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Recent Advances in Inducible Cyclooxygenase (COX-2) Inhibition

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Abstract:

Cyclooxygenase is the key enzyme in the biosynthesis of prostanoids, biologically active substances that are involved in several physio- logical processes but also in pathological conditions such as inflammation. Since ten years now, it is well known that this enzyme exists under two forms: a constitutive (COX-1) and an inducible form (COX-2). Both enzymes are sensitive to inhibition by conventional nonsteroidal anti-inflammatory drugs (NSAIDs). Observations that COX-1, involved in several homeostatic processes, played a housekeeping role while COX-2 expression was associated with inflammation and other pathologies such as cancer proliferation have led to the development of COX-2 selective inhibitors in order to reduce the classical side-effects, of which gastric irritation is the most common, associated with the use of conventional NSAIDs.

Keywords: COD-2; COX-1; COX-2 inhibitors; Cyclooxygenase (COX-2) Inhibition; Cyclooxygenase 1; Cyclooxygenase 2; Di-tert-butylphenols; Diaryl-substituted cycles; Furans; Inflammation; Methanesulfonanilide inhibitors; Nonsteroidal anti-inflammatory drugs (NSAIDs); Oxazoles and Isoxazoles; Prostanoids; Pyrazoles; Pyrroles; Thiophenes

Document Type: Review Article

DOI: http://dx.doi.org/10.2174/0929867003374417

Publication date: October 1, 2000

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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