Table 5.
SAR studies using different substitutions.
| Compound No. | R1 | R2 | R3 | R4 | EC50 (μM)a |
|---|---|---|---|---|---|
| 180 | Cl | H | H | Ph | 1.3 |
| 181 | F | H | H | Ph | 0.1 |
| 182 | Br | H | H | Ph | 3.1 |
| 183 | OCF3 | H | H | Ph | 95.6 |
| 184 | OCH3 | H | H | Ph | 2611 |
| 185 | NO2 | H | H | Ph | 2.0 |
| 186 | CF3 | H | H | Ph | 16.6 |
| 187 | H | H | H | Ph | 1.0 |
| 188 | H | H | H | Ph | 1.2 |
| 189 | H | F | H | Ph | 158.8 |
| 190 | F | F | H | Ph | 11.6 |
| 191 | F | H | H | CH3 | 0.1 |
| 192 | F | H | H | CH2CH3 | 6.4 |
| 193 | F | H | H | (CH2)2CH3 | 19.0 |
| 194 | F | H | H | (CH2)3CH3 | 2.1 |
| 195 | F | H | H | CH2(C3H5) | 6.8 |
| 196 | F | H | H | CF3 | 1.0 |
| 197 | F | H | H | 4-Cl-Ph | 2.0 |
| 198 | F | H | H | 4-NO2-Ph | 4.9 |
| 199 | F | H | H | 3,4-(OCH2O)-Ph | 0.9 |
| 200 | F | H | H | 2-F-Ph | 0.3 |
| 201 | F | H | H | 3-F-Ph | 0.1 |
| 202 | F | H | H | 4-F-Ph | 1.0 |
| 203 | F | H | H | 2-pyridyl | 22.9 |
| 204 | F | H | H | 3-pyridyl | 2.5 |
| 205 | F | H | H | 2-thiazolyl | 14.6 |

Inhibition of VSV replication in MDCK epithelial cells.