Abstract
Acetylcholinesterase inhibitors are currently of high interest due to the many reasons. Among them, Alzheimers disease drugs are of great interest. In this study, eleven monoquaternary pyridinium salts substituted by different groups (electron donors and electron acceptors) in position four were prepared. Then, their anticholinesterase activity was tested. As observed, their IC50s ranged from 33 μM to 3981 μM. Moreover, probability of blood-brain barrier penetration was predicted.
Keywords: Quaternary ammonium salts, pyridinium salts, inhibitor, cholinesterase, Alzheimer's disease, prophylaxis
Letters in Organic Chemistry
Title: Preparation and In Vitro Evaluation of Monoquaternary Inhibitors of Brain Cholinesterases
Volume: 6 Issue: 6
Author(s): Daniel Jun, Martin Paar, Jiri Binder, Jan Marek, Miroslav Pohanka, Petr Stodulka and Kamil Kuca
Affiliation:
Keywords: Quaternary ammonium salts, pyridinium salts, inhibitor, cholinesterase, Alzheimer's disease, prophylaxis
Abstract: Acetylcholinesterase inhibitors are currently of high interest due to the many reasons. Among them, Alzheimers disease drugs are of great interest. In this study, eleven monoquaternary pyridinium salts substituted by different groups (electron donors and electron acceptors) in position four were prepared. Then, their anticholinesterase activity was tested. As observed, their IC50s ranged from 33 μM to 3981 μM. Moreover, probability of blood-brain barrier penetration was predicted.
Export Options
About this article
Cite this article as:
Jun Daniel, Paar Martin, Binder Jiri, Marek Jan, Pohanka Miroslav, Stodulka Petr and Kuca Kamil, Preparation and In Vitro Evaluation of Monoquaternary Inhibitors of Brain Cholinesterases, Letters in Organic Chemistry 2009; 6 (6) . https://dx.doi.org/10.2174/157017809789124876
DOI https://dx.doi.org/10.2174/157017809789124876 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Pharmacophore-based Drug Design of Novel Potential Tau Ligands for Alzheimer's Disease Treatment
Current Physical Chemistry Clearance of Amyloid-β Peptide by Neuronal and Non-Neuronal Cells: Proteolytic Degradation by Secreted and Membrane associated Proteases
Current Neurovascular Research Conjugative Post-Translational Modifications for Pharmacological Improvement of Therapeutic Proteins
Current Proteomics Quorum Sensing Inhibitors from the Sea: Lessons from Marine Symbiotic Relationships
Current Organic Chemistry Can Environmentally Relevant Levels of Aluminium Promote the Onset and Progression of Neurodegenerative Diseases?
Current Inorganic Chemistry (Discontinued) Biology and Clinical Management of Myeloproliferative Neoplasms and Development of the JAK Inhibitor Ruxolitinib
Current Medicinal Chemistry Different Inflammatory Biomarker Patterns in the Cerebro-Spinal Fluid Following Heart Surgery and Major Non-Cardiac Operations
Current Drug Metabolism Kappa Opioids, Salvinorin A and Major Depressive Disorder
Current Neuropharmacology Paroxetine Hydrochloride Push-pull Osmotic Pump Tablets: Designing an Innovative, Scalable Push-pull Osmotic Drug Delivery System Using QbD Approach
Drug Delivery Letters Symmetry-Correlated Component in the Visual-Evoked Potential: Electrophysiological Study of Visual Symmetry Perception in Humans
Neuroscience and Biomedical Engineering (Discontinued) A Review of Pharmacological Properties and Toxicological Effects of Adiantum capillus-veneris L.
Current Drug Discovery Technologies The New Era of Nutraceuticals: Beneficial Effects of Polyphenols in Various Experimental and Clinical Settings
Current Pharmaceutical Design Creating Change: How Knowledge Translates into Action for Protecting Babies from Sudden Infant Death?
Current Pediatric Reviews The Use of Dexmedetomidine in Anesthesia and Intensive Care: A Review
Current Pharmaceutical Design Structure, Pharmacology and Therapeutic Prospects of Family C G-Protein Coupled Receptors
Current Drug Targets The Anticonvulsant Effects of Ketogenic Diet on Epileptic Seizures and Potential Mechanisms
Current Neuropharmacology Cellular and Molecular Networks in Chronic Myeloid Leukemia: The Leukemic Stem, Progenitor and Stromal Cell Interplay
Current Drug Targets Nutrition and Physical Activity on Hypertension: Implication of Current Evidence and Guidelines
Current Hypertension Reviews Potential Anti-Catabolic and Anabolic Properties of Strontium Ranelate
Current Molecular Pharmacology Trigonelline: A Plant Alkaloid with Therapeutic Potential for Diabetes and Central Nervous System Disease
Current Medicinal Chemistry