New biologically active sulfonamides as potential drugs for Alzheimer's disease
Language English Country Germany Media print-electronic
Document type Journal Article
Grant support
Univerzita Pardubice
Internal Grant Agency of the University of Pardubice
- Keywords
- Alzheimer's disease, cholinesterase inhibitors, dissolution testing, sulfonamides, synthesis,
- MeSH
- Acetylcholinesterase metabolism MeSH
- Alzheimer Disease * drug therapy MeSH
- Butyrylcholinesterase * metabolism MeSH
- Cholinesterase Inhibitors * pharmacology chemical synthesis chemistry MeSH
- Hydrogen-Ion Concentration MeSH
- Humans MeSH
- Molecular Structure MeSH
- Rivastigmine pharmacology chemical synthesis chemistry MeSH
- Solubility MeSH
- Sulfonamides * pharmacology chemistry chemical synthesis MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Acetylcholinesterase MeSH
- Butyrylcholinesterase * MeSH
- Cholinesterase Inhibitors * MeSH
- Rivastigmine MeSH
- Sulfonamides * MeSH
A family of new compounds with sulfonamide and amide functional groups as potential Alzheimer's disease drugs were prepared by multistep synthesis. Thermal stability measurements recorded the initial decomposition in the range of 200-220°C, close above the melting point. The final compounds were tested for their ability to inhibit acetylcholinesterase and butyrylcholinesterase, and the in vitro dissolution behavior of selected compounds was studied through both lipophilic and hydrophilic matrix tablets. All nine tested derivatives were even more active in inhibiting acetylcholinesterase than the clinically used rivastigmine. Regression analysis of the obtained dissolution profiles was performed, and the effects of the pH and the release mechanism were determined. Some substances showed remarkable biological activity and became a subject of interest for further extensive study.
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