Table 2. CXCR1/2 Antagonistic Activity for Compounds B1–B10.

| R1 | CXCR1 IC50 (μM)a | CXCR2 IC50 (μM)a | ratiob | |
|---|---|---|---|---|
| 2 | Ph | 4.7 | 0.006 | 778 |
| B1 | H | >100 | 29.7 | 3 |
| B2 | 4-Cl-Ph | 38.1 | 0.915 | 42 |
| B3 | 3-Cl-Ph | 47.8 | 0.305 | 157 |
| B4 | 2-Cl-Ph | 21.7 | 0.054 | 402 |
| B5 | 4-F-Ph | ∼100 | 2.19 | ∼46 |
| B6 | methyl | >100 | 0.269 | >372 |
| B7 | ethyl | ∼100 | 0.140 | ∼714 |
| B8 | propyl | 14.7 | 0.068 | 216 |
| B9 | n-butyl | 54.6 | 0.043 | 1270 |
| B10 | isobutyl | 41.8 | 0.305 | 137 |
| SCH527123 | 0.16 | 0.01 | 16 |
The IC50 values are an average of triplicate determinations.
Ratio = CXCR1 IC50/CXCR2 IC50.