Synthesis and Anticholinesterase Activity of Coumarin-3-Carboxamides Bearing Tryptamine Moiety

Synthesis and Anticholinesterase Activity of Coumarin-3-Carboxamides Bearing Tryptamine Moiety Publisher Pubmed

Ghaneinasab S¹ ; Khoobi M^{2, 3} ; Hadizadeh F⁴ ; Marjani A¹ ; Moradi A⁵ ; Nadri H⁵ ; Emami S⁶ ; Foroumadi A³ ; Shafiee A³

Show Affiliations

1. Department of Chemistry, Arak Branch, Islamic Azad University, Arak, Iran
2. Department of Pharmaceutical Biomaterials and Medical Biomaterials Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
3. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medicinal Sciences, Tehran, Iran
4. Biotechnology Research Center, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
5. Department of Medicinal Chemistry, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran
6. Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran

Source: European Journal of Medicinal Chemistry Published:2016

Abstract

A number of N-(2-(1H-indol-3-yl)ethyl)-2-oxo-2H-chromene-3-carboxamides were synthesized and tested against AChE and BuChE. The in vitro assessment of the synthesized compounds 4a-o revealed that most of them had significant activity toward AChE. The SAR study demonstrated that the introduction of benzyloxy moiety on the 7-position of coumarin scaffold can improve the anti-AChE activity. The best result was obtained with 7-(4-fluorobenzyl)oxy moiety in the case of compound 4o, displaying IC50value of 0.16 μM. Based on the docking study of AChE, the prototype compound 4o was laid across the active site and occupied both peripheral anionic site (PAS) and catalytic anionic site (CAS). © 2016 Elsevier Masson SAS

Style	Citing Format
MLA	Ghaneinasab S, et al.. "Synthesis and Anticholinesterase Activity of Coumarin-3-Carboxamides Bearing Tryptamine Moiety." European Journal of Medicinal Chemistry, vol. 121, no. , 2016, pp. 40-46.
APA	Ghaneinasab S, Khoobi M, Hadizadeh F, Marjani A, Moradi A, Nadri H, Emami S, Foroumadi A, Shafiee A (2016). Synthesis and Anticholinesterase Activity of Coumarin-3-Carboxamides Bearing Tryptamine Moiety. European Journal of Medicinal Chemistry, 121(), 40-46.
Chicago	Ghaneinasab S, Khoobi M, Hadizadeh F, Marjani A, Moradi A, Nadri H, Emami S, Foroumadi A, Shafiee A. "Synthesis and Anticholinesterase Activity of Coumarin-3-Carboxamides Bearing Tryptamine Moiety." European Journal of Medicinal Chemistry 121, no. (2016): 40-46.
Harvard	Ghaneinasab S et al. (2016) 'Synthesis and Anticholinesterase Activity of Coumarin-3-Carboxamides Bearing Tryptamine Moiety', European Journal of Medicinal Chemistry, 121(), pp. 40-46.
Vancouver	Ghaneinasab S, Khoobi M, Hadizadeh F, Marjani A, Moradi A, Nadri H, et al.. Synthesis and Anticholinesterase Activity of Coumarin-3-Carboxamides Bearing Tryptamine Moiety. European Journal of Medicinal Chemistry. 2016;121():40-46.
BibTex	@article{ author = {Ghaneinasab S and Khoobi M and Hadizadeh F and Marjani A and Moradi A and Nadri H and Emami S and Foroumadi A and Shafiee A}, title = {Synthesis and Anticholinesterase Activity of Coumarin-3-Carboxamides Bearing Tryptamine Moiety}, journal = {European Journal of Medicinal Chemistry}, volume = {121}, number = {}, pages = {40-46}, year = {2016} }
RIS	TY - JOUR AU - Ghaneinasab S AU - Khoobi M AU - Hadizadeh F AU - Marjani A AU - Moradi A AU - Nadri H AU - Emami S AU - Foroumadi A AU - Shafiee A TI - Synthesis and Anticholinesterase Activity of Coumarin-3-Carboxamides Bearing Tryptamine Moiety JO - European Journal of Medicinal Chemistry VL - 121 IS - SP - 40 EP - 46 PY - 2016 ER -

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