Table 3. CXCR1/2 Antagonistic Activity for Compounds C1–C8.
| R1 | CXCR1 IC50 (μM)a | CXCR2 IC50 (μM)a | ratiob | |
|---|---|---|---|---|
| C1 | methyl | >100 | 0.47 | >212 |
| C2 | methyl | >100 | 3.1 | >32 |
| C3 | propyl | 20.3 | 0.029 | 700 |
| C4 | propyl | >100 | 2.8 | >36 |
| C5 | cyclohexyl | 9.1 | 0.01 | 910 |
| C6 | cyclohexyl | ∼100 | 4.0 | ∼25 |
| C7 | benzyl | >100 | 0.098 | >1020 |
| C8 | benzyl | >100 | 25.0 | >4 |
| SCH527123 | 0.16 | 0.01 | 16 |
The IC50 values are an average of triplicate determinations.
Ratio = CXCR1 IC50/CXCR2 IC50.
