Abstract
The identification and characterisation of the isoenzyme cyclooxygenase 2 (COX-2) stimulated investigations to develop efficient nonsteroidal anti-inflammatory drugs with reduced side effects compared to standard NSAIDs. This review will focus on the structural features needed to achieve COX-2 selectivity. Five structural classes can be identified together with a class bearing little or no resemblance to one another in their molecular structure. The most interesting point is the very distinct structure/activity relationship. On the one hand only minor modifications to a particular compound induce a drastic change in its COX selectivity and on the other hand the structural prerequisites in terms of molecular shape, lipophilicity, electron density, flexibility, polarity and H-bonding dynamics allow a wide range of diversity.
Current Medicinal Chemistry
Title: Structural Approaches to Explain the Selectivity of COX-2 Inhibitors: Is There a Common Pharmacophore?
Volume: 7 Issue: 11
Author(s): G. Dannhardt and S. Laufer
Affiliation:
Abstract: The identification and characterisation of the isoenzyme cyclooxygenase 2 (COX-2) stimulated investigations to develop efficient nonsteroidal anti-inflammatory drugs with reduced side effects compared to standard NSAIDs. This review will focus on the structural features needed to achieve COX-2 selectivity. Five structural classes can be identified together with a class bearing little or no resemblance to one another in their molecular structure. The most interesting point is the very distinct structure/activity relationship. On the one hand only minor modifications to a particular compound induce a drastic change in its COX selectivity and on the other hand the structural prerequisites in terms of molecular shape, lipophilicity, electron density, flexibility, polarity and H-bonding dynamics allow a wide range of diversity.
Export Options
About this article
Cite this article as:
Dannhardt G. and Laufer S., Structural Approaches to Explain the Selectivity of COX-2 Inhibitors: Is There a Common Pharmacophore?, Current Medicinal Chemistry 2000; 7 (11) . https://dx.doi.org/10.2174/0929867003374237
DOI https://dx.doi.org/10.2174/0929867003374237 |
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
-
Emergence of Lipid-Based Vesicular Carriers as Nanoscale Pharmacotherapy in Rheumatoid Arthritis
Recent Patents on Nanomedicine NTproBNP: An Important Biomarker in Cardiac Diseases
Current Topics in Medicinal Chemistry A Systematic Review of Randomized Controlled Trials Examining the Nephroprotective Properties of Antihypertensive Medications
Current Hypertension Reviews XMT-1001, A Novel Biodegradable Polyacetal Polymer Conjugate of Camptothecin in Clinical Development
Current Bioactive Compounds Low Molecular Weight Inhibitors of the Protease Anthrax Lethal Factor
Mini-Reviews in Medicinal Chemistry C/EBPα Regulates FOXC1 to Modulate Tumor Growth by Interacting with PPARγ in Hepatocellular Carcinoma
Current Cancer Drug Targets Microcirculation in Sepsis: New Perspectives
Current Vascular Pharmacology Graphical Abstracts
Letters in Drug Design & Discovery Processing of Amyloid β-Peptides by Neutral Cysteine Protease Bleomycin Hydrolase
Protein & Peptide Letters Interaction of Nerve Agent Antidotes with Cholinergic Systems
Current Medicinal Chemistry The Role of Organic Transporters in Pharmacokinetics and Nephrotoxicity of Newer Antiviral Therapies for HIV and Hepatitis C
Current Drug Metabolism The SCF-type E3 Ubiquitin Ligases as Cancer Targets
Current Cancer Drug Targets Docking Prediction for Luteolin Inhibiting TNF-α and NF-κB Pathway
Letters in Drug Design & Discovery Probiotics and Oral Health
Current Pharmaceutical Design Nitric Oxide and Dietary Factors: Part III Minerals, Vitamins and Other Dietary and Lifestyle Factors
Vascular Disease Prevention (Discontinued) Nitrogen Containing Privileged Structures and their Solid Phase Combinatorial Synthesis
Combinatorial Chemistry & High Throughput Screening Targeting Tumors with Small Molecule Peptides
Current Cancer Drug Targets Oxidative Stress, Mitochondrial Abnormalities and Proteins Deposition: Multitarget Approaches in Alzheimer's Disease
Current Topics in Medicinal Chemistry Nanoparticles in Melanoma
Current Medicinal Chemistry Metallocarboxypeptidases and their Inhibitors: Recent Developments in Biomedically Relevant Protein and Organic Ligands
Current Medicinal Chemistry