Novel Synthesis of 3,4-Diarylisoxazole Analogues of Valdecoxib: Reversal Cyclooxygenase-2 Selectivity by Sulfonamide Group Removal - Di Nunno, Leonardo; Vitale, Paola; Scilimati, Antonio; Tacconelli, Stefania; Patrignani, Paola (Journal of medicinal chemistry, 2004)
Keywords: Adult; Biochemistry - methods; Biological and medical sciences; Blood - drug effects; Blood - metabolism; Blood Platelets - drug effects; Blood Platelets - enzymology; Bones, joints and connective tissue. Antiinflammatory agents; Chemistry, Medicinal; Cyclooxygenase 1; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Cyclooxygenase Inhibitors - chemical synthesis; Cyclooxygenase Inhibitors - chemistry; Cyclooxygenase Inhibitors - pharmacology; Dinoprostone - metabolism; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical - methods; Female; Humans; Inhibitory Concentration 50; Isoenzymes - antagonists & inhibitors; Isoenzymes - metabolism; Isoxazoles - chemistry; Isoxazoles - pharmacology; Life Sciences & Biomedicine; Lipopolysaccharides - pharmacology; Medical sciences; Membrane Proteins; Monocytes - drug effects; Monocytes - enzymology; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Prostaglandin-Endoperoxide Synthases - metabolism; Science & Technology; Structure-Activity Relationship; Sulfonamides - chemistry; Sulfonamides - pharmacology; Thromboxane B2 - metabolism; RHEUMATOID-ARTHRITIS; INHIBITION; LOW-DOSE ASPIRIN; CHLOROSULFURIC ACID; HEALTHY-SUBJECTS; ACUTE PAIN; BIOCHEMICAL SELECTIVITY; INTESTINAL TUMORIGENESIS; AROMATIC SULFONATION; THICK ASCENDING LIMB; Prostaglandin-endoperoxide synthase; Sulfonamide; Isoxazole derivatives; Enzyme; Cyclooxygenase 2; Enzyme inhibitor; Cyclooxygenase 2 inhibitor; Selectivity; Valdecoxib; In vitro; Dose activity relation; Structure activity relation; Benzenic compound; Oxidoreductases; Chemical synthesis