183610-69-7Relevant academic research and scientific papers
Synthesis and SAR of a new series of COX-2-selective inhibitors: Pyrazolo[1,5-α]pyrimidines
Almansa,De Arriba,Cavalcanti,Gómez,Miralles,Merlos,García-Rafanell,Forn
, p. 350 - 361 (2007/10/03)
The synthesis and pharmacological activity of a series of bicyclic pyrazolo[1,5-α]pyrimidines as potent and selective cyclooxygenase-2 (COX-2) inhibitors are described. The new compounds were evaluated both in vitro (COX-1 and COX-2 inhibition in human whole blood) and in vivo (carrageenan-induced paw edema and air-pouch model). Modification of the pyrimidine substituents showed that 6,7-disubstitution provided the best activity and led to the identification of 3-(4-fluorophenyl)-6,7-dimethyl-2-(4-methylsulfonylphenyl) pyrazolo[1,5-α]pyrimidine (10f) as one of the most potent and selective COX-2 inhibitor in this series.
