piroxicam and Osteoarthritis

piroxicam has been researched along with Osteoarthritis* in 2 studies

Other Studies

2 other study(ies) available for piroxicam and Osteoarthritis

Article	Year
New quaternary ammonium oxicam derivatives: synthesis and in vitro antiosteoarthritis evaluation. European journal of medicinal chemistry, 2010, Volume: 45, Issue:1 A series of new oxicam derivatives bearing a quaternary ammonium (QA) moiety was synthesized and evaluated in vitro for antiosteoarthritis properties. Propyltrimethyl ammonium 3 and propyldiethylmethyl ammonium 11 stimulated aggrecan expression and mitigated the inhibitory action of IL-1. QA derivative 3 also increased TGF-beta2 and type II receptor expression. These results suggest that such derivatives may not only inhibit the osteoarthritis degradation process but also stimulate its regeneration. QA derivatives 3 and 11 offer potential for developing new therapeutic approaches to osteoarthritis treatment. Topics: Aggrecans; Animals; Cartilage, Articular; Cattle; Cells, Cultured; Chondrocytes; Gene Expression Regulation; Osteoarthritis; Quaternary Ammonium Compounds; Receptors, Transforming Growth Factor beta; Transforming Growth Factor beta	2010
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib). Journal of medicinal chemistry, 1997, Apr-25, Volume: 40, Issue:9 A series of sulfonamide-containing 1,5-diarylpyrazole derivatives were prepared and evaluated for their ability to block cyclooxygenase-2 (COX-2) in vitro and in vivo. Extensive structure-activity relationship (SAR) work was carried out within this series, and a number of potent and selective inhibitors of COX-2 were identified. Since an early structural lead (1f, SC-236) exhibited an unacceptably long plasma half-life, a number of pyrazole analogs containing potential metabolic sites were evaluated further in vivo in an effort to identify compounds with acceptable pharmacokinetic profiles. This work led to the identification of 1i (4-[5-(4-methylphenyl)-3-(trifluoromethyl)- H-pyrazol-1-yl]benzenesulfonamide, SC-58635, celecoxib), which is currently in phase III clinical trials for the treatment of rheumatoid arthritis and osteoarthritis. Topics: Animals; Arthritis, Experimental; Arthritis, Rheumatoid; Carrageenan; Celecoxib; Cyclooxygenase 1; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Cyclooxygenase Inhibitors; Hyperalgesia; Isoenzymes; Magnetic Resonance Spectroscopy; Male; Membrane Proteins; Molecular Structure; Osteoarthritis; Prostaglandin-Endoperoxide Synthases; Pyrazoles; Rats; Rats, Inbred Lew; Rats, Sprague-Dawley; Structure-Activity Relationship; Sulfonamides	1997

Article

Year

New quaternary ammonium oxicam derivatives: synthesis and in vitro antiosteoarthritis evaluation.

European journal of medicinal chemistry, 2010, Volume: 45, Issue:1

A series of new oxicam derivatives bearing a quaternary ammonium (QA) moiety was synthesized and evaluated in vitro for antiosteoarthritis properties. Propyltrimethyl ammonium 3 and propyldiethylmethyl ammonium 11 stimulated aggrecan expression and mitigated the inhibitory action of IL-1. QA derivative 3 also increased TGF-beta2 and type II receptor expression. These results suggest that such derivatives may not only inhibit the osteoarthritis degradation process but also stimulate its regeneration. QA derivatives 3 and 11 offer potential for developing new therapeutic approaches to osteoarthritis treatment.

Topics: Aggrecans; Animals; Cartilage, Articular; Cattle; Cells, Cultured; Chondrocytes; Gene Expression Regulation; Osteoarthritis; Quaternary Ammonium Compounds; Receptors, Transforming Growth Factor beta; Transforming Growth Factor beta

2010

Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).

Journal of medicinal chemistry, 1997, Apr-25, Volume: 40, Issue:9

A series of sulfonamide-containing 1,5-diarylpyrazole derivatives were prepared and evaluated for their ability to block cyclooxygenase-2 (COX-2) in vitro and in vivo. Extensive structure-activity relationship (SAR) work was carried out within this series, and a number of potent and selective inhibitors of COX-2 were identified. Since an early structural lead (1f, SC-236) exhibited an unacceptably long plasma half-life, a number of pyrazole analogs containing potential metabolic sites were evaluated further in vivo in an effort to identify compounds with acceptable pharmacokinetic profiles. This work led to the identification of 1i (4-[5-(4-methylphenyl)-3-(trifluoromethyl)- H-pyrazol-1-yl]benzenesulfonamide, SC-58635, celecoxib), which is currently in phase III clinical trials for the treatment of rheumatoid arthritis and osteoarthritis.

Topics: Animals; Arthritis, Experimental; Arthritis, Rheumatoid; Carrageenan; Celecoxib; Cyclooxygenase 1; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Cyclooxygenase Inhibitors; Hyperalgesia; Isoenzymes; Magnetic Resonance Spectroscopy; Male; Membrane Proteins; Molecular Structure; Osteoarthritis; Prostaglandin-Endoperoxide Synthases; Pyrazoles; Rats; Rats, Inbred Lew; Rats, Sprague-Dawley; Structure-Activity Relationship; Sulfonamides

1997