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Date Published: 25/01/2025
Abstract Views: 384
Views PDF: 171
DOI: 10.58490/ctump.2025i83.3325
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No. 83 (2025)
Section
Article
How to Cite
Nguyen, V. H., Tran, P. T., Hoang, V. H., Le, T. B. L., Ngo, S. T., Le, Q. T., Bui, T. H. N., Tran, D. H., & Vu, N. H. L. (2025). SYNTHESIS AND EVALUATION OF THE ACETYLCHOLINESTERASE INHIBITORY EFFECT OF SOME NEW FLUOROAROMATIC DERIVATIVES BEARING 2-(5-(PYRIDIN-2-YL)-1H-TETRAZOL-1-YL)ACETAMID SCAFFOLD. Cantho Journal of Medicine and Pharmacy, 83, 46-52. https://doi.org/10.58490/ctump.2025i83.3325

SYNTHESIS AND EVALUATION OF THE ACETYLCHOLINESTERASE INHIBITORY EFFECT OF SOME NEW FLUOROAROMATIC DERIVATIVES BEARING 2-(5-(PYRIDIN-2-YL)-1H-TETRAZOL-1-YL)ACETAMID SCAFFOLD

Viet Hung Nguyen1,2, , Phuong Thao Tran1, Van Hai Hoang3, Thien Bao Long Le1, Son Tung Ngo4, Quoc Tien Le1, Thi Hong Nhung Bui1, Dinh Hoang Tran1, Ngoc Hai Linh Vu1
1 Hanoi University of Pharmacy
2 Hanoi University of Mining and Geology
3 PHENIKAA University
4 Ton Duc Thang University

Main Article Content

Abstract

Background: Alzheimer's disease (AD) is associated with a deficiency of the neurotransmitter acetylcholine (ACh) due to its hydrolysis and inactivation by the enzyme acetylcholinesterase (AChE). Therefore, AChE is an important and potential target in the discovery and development of new drugs for the treatment of AD. Objectives: Synthesizing five new fluoroaromatic derivatives IVa-e bearing the 2-(5-(pyridine-2-yl)-1H-tetrazol-1-yl)acetamid scaffold, evaluate the AChE inhibitory effect and study the "drug-like" properties. Materials and methods: Synthesized from the starting material 2pyridine carbonitrile. Five derivatives were structurally confirmed by infrared spectroscopy (IR), mass spectrometry (MS), nuclear magnetic resonance spectroscopy (NMR). Accordingly, drug-like properties and AChE inhibitory activity studies were conducted. Results: All compounds have “druglike” properties. The spectral structure confirmation results showed good agreement with the expected structures. The IVa-e derivatives all had certain AChE inhibitory abilities at concentrations of 75 µM and 125 µM. In particular, IV-b inhibited AChE the most at both concentrations. Conclusion: Five derivatives were synthesized that fit the intended structures, they didn’t violate Lipinski's 5 rules and Veber's rule, and they all capable of inhibiting AChE.

Keywords

Alzheimer, Acetylcholinesterase inhibitors, Tetrazole, Fluoroaromatic

Article Details

References

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