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 |
![Wayfinder Image](/images/wayfinder.jpg)
- 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
-
Insights into Aβ Aggregation: A Molecular Dynamics Perspective
Current Topics in Medicinal Chemistry The Role of the Catechol-o-Methyltransferase (COMT) GeneVal158Met in Aggressive Behavior, a Review of Genetic Studies
Current Neuropharmacology Psychological Problems in Female Fragile X Premutations Carriers
Current Psychiatry Reviews Editorial (Thematic Issue: Ceramics, Nanotubes, Advanced Materials: Theoretical and Experimental Structure-Property Relationships Part IV)
Current Physical Chemistry Neuron Protection as a Therapeutic Target in Acute Ischemic Stroke
Current Topics in Medicinal Chemistry A Medicinal Mushroom: Phellinus Linteus
Current Medicinal Chemistry Endothelial Dysfunction in the Hypertensive State: Mechanisms of Hypertensive Cardiovascular Complications
Current Hypertension Reviews Hydrophobic Plant Antioxidants. Preparation of Nanoparticles and their Application for Prevention of Neurodegenerative Diseases. Review and Experimental Data
Current Topics in Medicinal Chemistry Mitochondria as a Therapeutic Target in Alzheimers Disease and Diabetes
CNS & Neurological Disorders - Drug Targets Aptamers as Innovative Diagnostic and Therapeutic Agents in the Central Nervous System
CNS & Neurological Disorders - Drug Targets Age-related Changes in Pharmacodynamics: Focus on Drugs Acting on Central Nervous and Cardiovascular Systems
Current Drug Metabolism Effects of Nicotine on the Cardiovascular System
Vascular Disease Prevention (Discontinued) Role of Amylin and its Receptors in Neurodegeneration
Current Protein & Peptide Science Recent Advances in the Treatment of Neurogenic Erectile Dysfunction
Recent Patents on CNS Drug Discovery (Discontinued) Hrd1 Facilitates Tau Degradation and Promotes Neuron Survival
Current Molecular Medicine Oxocarbon Acids and their Derivatives in Biological and Medicinal Chemistry
Current Medicinal Chemistry Delivery of Anti-Viral Nucleoside Analogues to the Central Nervous System
Current Medicinal Chemistry - Anti-Infective Agents Aging Affects Nicotinic Acetylcholine Receptors in Brain
Central Nervous System Agents in Medicinal Chemistry Advances in Drug Discovery to Assess Cholinergic Neurotransmission: A Systematic Review
Current Drug Discovery Technologies Advances in Studies on Stroke-Induced Secondary Neurodegeneration (SND) and Its Treatment
Current Topics in Medicinal Chemistry