Design, Synthesis and Anti-Alzheimer's Activity of Novel 1,2,3-Triazole-Chromenone Carboxamide Derivatives

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Design, Synthesis and Anti-Alzheimer's Activity of Novel 1,2,3-Triazole-Chromenone Carboxamide Derivatives Publisher Pubmed

Rastegari A¹ ; Nadri H² ; Mahdavi M³ ; Moradi A² ; Mirfazli SS⁴ ; Edraki N⁵ ; Moghadam FH⁶ ; Larijani B³ ; Akbarzadeh T^{1, 7} ; Saeedi M^{7, 8}

Source: Bioorganic Chemistry Published:2019

Abstract

Alzheimer's disease (AD) is a well-known neurodegenerative disorder affecting millions of old people worldwide and the corresponding epidemiological data highlights the significance of the disease. As AD is a multifactorial illness, various single-target directed drugs that have reached clinical trials have failed. Therefore, various factors associated with outset of AD have been considered in targeted drug discovery and development. In this work, a wide range of 1,2,3-triazole-chromenone carboxamides were designed, synthesized, and evaluated for their cholinesterase inhibitory activity. Among them, N-(1-benzylpiperidin-4-yl)-7-((1-(3,4-dimethylbenzyl)-1H-1,2,3-triazol-4-yl)methoxy)-2-oxo-2H-chromene-3-carboxamide (11b) showed the best acetylcholinesterase inhibitory activity (IC 50 = 1.80 µM), however, it was inactive toward butyrylcholinesterase. It should be noted that compound 11b was evaluated for its BACE1 inhibitory activity and calculated IC 50 = 21.13 µM confirmed desired inhibitory activity. Also, this compound revealed satisfactory neuroprotective effect against H 2 O 2 -induced cell death in PC12 neurons at 50 µM as well as metal chelating ability toward Fe 2+ , Cu 2+ , and Zn 2+ ions. © 2018 Elsevier Inc.

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Style	Citing Format
MLA	Rastegari A, et al.. "Design, Synthesis and Anti-Alzheimer's Activity of Novel 1,2,3-Triazole-Chromenone Carboxamide Derivatives." Bioorganic Chemistry, vol. 83, no. , 2019, pp. 391-401.
APA	Rastegari A, Nadri H, Mahdavi M, Moradi A, Mirfazli SS, Edraki N, Moghadam FH, Larijani B, Akbarzadeh T, Saeedi M (2019). Design, Synthesis and Anti-Alzheimer's Activity of Novel 1,2,3-Triazole-Chromenone Carboxamide Derivatives. Bioorganic Chemistry, 83(), 391-401.
Chicago	Rastegari A, Nadri H, Mahdavi M, Moradi A, Mirfazli SS, Edraki N, Moghadam FH, Larijani B, Akbarzadeh T, Saeedi M. "Design, Synthesis and Anti-Alzheimer's Activity of Novel 1,2,3-Triazole-Chromenone Carboxamide Derivatives." Bioorganic Chemistry 83, no. (2019): 391-401.
Harvard	Rastegari A et al. (2019) 'Design, Synthesis and Anti-Alzheimer's Activity of Novel 1,2,3-Triazole-Chromenone Carboxamide Derivatives', Bioorganic Chemistry, 83(), pp. 391-401.
Vancouver	Rastegari A, Nadri H, Mahdavi M, Moradi A, Mirfazli SS, Edraki N, et al.. Design, Synthesis and Anti-Alzheimer's Activity of Novel 1,2,3-Triazole-Chromenone Carboxamide Derivatives. Bioorganic Chemistry. 2019;83():391-401.
BibTex	@article{ author = {Rastegari A and Nadri H and Mahdavi M and Moradi A and Mirfazli SS and Edraki N and Moghadam FH and Larijani B and Akbarzadeh T and Saeedi M}, title = {Design, Synthesis and Anti-Alzheimer's Activity of Novel 1,2,3-Triazole-Chromenone Carboxamide Derivatives}, journal = {Bioorganic Chemistry}, volume = {83}, number = {}, pages = {391-401}, year = {2019} }
RIS	TY - JOUR AU - Rastegari A AU - Nadri H AU - Mahdavi M AU - Moradi A AU - Mirfazli SS AU - Edraki N AU - Moghadam FH AU - Larijani B AU - Akbarzadeh T AU - Saeedi M TI - Design, Synthesis and Anti-Alzheimer's Activity of Novel 1,2,3-Triazole-Chromenone Carboxamide Derivatives JO - Bioorganic Chemistry VL - 83 IS - SP - 391 EP - 401 PY - 2019 ER -

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