Abstract
The aim of this study was to synthesize and evaluate diazapentacyclic analogs for their acetylcholinesterase (AChE) inhibitory activity. The pentacyclic analogs were synthesized by one-pot three-component domino reactions in a microwave synthesizer. Most of the compounds exhibited moderate to good AChE inhibitory activity, compound 5i showed potent inhibitory activity with IC50 1.12±0.01 µM and this may provide a new lead for developing potential inhibitors for Alzheimer's disease.
Keywords: Alzheimer's disease, AChE inhibitor, 1, 3-Dipolar cycloaddition, azomethine ylide, diazapentacycles and microwave irradiation.
Medicinal Chemistry
Title:An Expedient Synthesis and Screening for Antiacetylcholinesterase Activity of Piperidine Embedded Novel Pentacyclic Cage Compounds
Volume: 10 Issue: 2
Author(s): Raju Suresh Kumar, Abdulrahman I. Almansour, Natarajan Arumugam, Hasnah Osman, Mohamed Ashraf Ali, Alireza Basiri and Yalda Kia
Affiliation:
Keywords: Alzheimer's disease, AChE inhibitor, 1, 3-Dipolar cycloaddition, azomethine ylide, diazapentacycles and microwave irradiation.
Abstract: The aim of this study was to synthesize and evaluate diazapentacyclic analogs for their acetylcholinesterase (AChE) inhibitory activity. The pentacyclic analogs were synthesized by one-pot three-component domino reactions in a microwave synthesizer. Most of the compounds exhibited moderate to good AChE inhibitory activity, compound 5i showed potent inhibitory activity with IC50 1.12±0.01 µM and this may provide a new lead for developing potential inhibitors for Alzheimer's disease.
Export Options
About this article
Cite this article as:
Kumar Suresh Raju, Almansour I. Abdulrahman, Arumugam Natarajan, Osman Hasnah, Ali Ashraf Mohamed, Basiri Alireza and Kia Yalda, An Expedient Synthesis and Screening for Antiacetylcholinesterase Activity of Piperidine Embedded Novel Pentacyclic Cage Compounds, Medicinal Chemistry 2014; 10 (2) . https://dx.doi.org/10.2174/157340641002140131170054
DOI https://dx.doi.org/10.2174/157340641002140131170054 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
![](/images/wayfinder.jpg)
- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
-
Berberine Ameliorates Cognitive Impairment by Regulating Microglial Polarization
and Increasing Expression of Anti-inflammatory Factors following
Permanent Bilateral Common Carotid Artery Occlusion in Rats
CNS & Neurological Disorders - Drug Targets Mitochondrial Triglyceride Transfer Protein Inhibition: New Achievements in the Treatment of Dyslipidemias
Current Pharmaceutical Design Visual and Quantitative Assessment of COVID-19 Pneumonia on Chest CT: The Relationship with Disease Severity and Clinical Findings
Current Medical Imaging Patent Selections
Recent Patents on Biotechnology New Potential Serum Biomarkers in Multiple Sclerosis Identified by Proteomic Strategies
Current Medicinal Chemistry Cross Sectional Observational Study on the Societal Costs of Alzheimers Disease
Current Alzheimer Research Cytoskeletal Pathologies of Age-Related Diseases between Elderly Sri Lankan (Colombo) and Indian (Bangalore) Brain Samples
Current Alzheimer Research Tailored Multi-Target Agents. Applications and Design Considerations
Current Pharmaceutical Design The Interaction of DNA-Binding Ligands with Trinucleotide-Repeat DNA: Implications for Therapy and Diagnosis of Neurological Disorders
Current Topics in Medicinal Chemistry Editorial (Thematic Issue: Neuroprotective Effects of Li - It is Elementary)
Current Alzheimer Research Probable Novel PSEN1 Gln222Leu Mutation in a Chinese Family with Early-Onset Alzheimer's Disease
Current Alzheimer Research Proteomic Analysis of Alzheimers Disease Cerebrospinal Fluid from Neuropathologically Diagnosed Subjects
Current Alzheimer Research Noradrenergic System in Down Syndrome and Alzheimer’s Disease A Target for Therapy
Current Alzheimer Research Mononuclear Cell Recruitment and Inflammation in Atherosclerosis
Vascular Disease Prevention (Discontinued) Glycoconjugates: Roles in Neural Diseases Caused by Exogenous Pathogens
CNS & Neurological Disorders - Drug Targets Preface
Current Medicinal Chemistry - Central Nervous System Agents An Apple Plus a Brazil Nut a Day Keeps the Doctors Away: Antioxidant Capacity of Foods and their Health Benefits
Current Pharmaceutical Design Development of Phthalimide-Donepezil Hybrids as Potent Multitarget- Directed Ligands for the Treatment of Alzheimer’s Disease
Letters in Drug Design & Discovery Cerebral Hypoperfusion During Carotid Artery Stenosis can Lead to Cognitive Deficits that may be Independent of White Matter Lesion Load
Current Neurovascular Research Cognitive Impairment and Diabetes
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued)