Abstract
Synthesis and biological evaluation of possible prodrugs of COX-2 inhibitors involving sulfonamide and hydroxymethyl groups of 2-hydroxymethyl-4-(5-phenyl-3-trifluoromethyl-pyrazol-1-yl) benzenesulfonamides are described. Out of many options, the sodium salt of N-propionyl sulfonamide demonstrated much improved pharmacological profiles and physicochemical properties suitable for oral as well as parenteral administration.
MeSH terms
-
Acylation
-
Animals
-
Area Under Curve
-
Biological Availability
-
Cyclooxygenase 2 / drug effects*
-
Cyclooxygenase Inhibitors / chemistry
-
Cyclooxygenase Inhibitors / pharmacokinetics
-
Cyclooxygenase Inhibitors / pharmacology*
-
Prodrugs / chemistry
-
Prodrugs / pharmacology*
-
Rats
-
Sulfonamides / chemistry
-
Sulfonamides / pharmacokinetics
-
Sulfonamides / pharmacology*
Substances
-
Cyclooxygenase Inhibitors
-
Prodrugs
-
Sulfonamides
-
Cyclooxygenase 2