Abstract
Taking into account that compounds bearing a thiazolyl, pyridyl and indolyl, moieties possess a wide spectrum of biological activities which is related to their capacity to transfer electrons and to scavenge reactive oxygen species (ROS), we synthesized some new heterocyclic aryl acetic acids and the corresponding acetohydroxamic acids and we explored their ability to inhibit soybean lipoxygenase, to present antioxidant and anti-inflammatory activities as well as to present serine proteases inhibition. The compounds were found to strongly inhibit lipid peroxidation. and to decrease in vivo the carrageenin induced rat paw edema (28-56%). Compound 1i possesses the highest decrease 56%, in vivo. The tested derivatives presented interesting inhibitory activity on soybean lipoxygenase. Compound 5ii showed significant in vitro inhibition on trypsin (IC50 87μM). The results are discussed in terms of structural and physicochemical characteristics of the compounds. The structures of the synthesized compounds were confirmed by spectral and elemental analysis. Their lipophilicity is experimentally determined by RPTLC method.
Keywords: Antioxidant agents, anti-inflammatory agents, lipoxygenase inhibitors, serine protease inhibitors, heterocyclic aryl -acetic, hydroxamic acids
Medicinal Chemistry
Title: Heterocyclic Aryl(Phenyl)Acetic Acid and Aryl Acetohydroxamic Acids as Antiinflammatory -Antioxidant Agents and Inhibitors of Lipoxygenase and Serine Proteases
Volume: 3 Issue: 5
Author(s): A. Michaelidou, D. Hadjipavlou-Litina, I. Matsini and E. Tsitsogianni
Affiliation:
Keywords: Antioxidant agents, anti-inflammatory agents, lipoxygenase inhibitors, serine protease inhibitors, heterocyclic aryl -acetic, hydroxamic acids
Abstract: Taking into account that compounds bearing a thiazolyl, pyridyl and indolyl, moieties possess a wide spectrum of biological activities which is related to their capacity to transfer electrons and to scavenge reactive oxygen species (ROS), we synthesized some new heterocyclic aryl acetic acids and the corresponding acetohydroxamic acids and we explored their ability to inhibit soybean lipoxygenase, to present antioxidant and anti-inflammatory activities as well as to present serine proteases inhibition. The compounds were found to strongly inhibit lipid peroxidation. and to decrease in vivo the carrageenin induced rat paw edema (28-56%). Compound 1i possesses the highest decrease 56%, in vivo. The tested derivatives presented interesting inhibitory activity on soybean lipoxygenase. Compound 5ii showed significant in vitro inhibition on trypsin (IC50 87μM). The results are discussed in terms of structural and physicochemical characteristics of the compounds. The structures of the synthesized compounds were confirmed by spectral and elemental analysis. Their lipophilicity is experimentally determined by RPTLC method.
Export Options
About this article
Cite this article as:
Michaelidou A., Hadjipavlou-Litina D., Matsini I. and Tsitsogianni E., Heterocyclic Aryl(Phenyl)Acetic Acid and Aryl Acetohydroxamic Acids as Antiinflammatory -Antioxidant Agents and Inhibitors of Lipoxygenase and Serine Proteases, Medicinal Chemistry 2007; 3 (5) . https://dx.doi.org/10.2174/157340607781745456
DOI https://dx.doi.org/10.2174/157340607781745456 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
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
-
Physical Means of Stratum Corneum Barrier Manipulation to Enhance Transdermal Drug Delivery
Current Drug Delivery The Role of β2-Adrenergic Receptors in Inflammation and Allergy
Current Drug Targets - Inflammation & Allergy Atrial Natriuretic Peptide: Structure, Function, and Physiological Effects: A Narrative Review
Current Cardiology Reviews Oligodendrocyte Development and Myelination in Neurodevelopment: Molecular Mechanisms in Health and Disease
Current Pharmaceutical Design Bortezomib Enhances the Antitumor Effects of Interferon-β Gene Transfer on Melanoma Cells
Anti-Cancer Agents in Medicinal Chemistry Dietary Phytochemicals in Chemoprevention of Cancer
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Delivering RNA Interference to the Mammalian Brain
Current Gene Therapy Cystatin C: An Emerging Biomarker in Cardiovascular Disease
Current Topics in Medicinal Chemistry Effects of Extracellular Vesicles Derived from Mesenchymal Stem/Stromal Cells on Liver Diseases
Current Stem Cell Research & Therapy Regulation by IFN-α/IFN-γ Co-Formulation (HerberPAG<sup>®</sup>) of Genes Involved in Interferon-STAT-Pathways and Apoptosis in U87MG
Current Topics in Medicinal Chemistry Neurological Aspects of Grief
CNS & Neurological Disorders - Drug Targets Therapeutic Monitoring of Immunotherapies in Autoimmune Diseases
Current Pharmaceutical Design Renal COX-2, Cytokines and 20-HETE: Tubular and Vascular Mechanisms
Current Pharmaceutical Design Enhanced Activity of pSTAT-3 Ser-727 in Functional Endothelial Cells Under Calcifying Conditions
Current Chemical Biology Therapeutics Interventions with Anti-Inflammatory Creams in Post Radiation Acute Skin Reactions: A Systematic Review of Most Important Clinical Trials
Recent Patents on Inflammation & Allergy Drug Discovery Ibrutinib: A New Frontier in the Treatment of Chronic Lymphocytic Leukemia by Bruton’s Tyrosine Kinase Inhibition
Cardiovascular & Hematological Agents in Medicinal Chemistry The Promise of Antimicrobial Peptides for Treatment of Human Schistosomiasis
Current Drug Targets Discovery Approaches for Novel Dyslipidemia Drugs
Current Drug Discovery Technologies Targeting the Secretory Pathway for Anti-Inflammatory Drug Development
Current Topics in Medicinal Chemistry Oxidative Stress and Opioids' Toxicity: An Update
Mini-Reviews in Organic Chemistry