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Cyclooxygenase-2 inhibitors

2001
Publisher Summary This chapter deals with aspects of the discovery and development of Cyclooxygenase-2 (Cox-2) inhibitors, which, in the case of rofecoxib, resulted from efforts that were initiated in July of 1992 and culminated in the launch of the drug in the United States in June of 1999. Nonsteroidal antiinflammatory drugs (NSAIDs) have long been
A S, Nies, M J, Gresser
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Cyclooxygenase Inhibitors

2013
Cyclooxygenase (COX) inhibitors are widely used to relieve musculoskeletal pain. COX inhibitors are a group of heterogenous substances including non-steroidal anti-inflammatory drugs (NSAIDs) and paracetamol (acetaminophen). Moreover, various selective cyclooxygenase-2 (COX-2) inhibitors with improved gastrointestinal tolerability as compared with ...
Burkhard Hinz, Kay Brune
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Cyclooxygenase-2 Inhibitors

Current Pharmaceutical Design, 1995
Prostaglandins are synthesized by the enzyme cyclooxygenase (COX), which is the target for nonsteroidal anti-inflammatory drugs (NSAIDs). Recently a second form of COX was discovered (COX-2) that is induced by inflammatory stimuli. The identification of an inducible form of COX led to the hypothesis that COX-2 is responsible for inflammatory ...
David B. Reitz, Peter C. Isakson
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Cyclooxygenase-2 selective inhibitors

Drugs of Today, 1999
The identification of two cyclooxygenase (COX) enzymes has been a tremendous advance in understanding the role of prostaglandins in inflammation and the actions of nonsteroidal antiinflammatory drugs (NSAIDs). COX-1 activity appears to be related to "constitutive" or "housekeeping" functions in the gastric mucosa, kidney and platelets.
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Selective Cyclooxygenase Inhibitors: Current Status

Current Drug Discovery Technologies, 2014
For ages aspirin has established its value as an analgesic, anti-inflammatory drug, but in 1938, it was found to be a causative factor of gastric inflammation (ulcer). Later discovered non-steroidal anti-inflammatory drugs (NSAIDs) were found effective as aspirin but failed to overcome the goal of safer aspirin.
Ravindran, Nandakishore   +3 more
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Enantiospecific, selective cyclooxygenase-2 inhibitors

Bioorganic & Medicinal Chemistry Letters, 2002
Cyclooxygenase inhibition studies with novel indomethacin alkanolamides demonstrate the potential for dramatic differences in inhibitor properties conferred by subtle structural modifications. The transformation of non-selective alpha-(S)-substituted indomethacin ethanolamides to potent, COX-2 selective inhibitors by simple stereocenter inversion ...
Kevin R, Kozak   +3 more
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[Cyclooxygenase inhibitors].

Presse medicale (Paris, France : 1983), 2001
DISTINCT EFFECTS: Since the discovery of the two isoforms of COX, the therapeutic effects of nonsteroidal antiinflammatory drugs (NSAID) can be distinguished from their adverse effects linked to the inhibition of the constitutional form via selective inhibition of the inducible form.
P, Eschwège   +8 more
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Dual Carbonic Anhydrase - Cyclooxygenase-2 Inhibitors

Current Topics in Medicinal Chemistry, 2007
Cyclooxygenase is a key enzyme responsible for metabolisation of arachidonic acid into prostaglandins and thromboxane. This enzyme is the target of non steroidal anti-inflammatory drugs (NSAIDs), used against inflammation and pain. The inducible COX-2 was associated with inflammatory conditions, whereas the constitutive form (COX-1) was responsible for
J. Dogné   +4 more
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Cyclooxygenase-2 Inhibitor Celecoxib:

Southern Medical Journal, 2000
Gastrointestinal side effects from nonsteroidal anti-inflammatory drugs (NSAIDs) result mainly from inhibition of the enzyme cyclooxygenase (COX)-1; it is responsible for the synthesis of prostaglandin E2, which leads to increased mucosal blood flow, increased bicarbonate secretion, and mucus production, thus protecting the gastrointestinal mucosa.
J D, Linder   +3 more
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Cyclooxygenase inhibitors: any reservations?

Internal Medicine Journal, 2001
AbstractThe discovery of two cyclooxygenase isozymes, constitutive COX‐1 and inducible COX‐2, has resulted in the rapid development of selective inhibitors of COX‐2, such as celecoxib and rofecoxib. Compared with traditional non‐steroidal anti‐inflammatory drug agents, use of COX‐2 selective inhibitors is associated with decreased incidence of adverse ...
Penglis, P., James, M., Cleland, L.
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