Nonsteroidal anti-inflammatory drugs selective cyclooxygenase-2 inhibitors

Spilding WM, Reeves MJ, Whelton A. Thromboembolic Cardiovascular Risk Among Arthritis Patients Using Cyclooxygenase-2-Selective Inhibitor or Nonselective Cyclooxygenase Inhibitor Nonsteroidal Anti-inflammatory Drugs. American Journal of... 

Mitchell J A, Akeirasereenont R Thiemermann C et al 1993 Selectivity of nonsteroidal anti-inflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proceedings of the National Academy of Sciences of the USA 90 11693-11697... 

TABLE 33—3. Selected Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) and Cyclooxygenase-2 (COX-2) Inhibitors... 

Nonsteroidal anti-inflammatory drugs (NSAIDs) Standard dosage regimens of aspirin or traditional NSAIDs (e.g., ibuprofen) selective cyclooxygenase-2 (COX-2) inhibitors should be used in patients at risk for upper Gl bleeding use with caution in renal insufficiency... 

Celecoxib (Celebrex) is a selective cyclooxygenase-2 (COX-2) inhibitor prescribed as a nonsteroidal anti-inflammatory drug (NSAID). The Paal-Knorr cyclization was the crucial step in preparing tri-substituted keto-pyrroles as COX-2 inhibitors. Here, the tri-ketone substrates were prepared in situ from phenacyl bromide and 1,3-diketone. ... 

Symbioimine (35) also significantly inhibited cyclooxygenase-2 (COX-2) activity (32%) at 10 pM. Meanwhile, it had only weak inhibitory ability (5%) toward COX-1 at 10 pM [72]. The overexpression of COX-2 has been observed in many kinds of tumors, and its role in carcinogenesis and angiogenesis has been extensively investigated [76,77]. Several COX-2-selective inhibitors, such as rofecoxib, celecoxib, and sulindac, have been developed. Because of its moderate subtype specificity, symbioimine (35) may be useful for the development of new nonsteroid anti-inflammatory drugs (NSAID) to treat COX-associated diseases, such as inflammatory diseases and cancer. 

Celebrex (celecoxib) is a selective cyclooxygenase (COX)-2 inhibitor nonsteroidal anti-inflammatory drug chemically designated as 4- [5-(4-methylphenyl)-3- (trifluoromethyl) -1 -H-pyrazol-1 -yl)benzenesulfon-amide. It is a diaryl-substituted pyrazole with an empirical formula of Cj Hj FjNjO S and a molecular weight of 381.38. The potent anti-inflammatory effects of an original diarylheterocyclic compound, phenylbutazone, directed scientists to pharmacologically manipulate this chemical scaffold. As a result, celecoxib was the first of the coxibs to be introduced in 1999 by Searle/Pharmacia (now part of Pfizer Inc., USA) [1]. 

M. A. Perazella and K. Tray, Selective cyclooxygenase-2 inhibitors a pattern of nephrotoxicity similar to traditional nonsteroidal anti-inflammatory drugs. Am. J. Med., 2001, 111, 64-67. 

The design of selective cyclooxygenase (COX) inhibitors has attracted much interest over the last few years because of the side effects associated with the existing nonsteroidal anti-inflammatory drugs (NSAIDs) which inhibit... 

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