Abstract
Non-steroidal anti-inflammatory drugs (NSAIDs) are agents that are used for various properties such as analgesic activity, anti-inflammatory activity, antipyretic activity, etc. But this class of drugs is associated with different side effects such as dyspepsia, gastroduodenal ulcers, gastrointestinal (GI) bleeding and perforation. The prodrug approach is quite beneficial to curb these side effects. Prodrugs are the inactive compounds that, on metabolism get converted into an active metabolite exhibiting desired activities. Commonly used approaches for synthesizing prodrugs are amide, esters, and mutual prodrugs by suppressing the free carboxylic groups responsible for these side effects. In this review, different schemes reported for the synthesis of NSAIDs that are devoid of undesired side effects such as irritation to gastric mucosa, gastrotoxicity, and ulcerogenicity have been compiled. Docking studies and the structure-activity relationship of some compounds are also discussed. The paper shall help the researchers to understand the methods to expedite the synthesis by carrying out substitutions of various groups of the parent compound and establish the mechanism of action of these derivatives of masking the unwanted side effects.
Keywords: NSAIDs, Prodrugs, GI bleeding, GI ulcers, gastroprotective, anti-inflammatory, analgesic.
Mini-Reviews in Medicinal Chemistry
Title:Synthetic Strategies Towards Safer NSAIDs Through Prodrug Approach: A Review
Volume: 21 Issue: 15
Author(s): Komal Gupta, Pooja A Chawla*Deepika Sharma
Affiliation:
- Department of Pharmaceutical Chemistry and Analysis, ISF College of Pharmacy, Moga 142001, Punjab,India
Keywords: NSAIDs, Prodrugs, GI bleeding, GI ulcers, gastroprotective, anti-inflammatory, analgesic.
Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) are agents that are used for various properties such as analgesic activity, anti-inflammatory activity, antipyretic activity, etc. But this class of drugs is associated with different side effects such as dyspepsia, gastroduodenal ulcers, gastrointestinal (GI) bleeding and perforation. The prodrug approach is quite beneficial to curb these side effects. Prodrugs are the inactive compounds that, on metabolism get converted into an active metabolite exhibiting desired activities. Commonly used approaches for synthesizing prodrugs are amide, esters, and mutual prodrugs by suppressing the free carboxylic groups responsible for these side effects. In this review, different schemes reported for the synthesis of NSAIDs that are devoid of undesired side effects such as irritation to gastric mucosa, gastrotoxicity, and ulcerogenicity have been compiled. Docking studies and the structure-activity relationship of some compounds are also discussed. The paper shall help the researchers to understand the methods to expedite the synthesis by carrying out substitutions of various groups of the parent compound and establish the mechanism of action of these derivatives of masking the unwanted side effects.
Export Options
About this article
Cite this article as:
Gupta Komal , Chawla A Pooja *, Sharma Deepika , Synthetic Strategies Towards Safer NSAIDs Through Prodrug Approach: A Review, Mini-Reviews in Medicinal Chemistry 2021; 21 (15) . https://dx.doi.org/10.2174/1389557521666201231140554
DOI https://dx.doi.org/10.2174/1389557521666201231140554 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
-
Astrocytes as a 5-HT2B-Mediated SERT-Independent SSRI Target, Slowly Altering Depression-Associated Genes and Function
Current Signal Transduction Therapy Intracellular Bioinorganic Chemistry and Cross Talk Among Different -Omics
Current Topics in Medicinal Chemistry Obesity and Body Composition in Man and Woman: Associated Diseases and the New Role of Gut Microbiota
Current Medicinal Chemistry Shutting Down the Furnace: Preferential Killing of Cancer Cells with Mitochondrial-Targeting Molecules
Current Medicinal Chemistry Protein Kinase C – Possible Therapeutic Target to Treat Cardiovascular Diseases
Cardiovascular & Hematological Disorders-Drug Targets Cardiac Stem Cell Characteristics in Physiological and Pathological Conditions
Current Pharmaceutical Design Drug-Induced Hypothermia in Stroke Models: Does it Always Protect?
CNS & Neurological Disorders - Drug Targets Valproate and Neuroendocrine Changes in Relation to Women Treated for Epilepsy and Bipolar Disorder: A Review
Current Medicinal Chemistry Physical Function and Exercise in Older Patients with Cardiovascular and Respiratory Conditions
Current Pharmaceutical Design Lipid-Lowering Therapies for Atherosclerosis: Statins, Fibrates, Ezetimibe and PCSK9 Monoclonal Antibodies
Current Medicinal Chemistry Phosphodiesterase 4 Inhibitors in Inflammatory Bowel Disease: A Comprehensive Review
Current Pharmaceutical Design Appraisal of Saxagliptin as Treatment of Type 2 Diabetes
Current Drug Therapy Herbal and Traditional Chinese Medicine for the Treatment of Cardiovascular Complications in Diabetes Mellitus
Current Diabetes Reviews Central Nervous System Circuitry and Peripheral Neural Sympathetic Activity Responsible for Essential Hypertension
Current Neurovascular Research Endothelial Therapy of Atherosclerosis and its Risk Factors
Current Vascular Pharmacology Ability of older people with dementia or cognitive impairment to manage medicine regimens: a narrative review
Current Clinical Pharmacology Molecular Mechanisms in Aging and Current Strategies to Counteract Sarcopenia
Current Aging Science Heart Failure in South America
Current Cardiology Reviews Peroxisome Proliferator-Activated Receptor (PPAR) in Metabolic Syndrome and Type 2 Diabetes Mellitus
Current Diabetes Reviews Molecular and Cellular Mechanisms in the Pathophysiology of Severe Head Injury
Current Pharmaceutical Design