Phenyl-Quinoline Derivatives As Lead Structure of Cholinesterase Inhibitors With Potency to Reduce the Gsk-3Β Level Targeting Alzheimer's Disease

Phenyl-Quinoline Derivatives As Lead Structure of Cholinesterase Inhibitors With Potency to Reduce the Gsk-3Β Level Targeting Alzheimer's Disease Publisher Pubmed

Noori M^{1, 2} ; Dastyafteh N¹ ; Safapoor S³ ; Khalili Ghomi M³ ; Tanideh R² ; Zomorodian K⁴ ; Hamedifar H^{5, 6} ; Dara M² ; Zare S² ; Irajie C⁷ ; Javanshir S¹ ; Rastegar H⁸ ; Panahi N¹⁰ ; Larijani B³ Show All Authors

Noori M^{1, 2}
Dastyafteh N¹
Safapoor S³
Khalili Ghomi M³
Tanideh R²
Zomorodian K⁴
Hamedifar H^{5, 6}
Dara M²
Zare S²
Irajie C⁷
Javanshir S¹
Rastegar H⁸
Panahi N¹⁰
Larijani B³
Mahdavi M³
Hajimiri MH^{5, 6}
Iraji A^{2, 9}

Show Affiliations

1. Pharmaceutical and Heterocyclic Chemistry Research Laboratory, Department of Chemistry, Iran University of Science and Technology, Tehran, Iran
2. Stem Cells Technology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
3. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
4. Department of Medical Mycology and Parasitology, School of Medicine, Shiraz University of Medical Sciences, Shiraz, Iran
5. CinnaGen Medical Biotechnology Research Center, Alborz University of Medical Sciences, Karaj, Iran
6. CinnaGen Research and Production Co., Alborz, Iran
7. Department of Medical Biotechnology, School of Advanced Medical Sciences and Technologies, Shiraz University of Medical Sciences, Shiraz, Iran
8. Food and Drug Research Institute, Food and Drug Administration, MOHE, Tehran, Iran
9. Research Center for Traditional Medicine and History of Medicine, Department of Persian Medicine, School of Medicine, Shiraz University of Medical Sciences, Shiraz, Iran
10. Metabolic Disorders Research Center, Endocrinology and Metabolism Molecular-Cellular Sciences Institute, Tehran University of Medical Science

Source: International Journal of Biological Macromolecules Published:2023

Abstract

Alzheimer's disease (AD) is a neurodegenerative disorder that leads to cognitive decline and memory loss. Unfortunately, there is no effective treatment for this condition, so there is a growing interest in developing new anti-AD agents. In this research project, a series of phenyl-quinoline derivatives were designed as potential anti-AD agents. These derivatives were substituted at two different positions on benzyl and phenyl rings. The structures of the derivatives were characterized using techniques such as IR spectroscopy, 1H NMR, 13C NMR, and elemental analysis. During the in vitro screening, the derivatives were tested against both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). It was observed that most of the derivatives showed higher selectivity against BChE compared to AChE. Among the derivatives, analog 7n (with a methoxy group at R1 and a 4-bromine substituent at R2 exhibited the highest potency, with a 75-fold improvement in the activity compared to the positive control. Importantly, this potent analog demonstrated no toxicity at the tested concentration on SH-SY5Y cells, indicating its potential as a safe anti-AD agent. The level of GSK-3β was also reduced after treatments with 7n at 50 μM. Overall, this study highlights the design and evaluation of phenyl-quinoline derivatives as promising candidates for developing novel anti-AD agents. © 2023

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Style	Citing Format
MLA	Noori M, et al.. "Phenyl-Quinoline Derivatives As Lead Structure of Cholinesterase Inhibitors With Potency to Reduce the Gsk-3Β Level Targeting Alzheimer's Disease." International Journal of Biological Macromolecules, vol. 253, no. , 2023, pp. -.
APA	Noori M, Dastyafteh N, Safapoor S, Khalili Ghomi M, Tanideh R, Zomorodian K, Hamedifar H, Dara M, Zare S, Irajie C, Javanshir S, Rastegar H, Panahi N, Larijani B, Mahdavi M, Hajimiri MH, Iraji A (2023). Phenyl-Quinoline Derivatives As Lead Structure of Cholinesterase Inhibitors With Potency to Reduce the Gsk-3Β Level Targeting Alzheimer's Disease. International Journal of Biological Macromolecules, 253(), -.
Chicago	Noori M, Dastyafteh N, Safapoor S, Khalili Ghomi M, Tanideh R, Zomorodian K, Hamedifar H, et al.. "Phenyl-Quinoline Derivatives As Lead Structure of Cholinesterase Inhibitors With Potency to Reduce the Gsk-3Β Level Targeting Alzheimer's Disease." International Journal of Biological Macromolecules 253, no. (2023): -.
Harvard	Noori M et al. (2023) 'Phenyl-Quinoline Derivatives As Lead Structure of Cholinesterase Inhibitors With Potency to Reduce the Gsk-3Β Level Targeting Alzheimer's Disease', International Journal of Biological Macromolecules, 253(), pp. -.
Vancouver	Noori M, Dastyafteh N, Safapoor S, Khalili Ghomi M, Tanideh R, Zomorodian K, et al.. Phenyl-Quinoline Derivatives As Lead Structure of Cholinesterase Inhibitors With Potency to Reduce the Gsk-3Β Level Targeting Alzheimer's Disease. International Journal of Biological Macromolecules. 2023;253():-.
BibTex	@article{ author = {Noori M and Dastyafteh N and Safapoor S and Khalili Ghomi M and Tanideh R and Zomorodian K and Hamedifar H and Dara M and Zare S and Irajie C and Javanshir S and Rastegar H and Panahi N and Larijani B and Mahdavi M and Hajimiri MH and Iraji A}, title = {Phenyl-Quinoline Derivatives As Lead Structure of Cholinesterase Inhibitors With Potency to Reduce the Gsk-3Β Level Targeting Alzheimer's Disease}, journal = {International Journal of Biological Macromolecules}, volume = {253}, number = {}, pages = {-}, year = {2023} }
RIS	TY - JOUR AU - Noori M AU - Dastyafteh N AU - Safapoor S AU - Khalili Ghomi M AU - Tanideh R AU - Zomorodian K AU - Hamedifar H AU - Dara M AU - Zare S AU - Irajie C AU - Javanshir S AU - Rastegar H AU - Panahi N AU - Larijani B AU - Mahdavi M AU - Hajimiri MH AU - Iraji A TI - Phenyl-Quinoline Derivatives As Lead Structure of Cholinesterase Inhibitors With Potency to Reduce the Gsk-3Β Level Targeting Alzheimer's Disease JO - International Journal of Biological Macromolecules VL - 253 IS - SP - EP - PY - 2023 ER -

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