Table 17. mGlu5 Potency in the N,N′-(1,3-Phenylene)Diamide Series.
| entry | R1 | R2 | mGlu5 IC50 (nM) |
|---|---|---|---|
| 240 | 2-OMe | 3-chlorophenyl | 880 |
| 241 | 2-OMe | 2-chlorophenyl | >30 000 |
| 242 | 2-OMe | 4-chlorophenyl | >30 000 |
| 243 | 2-OMe | 3-fluorophenyl | 6480 |
| 244 | 2-OMe | 3-methylphenyl | 1350 |
| 245 | 2-OMe | 3-(CF3)phenyl | 10,600 |
| 246 | 2-OMe | 3-cyanophenyl | 1800 |
| 247 | 2-OMe | benzyl | >30 000 |
| 248 | 3-Cl | 2-chlorophenyl | 2620 |
| 249 | 3-Cl | 3-chlorophenyl | >30 000 |
| 250 | 3-Cl | 2-furyl | 4510 |
| 251 | 3-Cl | cyclopentyl | >30 000 |
| 252 | 3-Cl | cyclobutyl | 5270 |
| 253 | 3-Cl | cyclopropyl | 2230 |
| 254 | 3-Cl | isonicotinamide | PAM |
| 255 | 3-Cl | nicotinamide | PAM |