Abstract
A series of substituted pyridinylpyrazole (or isoxazole) derivatives were synthesized and evaluated for their anti-inflammatory (AI) activity using formalin-induced paw edema bioassays. Their inhibitory activities of cyclooxygenase-1 and cyclooxygenase-2 (COX-1 and COX-2) were also determined. The analgesic activity of the same compounds was evaluated using rat-tail withdrawal technique. Their antipyretic activity was also evaluated. The results revealed that compounds 4a,b, 6a, 8a, 14c and 15a exhibited significant AI and analgesic activities. Compounds 5a, 6a and 8a displayed good antipyretic activity. Compounds 14c and 15a showed good COX-2 inhibitory activity and weak inhibition of COX-1. Additionally, the most active compounds were shown to have a large safety margin (ALD50 >300-400 mg / Kg) and minimal ulcerogenic potentialities when administered orally at a dose of 300 mg/Kg. Docking studies for 14c and 15a with COX-2 showed good binding profile. Antimicrobial evaluation proved that most of the compounds exhibited distinctive activity against the gram negative bacteria, P. aeruginosa and E coli.
Keywords: Pyridinylpyrazoles, pyridinylisoxazoles, anti-inflammatory activity, analgesic activity, antipyretic activity, antimicrobial activity.
Medicinal Chemistry
Title:Design, Synthesis and Biological Screening of Some Pyridinylpyrazole and Pyridinylisoxazole Derivatives as Potential Anti-inflammatory, Analgesic, Antipyretic and Antimicrobial Agents
Volume: 10 Issue: 3
Author(s): Soad A.M. El-Hawash, Raafat Soliman, Amal M. Youssef, Hanan M.A. Ragab, Perihan A.S. Elzahhar, Ibrahim M. El-Ashmawey, Abeer E. Abdel Wahab and Iman A. Shaat
Affiliation:
Keywords: Pyridinylpyrazoles, pyridinylisoxazoles, anti-inflammatory activity, analgesic activity, antipyretic activity, antimicrobial activity.
Abstract: A series of substituted pyridinylpyrazole (or isoxazole) derivatives were synthesized and evaluated for their anti-inflammatory (AI) activity using formalin-induced paw edema bioassays. Their inhibitory activities of cyclooxygenase-1 and cyclooxygenase-2 (COX-1 and COX-2) were also determined. The analgesic activity of the same compounds was evaluated using rat-tail withdrawal technique. Their antipyretic activity was also evaluated. The results revealed that compounds 4a,b, 6a, 8a, 14c and 15a exhibited significant AI and analgesic activities. Compounds 5a, 6a and 8a displayed good antipyretic activity. Compounds 14c and 15a showed good COX-2 inhibitory activity and weak inhibition of COX-1. Additionally, the most active compounds were shown to have a large safety margin (ALD50 >300-400 mg / Kg) and minimal ulcerogenic potentialities when administered orally at a dose of 300 mg/Kg. Docking studies for 14c and 15a with COX-2 showed good binding profile. Antimicrobial evaluation proved that most of the compounds exhibited distinctive activity against the gram negative bacteria, P. aeruginosa and E coli.
Export Options
About this article
Cite this article as:
El-Hawash A.M. Soad, Soliman Raafat, Youssef M. Amal, Ragab M.A. Hanan, Elzahhar A.S. Perihan, El-Ashmawey M. Ibrahim, Abdel Wahab E. Abeer and Shaat A. Iman, Design, Synthesis and Biological Screening of Some Pyridinylpyrazole and Pyridinylisoxazole Derivatives as Potential Anti-inflammatory, Analgesic, Antipyretic and Antimicrobial Agents, Medicinal Chemistry 2014; 10 (3) . https://dx.doi.org/10.2174/15734064113096660044
DOI https://dx.doi.org/10.2174/15734064113096660044 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...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
Related Articles
-
Therapeutic Strategies Targeting Endothelial Function in Humans:Clinical Implications
Current Vascular Pharmacology The Role of Endothelial Related Circulating Biomarkers in COVID-19. A Systematic Review and Meta-analysis
Current Medicinal Chemistry Recent Advances on Nitric Oxide in the Upper Airways
Current Medicinal Chemistry The Effectiveness of Different Treatment Modalities for the Management of Ocular Injuries Following Sulfur Mustard Exposure
Letters in Drug Design & Discovery Effect of Androgenic and Antiandrogenic Acting Compounds in Macrophage Accumulation and Cell Replication in the Aorta of Oophorectomized Hypercholesterolemic Rabbits
Vascular Disease Prevention (Discontinued) Endothelial Dysfunction and Coronary Artery Spasm
Current Drug Targets - Cardiovascular & Hematological Disorders Endothelial Dysfunction and the Effects of TNF Inhibitors on the Endothelium in Psoriasis and Psoriatic Arthritis: A Systematic Review
Current Pharmaceutical Design Acetaminophen (Paracetamol) and Injury in the Cardiovascular System
Vascular Disease Prevention (Discontinued) Pharmacokinetic Mechanisms for Reduced Toxicity of Irinotecan by Coadministered Thalidomide
Current Drug Metabolism Ghrelin and Motilin in the Gastrointestinal System
Current Pharmaceutical Design Potential Role of Rho-Associated Protein Kinase Inhibitors for Glaucoma Treatment
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Involvement of Orexigenic Peptides in the Mechanism of Gastric Mucosal Integrity and Healing of Chronic Gastric Ulcers
Current Pharmaceutical Design Intracoronary Injection of Drugs to Treat No – Reflow Phenomenon and Microcirculatory Dysfunction
Cardiovascular & Hematological Agents in Medicinal Chemistry Myocardial Infarction. Pathological Relevance and Relationship with Coronary Risk Factors
Current Pharmaceutical Design Anti-platelet Drug-loaded Targeted Technologies for the Effective Treatment of Atherothrombosis
Current Drug Targets Bacterial Conjunctivitis in Childhood: Etiology, Clinical Manifestations, Diagnosis, and Management
Recent Patents on Inflammation & Allergy Drug Discovery Glaucoma and Aging
Current Aging Science The Effect of Serotonin 5-HT2 Receptor Inhibitor on Vasomotor Responses
Vascular Disease Prevention (Discontinued) Smoking and Atherosclerosis: Mechanisms of Disease and New Therapeutic Approaches
Current Medicinal Chemistry On the Biomaterials for Nanostructured Ocular Therapeutics
Current Organic Chemistry