By Regina M. Botting, Jack H. Botting (auth.), Michel Pairet, Joanne van Ryn (eds.)
COX-2 inhibitors are vital medicines with analgesic and anti inflammatory results. the invention of COX-2, the evolution of drug improvement during this box and the consequences of those advancements in sufferer remedy are subject matters of this quantity. This booklet offers either pre-clinical and scientific info and is critical for clinicians drawn to the newest information regarding this category of gear, for researchers and for college kids within the field.
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Additional info for COX-2 Inhibitors
This binding mode of APHS contrasts with aspirin in which the carboxylate moiety is involved in electrostatic interactions with the positively charged Arg120 residue in the mouth of the active site . Whether these differences in binding are also responsible for the COX-2 selectivity of APHS remain unclear. Di-tert-butylphenols and dihydrobenzofurans Certain di-tert-butylphenolic analogs containing five-membered heterocyclic rings para to the phenolic OH group were recently disclosed as a novel class of potent and selective COX-2 inhibitors [140-142].
Activity as a function of cyclooxygenase-2 inhibition. J Med Chern 38: 3895-3901 62 Bertenshaw SR, Collins PW, Penning TD, Reitz DB, Rogers RS (1994) Novel 3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents. GD Searle & Co PCT W09415932. 63 Ducharme Y, Gauthier 1Y, Prasit P, Leblanc y, Wang Z, Leger S, Therien M (1995) Phenyl heterocycles as COX-2 inhibitors. Merck Frosst Canada Inc US5474995. 64 Dube D, Brideau C, Deschenes D, Fortin R, Friesen RW, Gordon R, Girard y, Riendeau D, Savoie C, Chan CC (1999) 2-heterosubstituted-3-(4-methylsulfonyl) phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors.
Kalgutkar ArzneirnittelJorschung 16: 87-89 25 Brown K, Cavalla JF, Green D, Wilson AB (1968) Diaryloxazole and diarylthiazolealkanoic acids: two novel series of non-steroidal anti-inflammatory agents. Nature 219: 164 26 Rosenthale ME, Begany AJ, Dervinis A, Malis JL, Shriver DA, Datko SL, Gluckman MI (1974) Anti-inflammatory properties of 4,5-diphenyl-2-oxazolepropionic acid (oxaprozin). Agents Actions 4: 151-159 27 Szmuszkovicz J, Glenn EM, Heinzelman RV, Hester JB Jr, Youngdale GA (1966) Synthesis and antiinflammatory activity of 2,3-bis(p-methoxyphenyl)indole and related compounds.
COX-2 Inhibitors by Regina M. Botting, Jack H. Botting (auth.), Michel Pairet, Joanne van Ryn (eds.)