Tehran University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share this content! By
Design and Synthesis of New Substituted Benzyl-1,2,3-Triazole-Methoxybenzylidene Coupled to Arylacetohydrazides Against Alzheimer's Disease Publisher



A Iraji AIDA ; D Shargheiboroujeni DIBA ; A Aliabadi ARIAN ; M Dara MAHINTAJ ; Mh Hashempur Mohammad HASHEM ; R Hariri ROSHANAK ; Dam Khassaki Dhuha Ali MAHDI ; M Saeedi MINA ; T Akbarzadeh TAHMINEH
Authors

Source: Journal of Molecular Structure Published:2025


Abstract

In this work, new hybrids of substituted benzyl-1,2,3-triazole-methoxybenzylidene-arylacetohydrazides were designed and synthesized to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), as one of the most promising strategies for the treatment of Alzheimer's disease (AD). Among them, compound 10c was found potent against AChE and BChE with IC50 values of 18.42 ± 0.89 and 21.25 ± 0.59 μM, respectively. Additionally, the conduct of kinetic and molecular docking studies revealed essential interactions between compound 10c and key catalytic residues of the enzymes. Furthermore, compound 10c revealed low cytotoxicity to downregulate important genes, including GSK-3β and BACE1, related to AD. © 2025 Elsevier B.V., All rights reserved.
Related Docs
View other Related Docs
1. Design and Evaluation of Substituted Cinnamoyl Piperidinyl Acetate Derivatives As Potent Cholinesterase Inhibitors, Scientific Reports (2025)
2. Cinnamic Acid Conjugated With Triazole Acetamides As Anti-Alzheimer and Anti-Melanogenesis Candidates: An in Vitro and in Silico Study, Scientific Reports (2025)
3. Design and Synthesis of New 1,2,3-Triazole-Methoxyphenyl-1,3,4-Oxadiazole Derivatives: Selective Butyrylcholinesterase Inhibitors Against Alzheimer’S Disease, BMC Chemistry (2025)
Experts (# of related papers)
View all Related Experts
Mohammad Mahdavi (14)
Bagher Larijani (8)
Other Related Docs
4. Isoindolinedione-Benzamide Pyridinium Derivatives for Targeting Alzheimer’S Disease, ACS Omega (2024)
5. Synthesis, and in Vitro Biological Evaluations of Novel Naphthoquinone Conjugated to Aryl Triazole Acetamide Derivatives As Potential Anti-Alzheimer Agents, Journal of Molecular Structure (2022)
6. 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)
7. Phenyldiazenyl-Phenoxy-1,2,3-Triazol-Acetamide Derivatives As New Dual Cholinesterase Inhibitors: Design, Synthesis, in Vitro, and in Silico Enzymatic Inhibition Evaluations, Journal of Molecular Structure (2025)
8. New Classes of Carbazoles As Potential Multi-Functional Anti-Alzheimer's Agents, Bioorganic Chemistry (2019)
9. Synthesis and Evaluation of Novel Arylisoxazoles Linked to Tacrine Moiety: In Vitro and in Vivo Biological Activities Against Alzheimer’S Disease, Molecular Diversity (2022)
10. Novel Diazen-Bis(Phenoxy-1,2,3-Triazole-N-Phenylacetamide) Derivatives As Potent Anti-Cholinesterase, Anti-Α-Glycosidase and Anti-Α-Amylase Agents: In Vitro and in Silico Evaluations, Journal of Molecular Structure (2025)
11. Synthesis and Biological Activity of Some Benzochromenoquinolinones: Tacrine Analogs As Potent Anti-Alzheimer's Agents, Chemistry and Biodiversity (2019)
12. Amino-7,8-Dihydro-4H-Chromenone Derivatives As Potential Inhibitors of Acetylcholinesterase and Butyrylcholinesterase for Alzheimer’S Disease Management; in Vitro and in Silico Study, BMC Chemistry (2024)
13. Anticholinesterase Activities of Novel Isoindolin-1,3-Dione-Based Acetohydrazide Derivatives: Design, Synthesis, Biological Evaluation, Molecular Dynamic Study, BMC Chemistry (2024)
14. Design, Synthesis and Biological Assessment of New 1-Benzyl-4-((4-Oxoquinazolin-3(4H)-Yl)Methyl) Pyridin-1-Ium Derivatives (Bops) As Potential Dual Inhibitors of Acetylcholinesterase and Butyrylcholinesterase, Heliyon (2021)
15. Novel N-Benzylpiperidine Derivatives of 5-Arylisoxazole-3-Carboxamides As Anti-Alzheimer's Agents, Archiv der Pharmazie (2021)
16. Synthesis and Anticholinesterase Activity of New Substituted Benzo[D]Oxazole-Based Derivatives, Chemical Biology and Drug Design (2017)
17. New 1E,1′E-Hydrazine-Bis(Phenoxy-1,2,3-Triazol-Acetamide) Derivatives As Potent Inhibitors Against Acetylcholinesterase, Butyrylcholinesterase, and Α-Glucosidase, RSC Advances (2025)
18. Phthalimide-Derived N-Benzylpyridinium Halides Targeting Cholinesterases: Synthesis and Bioactivity of New Potential Anti-Alzheimer's Disease Agents, Archiv der Pharmazie (2016)
19. Design, Synthesis and Anti-Alzheimer's Activity of Novel 1,2,3-Triazole-Chromenone Carboxamide Derivatives, Bioorganic Chemistry (2019)
20. Synthesis and Bio-Evaluation of New Multifunctional Methylindolinone-1,2,3-Triazole Hybrids As Anti-Alzheimer's Agents, Journal of Molecular Structure (2021)