Abstract
Non-steroidal anti-inflammatory drugs (NSAIDs) are an important class of therapeutics, incorporate a heterocyclic core in their molecular structure and are used for the alleviation of pain and inflammation associated with several pathological conditions. NSAIDs exert anti-inflammatory effects by inhibiting cyclooxygenase enzymes (COXs) which, are useful in the synthesis of prostanoids generated from arachidonic acid. Selective COX-II inhibitors, compared to nonselective inhibitors exhibit reduced gastrointestinal, ulceration and renal side effects. In general, COX-II inhibitors incorporate a five or six-membered heterocyclic motif with built-in sulfonamide or methylsulfonate moiety. Celecoxib, a selective COX-II inhibitor drug, commercialized by Pfizer is applied in the treatment of rheumatoid arthritis, osteoarthritis, and painful menstruation related symptoms. The current review provides a discussion on the methodologies used to construct celecoxib/celebrex® and structural analogs.
Keywords: Celecoxib, Celebrex®, Pyrazoles, Heterocycles, COX, Cycloadditions, Couplings, and Condensations
Current Organic Chemistry
Title:Synthesis of Celecoxib and Structural Analogs- A Review
Volume: 16 Issue: 11
Author(s): Sureshbabu Dadiboyena and Ashton T. Hamme II
Affiliation:
Keywords: Celecoxib, Celebrex®, Pyrazoles, Heterocycles, COX, Cycloadditions, Couplings, and Condensations
Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) are an important class of therapeutics, incorporate a heterocyclic core in their molecular structure and are used for the alleviation of pain and inflammation associated with several pathological conditions. NSAIDs exert anti-inflammatory effects by inhibiting cyclooxygenase enzymes (COXs) which, are useful in the synthesis of prostanoids generated from arachidonic acid. Selective COX-II inhibitors, compared to nonselective inhibitors exhibit reduced gastrointestinal, ulceration and renal side effects. In general, COX-II inhibitors incorporate a five or six-membered heterocyclic motif with built-in sulfonamide or methylsulfonate moiety. Celecoxib, a selective COX-II inhibitor drug, commercialized by Pfizer is applied in the treatment of rheumatoid arthritis, osteoarthritis, and painful menstruation related symptoms. The current review provides a discussion on the methodologies used to construct celecoxib/celebrex® and structural analogs.
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Cite this article as:
Dadiboyena Sureshbabu and T. Hamme II Ashton, Synthesis of Celecoxib and Structural Analogs- A Review, Current Organic Chemistry 2012; 16 (11) . https://dx.doi.org/10.2174/138527212800672664
DOI https://dx.doi.org/10.2174/138527212800672664 |
Print ISSN 1385-2728 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5348 |
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