Abstract
In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, new compounds based on a combination of clofibric acid, the active metabolite of clofibrate, and trans-stilbene, chalcone, and other lipophilic groups were synthesized. They were evaluated for PPARα transactivation activity; all branched derivatives showed an increase of the transcriptional activity of receptor compared to the linear ones. Noteworthy, stilbene and benzophenone branched derivatives activated the PPARα better than clofibric acid.
Keywords: PPARs, clofibrate, chalcone, stilbene, transactivation assay.
Medicinal Chemistry
Title:Effect of Stilbene and Chalcone Scaffolds Incorporation in Clofibric Acid on PPARα Agonistic Activity
Volume: 10 Issue: 1
Author(s): Letizia Giampietro, Alessandra D’Angelo, Antonella Giancristofaro, Alessandra Ammazzalorso, Barbara De Filippis, Mauro DiMatteo, Marialuigia Fantacuzzi, Pasquale Linciano, Cristina Maccallini and Rosa Amoroso
Affiliation:
Keywords: PPARs, clofibrate, chalcone, stilbene, transactivation assay.
Abstract: In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, new compounds based on a combination of clofibric acid, the active metabolite of clofibrate, and trans-stilbene, chalcone, and other lipophilic groups were synthesized. They were evaluated for PPARα transactivation activity; all branched derivatives showed an increase of the transcriptional activity of receptor compared to the linear ones. Noteworthy, stilbene and benzophenone branched derivatives activated the PPARα better than clofibric acid.
Export Options
About this article
Cite this article as:
Giampietro Letizia, D’Angelo Alessandra, Giancristofaro Antonella, Ammazzalorso Alessandra, Filippis De Barbara, DiMatteo Mauro, Fantacuzzi Marialuigia, Linciano Pasquale, Maccallini Cristina and Amoroso Rosa, Effect of Stilbene and Chalcone Scaffolds Incorporation in Clofibric Acid on PPARα Agonistic Activity, Medicinal Chemistry 2014; 10 (1) . https://dx.doi.org/10.2174/157340641001131226123613
DOI https://dx.doi.org/10.2174/157340641001131226123613 |
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
-
Immunosuppressive Properties of Mesenchymal Stem Cells: Advances and Applications
Current Molecular Medicine Glucocorticoids and the Cardiovascular System: State of the Art
Current Pharmaceutical Design The Role of White Matter Abnormalities in Treatment-Resistant Depression: A Systematic Review
Current Pharmaceutical Design Non-Alcoholic Fatty Liver Disease in the Metabolic Syndrome
Current Pharmaceutical Design Lysophospholipids: Their Generation, Physiological Role and Detection. Are They Important Disease Markers?
Mini-Reviews in Medicinal Chemistry Endothelial Dysfunction in Morbid Obesity
Current Pharmaceutical Design Recent Advances on 3-Hydroxyflavone Derivatives: Structures and Properties
Mini-Reviews in Medicinal Chemistry Association between ALDH2 Gene Polymorphism and Late-onset Alzheimer Disease: An Up-to-date Meta-analysis
Current Alzheimer Research Safety of Drug Eluting Stents: Current Concerns and Controversies
Current Drug Safety The Interplay of Marine Exposure in Gestational Diabetes
Current Women`s Health Reviews Prebiotic Carbohydrates for Therapeutics
Endocrine, Metabolic & Immune Disorders - Drug Targets Continuous Glucose Monitoring: Physiological and Technological Challenges
Current Diabetes Reviews Modulating Poly (ADP-Ribose) Polymerase Activity: Potential for the Prevention and Therapy of Pathogenic Situations Involving DNA Damage and Oxidative Stress
Current Pharmaceutical Biotechnology 21-Hydroxy-6,19-epoxyprogesterone: A Promising Therapeutic Agent and a Molecular Tool for Deciphering Glucocorticoid Action
Mini-Reviews in Medicinal Chemistry Infant Breast-Feeding and Suppression of Biomarkers of Future Cardiovascular Disease
Current Nutrition & Food Science Anti-Proliferative Activity of Standardized Methanol Extract of Coscinium fenestratum and Its Major Constituent, Berberine, Against Nasopharyngeal Carcinoma Cells
The Natural Products Journal Progesterone: Indications for the Prevention of Preterm Birth
Current Women`s Health Reviews Overactive Bladder Symptoms in Patients with Fibromyalgia: A Systematic Case-Controlled Study
Reviews on Recent Clinical Trials Arterial Stiffness: A Novel Cardiovascular Risk Factor in Kidney Disease Patients
Current Vascular Pharmacology Mechanisms of Cardiovascular Changes in an Experimental Model of Syndrome X and Pharmacological Intervention on the Renin-Angiotensin- System
Current Vascular Pharmacology