VANILLIN-BASED THIAZINE, OXAZINE, AND PYRAZOLE AS A NON-COMPETITIVE AMPA RECEPTOR ANTAGONISTS
No Thumbnail Available
Date
2024-07-27
Authors
Awwadeh, Ata'
Journal Title
Journal ISSN
Volume Title
Publisher
An-Najah National University
Abstract
Background: Heterocyclic derivatives have received much attention from researchers because they are important components of natural compounds and synthetic drugs, as they are considered safe, abundant, and available at a reasonable cost.
Objictive: This work aims to create an anti-alzheimer's disease and anti-microbial drug with enhanced efficacy and lower toxicity based on heterocyclic derivatives including oxazine, thiazine, and pyrazole. The objective of this work is to manufacture a drug from the aforementioned derivatives aimed at alleviating and treating alzheimer's disease, and the drug has very few side effects.
Methodology: To achieve the goal of the study, several compounds derived from oxazine, thiazine, pyrazole, phenyl pyrazole, and pyrazole with semicarbazide were synthesized. The synthesis was performed in a two-step process. It is considered a condensation reaction. In the first step, chalcone is prepared from the reacting benzophenone with vanillin in an alkaline medium. The α-H of the benzophenone is extracted, and this creates a nucleophilic center (enolate) that attacks the carbonyl of the aldehyde. Neutralization followed by dehydration results in the production of the target compound.
Results: The structures of the prepared compounds were identified by FT-IR and by 1H-NMR spectroscopy. The productivity of the compounds ranged from 80 to 90%. The compounds showed clear activity in treating alzheimer's disease vanillin-based noncompetitive antagonists of AMPA receptors, reducing amyloid plaques, reducing tau tangles, and improving brain functions.
Conclusion: The study concluded that the compounds were successfully manufactured by condensation reaction and their anti-alzheimer's activity as well as the anti-microbial results are pending. They are expected to show promising results. There is still more work to be done to determine the most potent of the prepared derivatives and their mechanism of action.