Design of ketoprofen derivatives linked to natural antioxidants.
Journal name: World Journal of Pharmaceutical Research
Original article title: Design and synthesis of new derivatives of ketoprofen linked to natural antioxidants (thymol, menthol & guaiacol) as possible mutual prodrugs
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Dhurgham Q. Shaheed, Ahmed Kareem Hussein Mubarak, Ammar Abdul Aziz libeg, Hayder Kadhium Abbas, Mohammed Dakhil ALRekabi, Ahmed Hashim Husssein
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Design and synthesis of new derivatives of ketoprofen linked to natural antioxidants (thymol, menthol & guaiacol) as possible mutual prodrugs
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
The study focuses on the design and synthesis of new derivatives of the non-steroidal anti-inflammatory drug (NSAID) ketoprofen linked to natural antioxidants, namely thymol, menthol, and guaiacol. These novel compounds are proposed as mutual prodrugs, aiming to achieve enhanced anti-inflammatory activity while minimizing the ulcerogenic side effects typically associated with NSAID therapy. Chronic use of NSAIDs is often limited by gastrointestinal complications, which have been attributed to the generation of reactive oxygen species (ROS) and the direct irritation caused by these medications.
Impact of Reactive Oxygen Species on Gastrointestinal Health
One critical concept presented in the study pertains to the role of reactive oxygen species (ROS) in inducing gastric mucosal lesions associated with NSAID use. The generation of ROS has been established as a significant contributor to the development of gastrointestinal ulcers during NSAID therapy. By co-administering NSAIDs with antioxidants, it is believed that the harmful effects of ROS can be mitigated, thereby reducing the risk of ulceration and improving overall gastrointestinal safety in patients using these medications. This approach aims to combine the therapeutic benefits of NSAIDs with the protective effects of natural antioxidants.
The Role of Natural Antioxidants
Another important concept is the incorporation of natural antioxidants such as thymol, menthol, and guaiacol into the design of mutual prodrugs. These compounds are known for their strong antioxidant properties and potential to scavenge free radicals. By conjugating these antioxidants with ketoprofen, the researchers aim to enhance the overall therapeutic efficacy while counteracting the adverse side effects linked to prolonged NSAID use. This innovative approach highlights the value of utilizing naturally occurring compounds in drug formulation to improve the safety and effectiveness of established therapies.
Synthesis and Characterization of New Compounds
The synthesis of ketoprofen derivatives involves a chemical reaction with antioxidants wherein ketoprofen is treated with dicyclohexylcarbodiimide (DCC) and DMAP in dry chloroform. The resulting compounds were then characterized through various analytical techniques, including FT-IR and CHNS microanalysis, to establish their purity and structural integrity. The detailed methodology of synthesis and the physical properties of each compound, including their melting points and yields, were documented, showcasing the systematic approach taken to achieve the target derivatives.
Conclusion
In conclusion, this study presents a pioneering method for creating mutual prodrugs that blend the anti-inflammatory effects of ketoprofen with the protective qualities of natural antioxidants. By addressing the common gastrointestinal side effects associated with NSAID therapy, the designed compounds hold promise for safer and more effective anti-inflammatory treatments. The research underscores the significance of merging pharmaceutical chemistry with natural product chemistry to develop advanced therapeutic agents catering to the needs of patients with chronic inflammatory conditions.
FAQ section (important questions/answers):
What are the main purposes of NSAIDs like ketoprofen?
NSAIDs are primarily used for treating chronic inflammatory diseases such as osteoarthritis and rheumatoid arthritis. They help alleviate pain and inflammation, making them widely prescribed in various medical settings.
What adverse effects are associated with the use of NSAIDs?
NSAIDs can cause gastrointestinal irritation, ulcers, and other side effects. These issues arise from the inhibition of prostaglandins, which protect the gastric mucosa, leading to increased vulnerability to damage.
What is a mutual prodrug in pharmaceutical terms?
A mutual prodrug is a compound formed by linking a drug with another agent, often providing complementary effects. In this study, ketoprofen is linked to natural antioxidants like thymol, menthol, and guaiacol to improve therapeutic effects and reduce side effects.
How were the ketoprofen-antioxidant derivatives synthesized in this study?
The synthesis involved dissolving ketoprofen in dry chloroform, adding dicyclohexylcarbodiimide, and incorporating antioxidants like thymol, menthol, or guaiacol. The mixture was then processed to yield semi-solid products, which were subsequently crystallized.
What are the potential benefits of combining NSAIDs with antioxidants?
Co-administration of NSAIDs with antioxidants could decrease the gastrointestinal side effects associated with NSAID therapy. The antioxidants help neutralize reactive oxygen species, potentially protecting the gastric mucosa from damage.
What methods were used to analyze the synthesized compounds?
The synthesized compounds were analyzed using methods like thin layer chromatography, melting point determination, Fourier Transform Infrared Spectroscopy (FT-IR), and CHNS microanalysis to confirm their identity and purity.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Design of ketoprofen derivatives linked to natural antioxidants.�. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.
1) Drug:
Drug refers to a substance used in the diagnosis, treatment, or prevention of diseases in humans. In this context, Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) that alleviates pain and inflammation, but is also associated with gastrointestinal side effects, necessitating the development of safer derivatives linked with antioxidants.
2) Substance:
Substance denotes a specific physical matter, particularly in a chemical composition context. In this research, various substances like ketoprofen, thymol, menthol, and guaiacol are synthesized to create derivatives aimed at enhancing therapeutic efficacy and reducing side effects, thus contributing to drug development and formulation.
3) Disease:
Disease represents any abnormal condition affecting the body that typically presents with specific symptoms and signs. The study focuses on inflammatory diseases, such as rheumatoid arthritis, and the need for effective pain management while minimizing adverse gastrointestinal effects caused by conventional treatments like NSAIDs.
4) Table:
Table refers to a structured arrangement of data, often used to present research findings. This study includes tables that summarize experimental data such as percent yield, physical properties, melting points, and spectral analysis, providing clear, concise information that aids in the evaluation of synthesized compounds.
5) Study (Studying):
Study signifies a systematic investigation into a scientific question. This research study aims to synthesize new ketoprofen derivatives linked with antioxidants to mitigate side effects associated with NSAIDs. It employs rigorous methodologies to explore the pharmacological properties and safety of these new compounds.
6) Pharmacological:
Pharmacological pertains to the effects of drugs on biological systems. In this research, it is crucial as the study investigates the complementary pharmacological actions of ketoprofen combined with antioxidants, aiming for enhanced therapeutic benefits while reducing ulcerogenic effects associated with standard NSAID therapy.
7) Activity:
Activity refers to the degree to which a drug exerts its effects in the body. The focus here is on the anti-inflammatory activity of ketoprofen and its derivatives, analyzing how these compounds can be effective in treating conditions while minimizing adverse outcomes like gastrointestinal irritation.
8) Ulcer:
Ulcer denotes a sore on a body surface, often resulting from the erosive effects of medication such as NSAIDs. This study concentrates on developing prodrugs that combine NSAIDs with antioxidants, aiming to reduce ulcer formation associated with treatments while maintaining therapeutic efficacy.
9) Rheumatoid arthritis:
Rheumatoid arthritis is a chronic inflammatory disorder affecting joints, leading to pain and disability. In this context, NSAIDs like ketoprofen are commonly used for its treatment; however, their associated gastrointestinal risks necessitate the development of safer variants linked with natural antioxidants.
10) Irritation:
Irritation signifies discomfort or inflammation in tissues, a common side effect of NSAIDs. The research highlights the critical importance of addressing gastrointestinal irritation caused by these medications and emphasizes the potential of synthesized antioxidant derivatives to mitigate these adverse effects.
11) Species:
Species refers to distinct biological classifications. In this study, the generation of reactive oxygen species (ROS) is noted as a factor in NSAID-induced gastric ulceration. Understanding such species is vital to exploring oxidative damage mechanisms related to gastrointestinal complications.
12) Cancer:
Cancer denotes a group of diseases characterized by uncontrolled cell growth. In this context, the research discusses the hypothesized protective effects of NSAIDs against cancer through prostaglandin inhibition. Understanding the relationship between inflamed conditions and cancer risk is critical for therapeutic strategies.
13) Dysmenorrhea (Dysmenorrhoea):
Dysmenorrhea describes painful menstruation, often treated with NSAIDs. Ketoprofen's effectiveness for this condition illustrates its significance as a therapeutic agent; however, the potential for gastrointestinal adverse effects necessitates novel approaches like the mutual prodrug synthesis evaluated in this study.
14) Observation:
Observation refers to the process of closely monitoring and noting phenomena during experiments. This study relies on careful observation of synthesized compounds' properties and behaviors to draw conclusions on their effectiveness, safety, and potential for clinical use in treating inflammatory disorders.
15) Discussion:
Discussion involves analyzing and interpreting the results obtained from research. In this study, the discussion evaluates the synthesis outcomes, the effectiveness of the derivatives in enhancing anti-inflammatory actions, and their safety profiles compared to traditional NSAIDs, informing future therapeutic applications.
16) Company:
Company signifies a business entity. The chemical companies mentioned in the study provide the necessary reagents and materials for research. Their role is vital, as the quality and source of chemicals significantly affect the synthesis and research outcomes.
17) Purity:
Purity indicates the absence of contaminants in a substance. In this study, assessing the purity of the synthesized ketoprofen derivatives is crucial for ensuring their safety and efficacy in potential therapeutic applications, as impurities may lead to unwanted side effects.
18) Nature:
Nature refers to the inherent qualities of substances or phenomenon. In the study, natural antioxidants (thymol, menthol, guaiacol) are explored for their properties, indicating an ongoing interest in utilizing naturally derived compounds to enhance the safety and efficacy of conventional pharmaceutical agents.
19) Fever:
Fever is a common symptom of inflammation and infection, often treated with NSAIDs like ketoprofen. This study acknowledges the dual role of NSAIDs in alleviating pain and reducing fever while seeking to minimize their gastrointestinal side effects through innovative drug design.
20) Fainting (Fainted):
Faint refers to a light or weak quality. In this study, the physical appearance described as 'faint yellow semisolid' characterizes one of the synthesized compounds, providing insight into the compound's formulation and aiding in its categorization and further analysis.
21) Cina:
China is mentioned as the source of ketoprofen in this study. The geographical significance highlights the global nature of pharmaceutical supply chains, as well as the collaborations that can occur in the context of drug development and ingredient sourcing in research.
22) Pain:
Pain is the primary indication for NSAID use and a common symptom managed in various inflammatory conditions. Ketoprofen's role in pain relief underscores the importance of continuing to innovate around safer formulations to treat pain effectively without adverse gastrointestinal effects.
23) Life:
Life encompasses the biological processes and health conditions that pharmaceuticals aim to improve. This study strives to enhance the quality of life for individuals suffering from inflammatory diseases by developing novel medications that reduce side effects while maintaining effectiveness in pain management.
Other Science Concepts:
Discover the significance of concepts within the article: �Design of ketoprofen derivatives linked to natural antioxidants.�. Further sources in the context of Science might help you critically compare this page with similair documents:
Gastrointestinal Tract, Antioxidant activity, Oxidative stress, Reactive oxygen species, Reactive oxygen species (ROS), Non-steroidal anti-inflammatory drugs (NSAIDs), Prostaglandin synthesis, Melting point, Elemental analysis, Chronic inflammatory disease, Chemical Entity, Cox inhibitor, Pharmaceutical dosage form, Gastrointestinal tract (GIT), Natural antioxidant, Phenolic compound, Anti-inflammatory drug, Therapeutic advantage, Dosage level, Phenolic antioxidants, C-H stretching vibration.