Abstract
The saccharin ring system has gained considerable attention in the past decades, especially in the field of medicinal chemistry. The wide applicability of saccharin derivatives remains the driving force behind the constant development of novel routes and methods that provide new access to the construction of saccharin. Since the functionalization of this heterocycle has proved difficult, except for N- and O-alkylation, novel strategic approaches are much sought-after and thus constitute a great value to any medicinal chemist. In addition to the synthetic novelties introduced into the synthesis and functionalization of this particular heterocycle, the numerous newly discovered biological activities of saccharin and its derivatives are also reviewed. Saccharin may be considered to constitute a privileged framework on account of its role as a key structural element in several biologically active compounds ranging from enzyme inhibitors to receptor ligands and beyond.
Keywords: Saccharin, 1,1-dioxo-1,2-benzothiazol-3-one, heterocycle, synthesis, functionalization, bioactive compounds
Current Medicinal Chemistry
Title: Advances in the Chemistry of Saccharins: From Synthetic Novelties Towards Biologically Active Compounds
Volume: 17 Issue: 7
Author(s): Z. Jakopin and M. S. Dolenc
Affiliation:
Keywords: Saccharin, 1,1-dioxo-1,2-benzothiazol-3-one, heterocycle, synthesis, functionalization, bioactive compounds
Abstract: The saccharin ring system has gained considerable attention in the past decades, especially in the field of medicinal chemistry. The wide applicability of saccharin derivatives remains the driving force behind the constant development of novel routes and methods that provide new access to the construction of saccharin. Since the functionalization of this heterocycle has proved difficult, except for N- and O-alkylation, novel strategic approaches are much sought-after and thus constitute a great value to any medicinal chemist. In addition to the synthetic novelties introduced into the synthesis and functionalization of this particular heterocycle, the numerous newly discovered biological activities of saccharin and its derivatives are also reviewed. Saccharin may be considered to constitute a privileged framework on account of its role as a key structural element in several biologically active compounds ranging from enzyme inhibitors to receptor ligands and beyond.
Export Options
About this article
Cite this article as:
Jakopin Z. and Dolenc S. M., Advances in the Chemistry of Saccharins: From Synthetic Novelties Towards Biologically Active Compounds, Current Medicinal Chemistry 2010; 17 (7) . https://dx.doi.org/10.2174/092986710790416236
DOI https://dx.doi.org/10.2174/092986710790416236 |
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
-
Nanotechnology-based Targeting of Neurodegenerative Disorders: A Promising Tool for Efficient Delivery of Neuromedicines
Current Drug Targets Local Use-Dependent Sleep; Synthesis of the New Paradigm
Current Topics in Medicinal Chemistry Protection of Blood Brain Barrier Integrity and Modulation of Inflammatory Mediators During Treatment of Pneumococcal Meningitis with Daptomycin or Ceftriaxone
Current Neurovascular Research Therapeutic Targeting of TRP Channels - The TR(i)P to Pain Relief
Current Topics in Medicinal Chemistry Bergenin - A Biologically Active Scaffold: Nanotechnological Perspectives
Current Topics in Medicinal Chemistry Hypoxia-inducible Factor (HIF) in Hormone Signaling During Health and Disease
Cardiovascular & Hematological Agents in Medicinal Chemistry Targeted Drug Delivery Systems for Lung Macrophages
Current Drug Targets Tanshinone IIA Protects Hippocampal Neuronal Cells from Reactive Oxygen Species Through Changes in Autophagy and Activation of Phosphatidylinositol 3-Kinase, Protein Kinas B, and Mechanistic Target of Rapamycin Pathways
Current Neurovascular Research Organotypic Hippocampal Slice Cultures for Studies of Brain Damage, Neuroprotection and Neurorepair
Current Drug Targets - CNS & Neurological Disorders Curcumin Efficacy in a Serum/Glucose Deprivation-Induced Neuronal PC12 Injury Model
Current Molecular Pharmacology Dual Acting Anti-Inflammatory Drugs
Current Topics in Medicinal Chemistry Increased Serum Endotoxin and Elevated CD14 and IL-1β Expression in a Rat Model of Cerebrogenic Multiple Organ Dysfunction Syndrome
Medicinal Chemistry Is Adult Hippocampal Neurogenesis Really Relevant for the Treatment of Psychiatric Disorders?
Current Neuropharmacology AKT and cytosolic phospholipase A<sub>2</sub>α form a positive loop in prostate cancer cells
Current Cancer Drug Targets Surgical Treatment of Neonatal Mastitis by Periareolar Drainage
Current Pediatric Reviews Therapeutic Targets in Prostaglandin E2 Signaling for Neurologic Disease
Current Medicinal Chemistry Current Directions in Non-Invasive Low Intensity Electric Brain Stimulation for Depressive Disorder
CNS & Neurological Disorders - Drug Targets Peripheral Opioid Analgesia
Current Pharmaceutical Biotechnology Experimental and Clinical Application of Plasmid DNA in the Field of Central Nervous Diseases
Current Gene Therapy Nutraceuticals for Promoting Longevity
Current Nutraceuticals