Synthesis and biological activity of disubstituted 4,5-polymethylenepyrazoles as selective cyclooxygenase-2 inhibitors.

摘要

A series of 1,3- and 2,3-disubstituted 4,5-polymethylenepyrazole derivatives were prepared and their inhibitory activities on cyclooxygenase-2 were evaluated. Among the compounds prepared, 1,3-isomer, 3-cyclohexyl-l-(4-fluorophenyl) 4,5-trimethylenepyra-zole (5be) showed the most potent (IC50 = 0.008 microM) inhibitory activity with little selectivity (13-fold) on cyclooxygenase-2.