Table 3. SAR of Biaryl Side Chain Derivatives with Second Phenyl Ring Meta to the Amide.

| entry | R1 | R2 | R3 | R4 | R5 | IC50 |
|---|---|---|---|---|---|---|
| 7h | H | OMe | H | H | H | 4.83 ± 0.9 μM |
| 16a | H | H | H | H | H | >10 μM |
| 16b | OMe | H | H | H | H | 9.65 ± 0.1 μM |
| 16c | OH | H | H | H | H | >10 μM |
| 16d | OMe | OMe | H | H | H | >10 μM |
| 16e | OMe | H | H | H | OMe | 9.05 ± 0.4 μM |
| 16f | H | OH | H | H | H | >10 μM |
| 16g | H | N(Me)2 | H | H | H | 3.36 ± 0.3 μM |
| 16h | H | NH2 | H | H | H | 7.23 ± 0.6 μM |
| 16i | H | CH2OH | H | H | H | >10 μM |
| 16j | H | Cl | H | H | H | >10 μM |
| 16k | H | F | H | H | H | >10 μM |
| 16l | H | CF3 | H | H | H | >10 μM |
| 16m | H | CF3 | Cl | H | H | >10 μM |
| 16n | H | Cl | Cl | H | H | >10 μM |
| 16o | H | H | Cl | H | H | >10 μM |
| 16p | H | H | CF3 | H | H | >10 μM |
| 16q | H | H | OMe | H | H | >10 μM |
| 16r | H | H | OH | H | H | 6.39 ± 1.4 μM |