Abstract
In this work we reported the design, synthesis and evaluation of the new diaryl heterocyclic derivatives based on the lead compounds of Rofecoxib and Celecoxib by application of the principle of isosterism. The in vivo pharmacological evaluation of these new compounds lead us to select the compounds (Ia) and (IIc) as a new prototype which a substituent ortho to the methylsulfone or sulfonamide group was introduced for further development, more active that celecoxib at the same mass concentration.
Keywords: NSAIDs, COX-2, Potency, Anti-inflammatory, Analgesic, Synthesis
Letters in Drug Design & Discovery
Title: Design and Synthesis of Novel Diaryl Heterocyclic Derivatives as Selective Cyclooxygenase-2
Volume: 5 Issue: 2
Author(s): S. X. Li, X. D. Deng, F. L. Jiang, Y. J. Zhao, W. S. Xiao, X. Z. Kuang and X. M. Sun
Affiliation:
Keywords: NSAIDs, COX-2, Potency, Anti-inflammatory, Analgesic, Synthesis
Abstract: In this work we reported the design, synthesis and evaluation of the new diaryl heterocyclic derivatives based on the lead compounds of Rofecoxib and Celecoxib by application of the principle of isosterism. The in vivo pharmacological evaluation of these new compounds lead us to select the compounds (Ia) and (IIc) as a new prototype which a substituent ortho to the methylsulfone or sulfonamide group was introduced for further development, more active that celecoxib at the same mass concentration.
Export Options
About this article
Cite this article as:
Li X. S., Deng D. X., Jiang L. F., Zhao J. Y., Xiao S. W., Kuang Z. X. and Sun M. X., Design and Synthesis of Novel Diaryl Heterocyclic Derivatives as Selective Cyclooxygenase-2, Letters in Drug Design & Discovery 2008; 5 (2) . https://dx.doi.org/10.2174/157018008783928517
DOI https://dx.doi.org/10.2174/157018008783928517 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
Related Articles
-
Synergistic Effect of Inhibitors of MMPs and ROS-dependent Modifications of Contractile Proteins on Protection Hearts Subjected to Oxidative Stress
Current Pharmaceutical Design Statins and Portal Hypertension: A New Pharmacological Challenge
Current Vascular Pharmacology Antiviral Activity of Substituted Salicylanilides - A Review
Mini-Reviews in Medicinal Chemistry The Use of DNA Microarray in the Pharmacogenetics of Antidepressants: Guidelines for a Targeted Approach
Current Genomics Editorial [Hot Topic: Influenza Virus Pathogenesis and Drug Targets (Guest Editor: Christopher F. Basler)]
Infectious Disorders - Drug Targets Prevention and Healing of Calcium Signaling Mediated Neuronal Damage on successive Administration of Flavonoid Enriched <i>Pterocarpus Marsupium Roxb</i> in Peripheral Neuropathy Model
Current Bioactive Compounds Differential TNF-Signaling in Chronic Inflammatory Disorders
Current Molecular Medicine ACE2-Ang-(1-7)-Mas Axis in Brain: A Potential Target for Prevention and Treatment of Ischemic Stroke
Current Neuropharmacology Diversity in the Accessory Proteins of SARS-CoV-2, SARS-CoV, and MERS-CoV Betacoronaviruses
Current Protein & Peptide Science Meet Our Editor-in-Chief
Current Psychiatry Reviews Biosimilars: Current Scientific and Regulatory Considerations
Current Clinical Pharmacology The Mechanism in Gastric Cancer Chemoprevention by Allicin
Anti-Cancer Agents in Medicinal Chemistry Signal Transducer and Activator of Transcription 5 (STAT5), a Crucial Regulator of Immune and Cancer Cells
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Systemic Delivery of Nanoformulations of Anti-cancer Drugs with Therapeutic Potency in Animal Models of Cancer
Current Cancer Therapy Reviews The Neurobiological Bases for Development of Pharmacological Treatments of Aggressive Disorders
Current Neuropharmacology Transfersomes: The Ultra-Deformable Carrier System for Non-Invasive Delivery of Drug
Current Drug Delivery Diagnostic and Therapeutic Nanoparticles in Cardiovascular Diseases
Current Pharmaceutical Design Inhibition of Sumoylation Alleviates Oxidative Stress-induced Retinal Pigment Epithelial Cell Senescence and Represses Proinflammatory Gene Expression
Current Molecular Medicine Therapeutic Potential of Natural Products in Parkinson’s Disease
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Towards Retinoid Therapy for Alzheimers Disease
Current Alzheimer Research