Abstract
Ibuprofen is one of the most popular NSAIDs for the last three decades but also known for its gastrointestinal side effects similar to other NSAIDs. To overcome this problem, we have designed and synthesized ibuprofen - antioxidant (thymol, guaiacol, eugenol, and menthol) hybrids (6-13) with and without spacer as gastro sparing agents. The hybrids have been found to be chemically stable, biolabile and exhibited retention of anti-inflammatory and analgesic activity with significant reduced ulcerogenicity as compared to the ibuprofen and ibuprofen + antioxidant physical mixture. The absence of ulcerogenicity may be attributed to antioxidants and improved physicochemical properties of these hybrid molecules.
Keywords: Ibuprofen, Antioxidants, Ulcerogenicity, Chemical stability.
Medicinal Chemistry
Title:Synthesis and Evaluation of Antioxidant-S-(+)-Ibuprofen Hybrids as Gastro Sparing NSAIDs
Volume: 9 Issue: 7
Author(s): Senthil Chandiran, Sandeep Vyas, Neetika Sharma and Manu Sharma
Affiliation:
Keywords: Ibuprofen, Antioxidants, Ulcerogenicity, Chemical stability.
Abstract: Ibuprofen is one of the most popular NSAIDs for the last three decades but also known for its gastrointestinal side effects similar to other NSAIDs. To overcome this problem, we have designed and synthesized ibuprofen - antioxidant (thymol, guaiacol, eugenol, and menthol) hybrids (6-13) with and without spacer as gastro sparing agents. The hybrids have been found to be chemically stable, biolabile and exhibited retention of anti-inflammatory and analgesic activity with significant reduced ulcerogenicity as compared to the ibuprofen and ibuprofen + antioxidant physical mixture. The absence of ulcerogenicity may be attributed to antioxidants and improved physicochemical properties of these hybrid molecules.
Export Options
About this article
Cite this article as:
Chandiran Senthil, Vyas Sandeep, Sharma Neetika and Sharma Manu, Synthesis and Evaluation of Antioxidant-S-(+)-Ibuprofen Hybrids as Gastro Sparing NSAIDs, Medicinal Chemistry 2013; 9 (7) . https://dx.doi.org/10.2174/1573406411309070015
DOI https://dx.doi.org/10.2174/1573406411309070015 |
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
-
Mechanism of Action of Flavonoids as Anti-inflammatory Agents: A Review
Inflammation & Allergy - Drug Targets (Discontinued) Bioorganic Compounds Produced by the Fungus Monascus and their Use in Health Sciences and Medicine
Mini-Reviews in Organic Chemistry HCV-Related Central and Peripheral Nervous System Demyelinating Disorders
Inflammation & Allergy - Drug Targets (Discontinued) Inflammatory Process as a Determinant Factor for the Degeneration of Substantia Nigra Dopaminergic Neurons: Possible Relevance to the Etiology of Parkinsons Disease
Current Medicinal Chemistry - Central Nervous System Agents Non-Steroidal Anti-Inflammatory Drugs as Anti-Amyloidogenic Compounds
Current Pharmaceutical Design Effects of Melatonin on Peripheral Nerve Regeneration
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery The Role of cMet in Non-Small Cell Lung Cancer Resistant to EGFRInhibitors: Did We Really Find the Target?
Current Drug Targets Cancer Neovascularization and Proinflammatory Microenvironments
Current Cancer Drug Targets Use of Corticosteroids in Critically Ill Septic Patients: A Review of Mechanisms of Adrenal Insufficiency in Sepsis and Treatment
Current Drug Targets The Rabbit as an Experimental and Production Animal: From Genomics to Proteomics
Current Protein & Peptide Science Granulocyte Colony-Stimulating Factor Attenuates Blood-Brain Barrier Damage and Improves Cognitive Function in Spontaneously Hypertensive Rats
CNS & Neurological Disorders - Drug Targets Selective Modulator of Cannabinoid Receptor Type 2 Reduces Memory Impairment and Infarct Size During Cerebral Hypoperfusion and Vascular Dementia
Current Neurovascular Research Targeted Drug Delivery in Brain Tumors-nanochemistry Applications and Advances
Current Topics in Medicinal Chemistry Commentary: Histaminergic Drugs Could be Novel Targets for Neuroprotection in CNS Disorders
CNS & Neurological Disorders - Drug Targets Novel Inhibitors of Inosine Monophosphate Dehydrogenase in Patent Literature of the Last Decade
Recent Patents on Anti-Cancer Drug Discovery Bronchiolitis Care in the Hospital
Reviews on Recent Clinical Trials Current Options and Perspectives in the Treatment of Diabetic Neuropathy
Current Pharmaceutical Design Targeted Therapies in Solid Tumours: Pinpointing the Tumours Achilles Heel
Current Pharmaceutical Design Inflammation and Immunology of the Vitreoretinal Compartment
Inflammation & Allergy - Drug Targets (Discontinued) Characteristics of Brain Tumor Stem Cells and the Rationale for Applying Tyrosine Kinase Inhibitors as Potential Targeting Agents
Recent Patents on Regenerative Medicine