Prodrugs of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs), More Than Meets the Eye: A Critical Review
Autor: | Amjad M. Qandil |
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Rok vydání: | 2012 |
Předmět: |
Intrinsic activity
NSAIDs medicine.drug_class Phospho-NSAIDs codrug mutual prodrug Nonprescription Drugs Review Pharmacology Cholinergic Antagonists Catalysis Anti-inflammatory lcsh:Chemistry Inorganic Chemistry chemistry.chemical_compound MISCELLANEOUS AGENTS medicine Anticholinergic Animals Humans Prodrugs Physical and Theoretical Chemistry lcsh:QH301-705.5 Molecular Biology Spectroscopy anti-inflammatory Nonsteroidal Codrug Chemistry Anti-Inflammatory Agents Non-Steroidal Organic Chemistry Biological activity General Medicine Prodrug digestive system diseases Computer Science Applications cyclooxygenase NO-NSAIDs lcsh:Biology (General) lcsh:QD1-999 prodrug |
Zdroj: | International Journal of Molecular Sciences, Vol 13, Iss 12, Pp 17244-17274 (2012) International Journal of Molecular Sciences |
ISSN: | 1422-0067 |
DOI: | 10.3390/ijms131217244 |
Popis: | The design and the synthesis of prodrugs for nonsteroidal anti-inflammatory drugs (NSAIDs) have been given much attention by medicinal chemists, especially in the last decade. As a therapeutic group, NSAIDs are among the most widely used prescribed and over the counter (OTC) medications. The rich literature about potential NSAID prodrugs clearly shows a shift from alkyl, aryalkyl or aryl esters with the sole role of masking the carboxylic acid group, to more elaborate conjugates that contain carefully chosen groups to serve specific purposes, such as enhancement of water solubility and dissolution, nitric oxide release, hydrogen sulfide release, antioxidant activity, anticholinergic and acetylcholinesterase inhibitory (AChEI) activity and site-specific targeting and delivery. This review will focus on NSAID prodrugs that have been designed or were, later, found to possess intrinsic pharmacological activity as an intact chemical entity. Such intrinsic activity might augment the anti-inflammatory activity of the NSAID, reduce its side effects or transform the potential therapeutic use from classical anti-inflammatory action to something else. Reports discussed in this review will be those of NO-NSAIDs, anticholinergic and AChEI-NSAIDs, Phospho-NSAIDs and some miscellaneous agents. In most cases, this review will cover literature dealing with these NSAID prodrugs from the year 2006 and later. Older literature will be used when necessary, e.g., to explain the chemical and biological mechanisms of action. |
Databáze: | OpenAIRE |
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