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  • Title: Synthesis and biological activity of disubstituted 4,5-polymethylenepyrazoles as selective cyclooxygenase-2 inhibitors.
    Author: Yu JW, Kim HH, Jahng Y.
    Journal: Pharmazie; 2002 May; 57(5):301-5. PubMed ID: 12061251.
    Abstract:
    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.
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