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. 2000 Jan 18;97(2):925–930. doi: 10.1073/pnas.97.2.925

Table 2.

SAR studies on the selective COX-2 inhibition by meclofenamic acid amides

graphic file with name pq0203908ts2.jpg

Compound R IC50*
IC50 (COX-1)/ IC50 (COX-2)†
oCOX-1 hCOX-2
Meclofenamic acid OH 0.040 0.050 0.72
24 HNCH3 16.5 5.5 3.0
25 HN(CH2)3Cl 2.4 0.060 40
26 HN(CH2)2OH 0.90 0.60 1.4
27 HN(CH2)2OC6H5 66 0.15 440
28 HNOCH2C6H5 66 1.0 66
29 HNOCH2C6H5(4-NO2) 60 0.20 273
30 HN(CH2)2C6H5 4.0 4.5 0.90
31 HNCH2CO2CH3 1.2 0.070 17
32 HNCH2CO2H 0.30 0.40 0.75
*

IC50 values in μM represent time-dependent COX inhibition and are average values from duplicate experiments. 

†COX-2 selectivity ratio.