Abstract
In this article we provide an overview on the medicinal chemistry of new bioactive N-acylhydrazone (NAH) derivatives designed through the structural optimization of N-arylhydrazone precursors, originally planned by molecular hybridization of two known 5-lipoxygenase inhibitors, i.e. CBS-1108 and BW-755c. The analgesic, antiedematogenic and platelet anti-aggregating profile of several isosteric NAH compounds was investigated by using classical in vivo and ex-vivo pharmacological assays, which allowed the identification of new potent centrally and peripherically-acting analgesic leads, new antiinflammatory agents and new antithrombotic prototypes. During this study, dozens of active NAH compounds were discovered, clarifying the structure-activity relationships for this series of derivatives and indicating the pharmacophoric character of the N-acylhydrazone moiety for its biological profile.
Keywords: Bioactive N-acylhydrazone derivatives, antiinflammatory, analgesic and antithrombotic properties, molecular hybridization and bioisosterism in drug design
Current Medicinal Chemistry
Title: Medicinal Chemistry of N-Acylhydrazones: New Lead-Compounds of Analgesic, Antiinflammatory and Antithrombotic Drugs
Volume: 13 Issue: 2
Author(s): Carlos A.M. Fraga and Eliezer J. Barreiro
Affiliation:
Keywords: Bioactive N-acylhydrazone derivatives, antiinflammatory, analgesic and antithrombotic properties, molecular hybridization and bioisosterism in drug design
Abstract: In this article we provide an overview on the medicinal chemistry of new bioactive N-acylhydrazone (NAH) derivatives designed through the structural optimization of N-arylhydrazone precursors, originally planned by molecular hybridization of two known 5-lipoxygenase inhibitors, i.e. CBS-1108 and BW-755c. The analgesic, antiedematogenic and platelet anti-aggregating profile of several isosteric NAH compounds was investigated by using classical in vivo and ex-vivo pharmacological assays, which allowed the identification of new potent centrally and peripherically-acting analgesic leads, new antiinflammatory agents and new antithrombotic prototypes. During this study, dozens of active NAH compounds were discovered, clarifying the structure-activity relationships for this series of derivatives and indicating the pharmacophoric character of the N-acylhydrazone moiety for its biological profile.
Export Options
About this article
Cite this article as:
Fraga A.M. Carlos and Barreiro J. Eliezer, Medicinal Chemistry of N-Acylhydrazones: New Lead-Compounds of Analgesic, Antiinflammatory and Antithrombotic Drugs, Current Medicinal Chemistry 2006; 13 (2) . https://dx.doi.org/10.2174/092986706775197881
DOI https://dx.doi.org/10.2174/092986706775197881 |
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
![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
- Announcements
Related Articles
-
Third and Fourth Generation Fluoroquinolone Antibacterials: A Systematic Review of Safety and Toxicity Profiles
Current Drug Safety Metal-Organic Compounds as Anticancer Agents: Versatile Building Blocks for Selective Action on G-quadruplexes
Current Medicinal Chemistry Multi-Target-Directed Ligands and other Therapeutic Strategies in the Search of a Real Solution for Alzheimer’s Disease
Current Neuropharmacology Discovery of Small Molecules that Target Autophagy for Cancer Treatment
Current Medicinal Chemistry Catechol-O-Methyltransferase and Alzheimer's Disease: A Review of Biological and Genetic Findings
CNS & Neurological Disorders - Drug Targets Arylurea Derivatives: A Class of Potential Cancer Targeting Agents
Current Topics in Medicinal Chemistry Apoptosis in the Homeostasis of the Immune System and in Human Immune Mediated Diseases
Current Pharmaceutical Design Antioxidative Properties of Flavonoids
Current Organic Chemistry Biodegradable Stimuli-Responsive Polymeric Micelles for Treatment of Malignancy
Current Pharmaceutical Biotechnology Factors Promoting Tamoxifen Resistance in Breast Cancer via Stimulating Breast Cancer Stem Cell Expansion
Current Medicinal Chemistry Vitamin D and Vascular Disease
Current Vascular Pharmacology Anti-Angiogenic Agents in Pancreatic Cancer: A Review
Anti-Cancer Agents in Medicinal Chemistry Evidences for iNOS Expression and Nitric Oxide Production in the Human Macrophages
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Exploration of the Medicinal Peptide Space
Protein & Peptide Letters Hypertension in China: Past, Present, and Future
Current Hypertension Reviews Phytochemicals to Prevent Inflammation and Allergy
Recent Patents on Inflammation & Allergy Drug Discovery The Updated Role of Oxidative Stress in Subarachnoid Hemorrhage
Current Drug Delivery High-Throughput Structural Biology in Drug Discovery: Protein Kinases
Current Pharmaceutical Design Tacrine Derivatives and Alzheimers Disease
Current Medicinal Chemistry Intracellular Signaling Pathways Modulated by Phenolic Compounds: Application for New Anti-Inflammatory Drugs Discovery
Current Medicinal Chemistry