuran-Derived Benzylpyridinium Bromides As Potent Acetylcholinesterase Inhibitors', European Journal of Medicinal Chemistry, 93(), pp. 196-201.
Vancouver	Baharloo F, Moslemin MH, Nadri H, Asadipour A, Mahdavi M, Emami S, et al.. Benzofuran-Derived Benzylpyridinium Bromides As Potent Acetylcholinesterase Inhibitors. European Journal of Medicinal Chemistry. 2015;93():196-201.
BibTex	@article{ author = {Baharloo F and Moslemin MH and Nadri H and Asadipour A and Mahdavi M and Emami S and Firoozpour L and Mohebat R and Shafiee A and Foroumadi A}, title = {Benzofuran-Derived Benzylpyridinium Bromides As Potent Acetylcholinesterase Inhibitors}, journal = {European Journal of Medicinal Chemistry}, volume = {93}, number = {}, pages = {196-201}, year = {2015} }
RIS	TY - JOUR AU - Baharloo F AU - Moslemin MH AU - Nadri H AU - Asadipour A AU - Mahdavi M AU - Emami S AU - Firoozpour L AU - Mohebat R AU - Shafiee A AU - Foroumadi A TI - Benzofuran-Derived Benzylpyridinium Bromides As Potent Acetylcholinesterase Inhibitors JO - European Journal of Medicinal Chemistry VL - 93 IS - SP - 196 EP - 201 PY - 2015 ER -

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