Pal, Manojit published the artcileSynthesis and Cyclooxygenase-2 Inhibiting Property of 1,5-Diarylpyrazoles with Substituted Benzenesulfonamide Moiety as Pharmacophore: Preparation of Sodium Salt for Injectable Formulation, Safety of 4-Fluoro-2-methylbenzenesulfonamide, the publication is Journal of Medicinal Chemistry (2003), 46(19), 3975-3984, database is CAplus and MEDLINE.
A series of 1,5-diarylpyrazoles having a substituted benzenesulfonamide moiety as pharmacophore, e.g. (I; Ar = 2 or 3-fluoro-4-sulfamoylphenyl, 3-methyl-4-sulfamoylphenyl; R = OMe, SMe) and (II; R1 = 4-methoxyphenyl, 4-methylthiophenyl, 4-fluorophenyl; R2= propanoyl, butyryl) was synthesized and evaluated for cyclooxygenase (COX-1/COX-2) inhibitory activities. Through SAR and mol. modeling, it was found that fluorine substitution on the benzenesulfonamide moiety along with an electron-donating group at the 4-position of the 5-aryl ring yielded selectivity as well as potency for COX-2 inhibition in vitro. Among such compounds 3-fluoro-4-[5-(4-methoxyphenyl)-3-trifluoromethyl-1H-1-pyrazolyl]-1-benzenesulfonamide 3 displayed interesting pharmacokinetic properties along with antiinflammatory activity in vivo. Among the sodium salts tested in vivo, 10, the propionyl analog of 3, showed excellent antiinflammatory activity and therefore represents a new lead structure for the development of injectable COX-2 specific inhibitors.
Journal of Medicinal Chemistry published new progress about 489-17-8. 489-17-8 belongs to amides-buliding-blocks, auxiliary class Fluoride,Sulfamide,Amine,Benzene, name is 4-Fluoro-2-methylbenzenesulfonamide, and the molecular formula is C7H8FNO2S, Safety of 4-Fluoro-2-methylbenzenesulfonamide.
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