First and second generations of COX-2 selective inhibitors.
The identification and characterization of the inducible form of cyclooxygenases (COX-2) stimulated the investigations to develop efficient, non-steroidal anti-inflammatory drugs (NSAIDs) with reduced side effects (essentially gastro-intestinal toxicity) compared to classical NSAIDs. This review focuses on the chemical and pharmacological properties (pre-clinical data) of marketed COX-2 inhibitors.
de Leval
Xavier
X
Natural and Synthetic Drugs Research Centre, Laboratory of Medicinal Chemistry, University of Liège, 1 av. de l'Hôpital, tour 4(+5) Sart-Tilman, B-4000 Liège, Belgium. xdeleval@ulg.ac.be
Julémont
Fabien
F
Benoit
Valérie
V
Frederich
Michel
M
Pirotte
Bernard
B
Dogné
Jean-Michel
JM
D000068579:Celecoxib; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D000077613:Etoricoxib; D005767:Gastrointestinal Diseases / Q000139:chemically induced; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D007555:Isoxazoles / Q000737:chemistry / Q000494:pharmacology; D007783:Lactones / Q000737:chemistry / Q000494:pharmacology; D008565:Membrane Proteins; D011451:Prostaglandin-Endoperoxide Synthases; D011720:Pyrazoles; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology; D013450:Sulfones / Q000737:chemistry / Q000494:pharmacology; D000096926:Benzenesulfonamides
D000068579:Celecoxib; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D000077613:Etoricoxib; D007527:Isoenzymes; D007555:Isoxazoles; D007783:Lactones; D008565:Membrane Proteins; D011451:Prostaglandin-Endoperoxide Synthases; D011720:Pyrazoles; D011725:Pyridines; D013449:Sulfonamides; D013450:Sulfones; C116926:rofecoxib; C406224:valdecoxib; D000096926:Benzenesulfonamides; C409945:parecoxib; C496540:PTGS2 protein, human; C012655:nimesulide