Design, Synthesis, and Evaluation of New Tripeptides as COX-2 Inhibitors
Table 3
Inhibitory activity of compounds synthesized and selectivity against COX-2 over COX-1.
COX-1 (IC50)
COX-2 (IC50)
Ratio
Indometacina
12.16 ± 1.16 μM
35.20 ± 1.41 μM
2.9
Diclofenac
18.23 ± 1.73 μM
23.62 ± 1.97 μM
1.3
FR122047
93.80 ± 6.55 μM
***
>1.066a
Nimesulide
***
231.40 ± 19.84 μM
<0.46a
DuP697
22.61 ± 1.56 μM
126.32 ± 7.41 μM
0.0056
S1
150.33 ± 2.34 μM
94.04 ± 2.59 μM
0.6255
S2
143.21 ± 2.57 μM
120.92 ± 2.33 μM
0.8443
S3
152.44 ± 5.18 μM
94.89 ± 2.12 μM
0.6225
S4
99.32 ± 1.14 μM
80.56 ± 2.14 μM
0.8111
S5
161.43 ± 2.57 μM
100.01 ± 2.33 μM
0.6195
S6
102.31 ± 1.14 μM
91.20 ± 2.41 μM
0.8914
S7
100.33 ± 2.19 μM
88.21 ± 3.01 μM
0.8792
S8
122.48 ± 3.78 μM
91.66 ± 2.98 μM
0.7484
S9
221.57 ± 1.04 μM
68.34 ± 5.43 μM
0.308
S10
99.11 ± 1.55 μM
79.20 ± 2.15 μM
0.7991
E1–E10**
—
—
—
Significant differences between the two means (P < 0.05 or P < 0.01) were determined by one-way analysis of variability (ANOVA) followed by Dunnett's post hoc test.
***No active at 500 μM (the highest concentration tested).
aValue obtained whereas the corresponding IC50 to COX-1 or COX-2 is the highest concentration tested.
**Data not shown.
