Abstract
Background: The design of multifunctional agents represents one of the most active research field in medicinal chemistry. In particular, tacrine, a well known Acetylcholinesterase inhibitor, is one of the most used starting point to develop multifunctional ligands and hundreds of papers report about these new agents. This is the third review of a series concerning tacrinebased multifunctional ligands; in particular, in the present, we will summarize and discuss the most intriguing examples of tacrine-based multifunctional agents published since 2013 until 2016.
Methods: We analyzed the bibliographic databases for peer-reviewed publications concerning tacrine-based multifunctional agents possessing biological actions that go beyond the simple “cholinergic” blockage. These papers have been subdivided according to their biological activities. Since this is the third review of a series, we took into considerations only the papers appeared since 2013 until 2016.
Results: In this review, we have analyzed more than 33 papers. All the reported compounds retain good inhibitory activity towards acetyl- and butyryl-cholinesterase. The other biological activities concern mostly inhibition of a) β-amyloid aggregation, b) β-secretase, c) monoamino oxidases, modulation of τ and ROS and metal chelation.
Conclusion: The analysis of the current literature reported in this review confirm the importance of tacrine as scaffold to develop multifunctional agents potentially usefull to contrast Alzheimer's disease. Furthermore, the compounds herein reported showed very intriguing biological activities that could be used as starting point to develop new compounds even more interesting and, hopefully, clinically usefull to contrast Alzheimer's Disease.
Keywords: Neurodegenerative diseases, Alzheimer's disease, tacrine, tacrine hybrids, dual binding acetylcholinesterase inhibitors, acetylcholinesterase inhibitors.
Current Medicinal Chemistry
Title:Tacrine-based Multifunctional Agents in Alzheimer's Disease: An Old Story in Continuous Development§
Volume: 24 Issue: 32
Author(s): Andrea Milelli*, Angela De Simone, Nicole Ticchi, Huan H. Chen, Nibal Betari, Vincenza Andrisano and Vincenzo Tumiatti
Affiliation:
- Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d'Augusto 237, 47921 Rimini,Italy
Keywords: Neurodegenerative diseases, Alzheimer's disease, tacrine, tacrine hybrids, dual binding acetylcholinesterase inhibitors, acetylcholinesterase inhibitors.
Abstract: Background: The design of multifunctional agents represents one of the most active research field in medicinal chemistry. In particular, tacrine, a well known Acetylcholinesterase inhibitor, is one of the most used starting point to develop multifunctional ligands and hundreds of papers report about these new agents. This is the third review of a series concerning tacrinebased multifunctional ligands; in particular, in the present, we will summarize and discuss the most intriguing examples of tacrine-based multifunctional agents published since 2013 until 2016.
Methods: We analyzed the bibliographic databases for peer-reviewed publications concerning tacrine-based multifunctional agents possessing biological actions that go beyond the simple “cholinergic” blockage. These papers have been subdivided according to their biological activities. Since this is the third review of a series, we took into considerations only the papers appeared since 2013 until 2016.
Results: In this review, we have analyzed more than 33 papers. All the reported compounds retain good inhibitory activity towards acetyl- and butyryl-cholinesterase. The other biological activities concern mostly inhibition of a) β-amyloid aggregation, b) β-secretase, c) monoamino oxidases, modulation of τ and ROS and metal chelation.
Conclusion: The analysis of the current literature reported in this review confirm the importance of tacrine as scaffold to develop multifunctional agents potentially usefull to contrast Alzheimer's disease. Furthermore, the compounds herein reported showed very intriguing biological activities that could be used as starting point to develop new compounds even more interesting and, hopefully, clinically usefull to contrast Alzheimer's Disease.
Export Options
About this article
Cite this article as:
Milelli Andrea *, De Simone Angela , Ticchi Nicole , Chen H. Huan , Betari Nibal , Andrisano Vincenza and Tumiatti Vincenzo , Tacrine-based Multifunctional Agents in Alzheimer's Disease: An Old Story in Continuous Development§, Current Medicinal Chemistry 2017; 24 (32) . https://dx.doi.org/10.2174/0929867324666170309123920
DOI https://dx.doi.org/10.2174/0929867324666170309123920 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- 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
- Announcements
Related Articles
-
Targeting Beta-Amyloid Pathogenesis Through Acetylcholinesterase Inhibitors
Current Pharmaceutical Design Cancer T Cell Immunotherapy with Bispecific Antibodies and Chimeric Antigen Receptors
Recent Patents on Anti-Cancer Drug Discovery Therapeutic Approaches Targeting Pathological Tau Aggregates
Current Pharmaceutical Design Neurokinin-1 Receptor Antagonists as Anticancer Drugs
Letters in Drug Design & Discovery Connections Between Herpes Simplex Virus Type 1 and Alzheimer's Disease Pathogenesis
Current Alzheimer Research Mechanism of Cancer Drug Resistance and the Involvement of Noncoding RNAs
Current Medicinal Chemistry Anabolic Androgenic Steroids and Intracellular Calcium Signaling: A Mini Review on Mechanisms and Physiological Implications
Mini-Reviews in Medicinal Chemistry New Molecular Targets in the Treatment of NSCLC
Current Pharmaceutical Design Neuroprotective Role of Nanoparticles Against Alzheimer's Disease
Current Drug Metabolism Protein Amyloidogenesis Investigated by Small Angle Scattering
Current Pharmaceutical Design Rapid Non-genomic Vasodilator Actions of Oestrogens and Sex Steroids
Current Medicinal Chemistry Snake Venom Metalloproteinase Containing a Disintegrin-like Domain, its Structure-activity Relationships at Interacting with Integrins
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Exploiting Microwave-Assisted Organic Synthesis (MAOS) for Accessing Bioactive Scaffolds
Current Organic Chemistry Prospects for Rational Development of Pharmacological Gap Junction Channel Blockers
Current Drug Targets Oxidation Chemistry of Catecholamines and Neuronal Degeneration: An Update
Current Medicinal Chemistry Irinotecan for Treatment of Childhood Cancers: A Promising Therapeutic Partner
Current Cancer Therapy Reviews The Impact of Small Heat Shock Proteins (HspBs) in Alzheimer’s and Other Neurological Diseases
Current Pharmaceutical Design Internal Ribosome Entry Site Elements in Eukaryotic Genomes
Current Genomics Immune Checkpoint Inhibitors: Basics and Challenges
Current Medicinal Chemistry Autism, Mitochondria and Polybrominated Diphenyl Ether Exposure
CNS & Neurological Disorders - Drug Targets