Abstract
Hydroxypyridinones (HPs) are a family of N-heterocyclic metal chelators, which have been an attractive target in the development of a variety of new pharmaceutical drugs, due to their high metal chelating efficacy/specificity and easy derivatization to tune the desired biological properties. In fact, along the last decades, hydroxypyridinone derivatives, but mostly 3-hydroxy-4-pyridinone (3,4-HP), have been intensively used in drug design, following either a multitarget approach, in which one chelating unity is extrafunctionalized (hybridized) to enable the interaction with other important specific biological sites, or a polydenticity approach, in which more than one chelating moiety is conveniently attached to one scaffold, to increase the metal chelating efficacy. This review represents an update of the most recent publications (2014-2016) in mono-HP hybrids, namely as potential anti-Alzheimer's drugs, inhibitors of metalloenzymes and anti-microbials, and also polychelating compounds (poly- HP), in view of potential application, such as anti-microbial/biostatic agents, luminescent biosensors or diagnostic agents.
Keywords: Hydroxypyridinones, 3-hydroxy-4-pyridinones, iron chelators, anti-neurodegeneratives, bioinorganic medicinal chemistry.
Current Medicinal Chemistry
Title:Hydroxypyridinone Derivatives: A Fascinating Class of Chelators with Therapeutic Applications - An Update
Volume: 25 Issue: 1
Author(s): Sílvia Chaves, Luca Piemontese, Asha Hiremathad and M. Amélia Santos*
Affiliation:
- Centro de Quimica Estrutural, Instituto Superior Tecnico, Universidade de Lisboa, Av. Rovisco Pais 1, 1049-001 Lisboa,Portugal
Keywords: Hydroxypyridinones, 3-hydroxy-4-pyridinones, iron chelators, anti-neurodegeneratives, bioinorganic medicinal chemistry.
Abstract: Hydroxypyridinones (HPs) are a family of N-heterocyclic metal chelators, which have been an attractive target in the development of a variety of new pharmaceutical drugs, due to their high metal chelating efficacy/specificity and easy derivatization to tune the desired biological properties. In fact, along the last decades, hydroxypyridinone derivatives, but mostly 3-hydroxy-4-pyridinone (3,4-HP), have been intensively used in drug design, following either a multitarget approach, in which one chelating unity is extrafunctionalized (hybridized) to enable the interaction with other important specific biological sites, or a polydenticity approach, in which more than one chelating moiety is conveniently attached to one scaffold, to increase the metal chelating efficacy. This review represents an update of the most recent publications (2014-2016) in mono-HP hybrids, namely as potential anti-Alzheimer's drugs, inhibitors of metalloenzymes and anti-microbials, and also polychelating compounds (poly- HP), in view of potential application, such as anti-microbial/biostatic agents, luminescent biosensors or diagnostic agents.
Export Options
About this article
Cite this article as:
Chaves Sílvia , Piemontese Luca , Hiremathad Asha and Santos Amélia M. *, Hydroxypyridinone Derivatives: A Fascinating Class of Chelators with Therapeutic Applications - An Update, Current Medicinal Chemistry 2018; 25 (1) . https://dx.doi.org/10.2174/0929867324666170330092304
DOI https://dx.doi.org/10.2174/0929867324666170330092304 |
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
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
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
-
Rivastigmine for Refractory REM Behavior Disorder in Mild Cognitive Impairment
Current Alzheimer Research <i>In Vivo</i> Longitudinal Monitoring of Changes in the Corpus Callosum Integrity During Disease Progression in a Mouse Model of Alzheimer’s Disease
Current Alzheimer Research Gene Therapy for Angelman Syndrome: Contemporary Approaches and Future Endeavors
Current Gene Therapy Brain Hyperthermia During Physiological and Pathological Conditions: Causes, Mechanisms, and Functional Implications
Current Neurovascular Research Imaging of Muscarinic Receptors in the Central Nervous System
Current Pharmaceutical Design Topiramate Decelerates Bicarbonate-Driven Acid-Elimination of Human Neocortical Neurons: Strategic Significance for its Antiepileptic, Antimigraine and Neuroprotective Properties
CNS & Neurological Disorders - Drug Targets Subject Index to Volume 1
Current Neurovascular Research Potential for Discovery of Neuroprotective Factors in Serum and Tissue from Hibernating Species
Mini-Reviews in Medicinal Chemistry Recent Development in Neuronal Migration Disorders: Clinical, Neuroradiologic and Genetics Aspects
Current Pediatric Reviews Transglutaminases as Possible Therapeutic Targets in Neurodegenerative Diseases
Recent Patents on CNS Drug Discovery (Discontinued) Transitional Polytherapy: Tricks of the Trade for Monotherapy to Monotherapy AED Conversions
Current Neuropharmacology Serotonin as a Modulator of Glutamate- and GABA-Mediated Neurotransmission: Implications in Physiological Functions and in Pathology
Current Neuropharmacology Redox Regulation and the Autistic Spectrum: Role of Tryptophan Catabolites, Immuno-inflammation, Autoimmunity and the Amygdala
Current Neuropharmacology Pharmacological Management of Huntingtons Disease: An Evidence- Based Review
Current Pharmaceutical Design Cell Type Specificity of GABAA Receptor Mediated Signaling in the Hippocampus
Current Drug Targets - CNS & Neurological Disorders Editorial (Thematic Issue: Measurements of ABC Transporters at the Blood-Brain Barrier: Novel Methods and Applications)
Current Pharmaceutical Design Cognitive Identity in Schizophrenia: Vision, Space, and Body Perception from Prodrome to Syndrome
Current Psychiatry Reviews Assessing Structure, Function and Druggability of Major Inhibitory Neurotransmitter γ-Aminobutyrate Symporter Subtypes
Current Medicinal Chemistry Therapeutic Targets for the Management of Peripheral Nerve Injury- Induced Neuropathic Pain
CNS & Neurological Disorders - Drug Targets A Synopsis of Nano-Technological Approaches Toward Anti-Epilepsy Therapy: Present and Future Research Implications
Current Drug Metabolism